Homo sapiens (Human) dipeptidyl peptidase IV (DPP4), T-cell activation antigen CD26
Dipeptidyl peptidase 4 regulates various physiological processes by cleaving peptides in the circulation, including many chemokines, mitogenic growth factors, neuropeptides and peptide hormones. Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline. Cleaves glucagon like peptide. This activity is inhibited by incretin fo example, reducing hyperglycemia without inducing hypoglycemia used in type 2 diabetes mellitus. DPP4 also acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor\/CD3-dependent manner ADABP Adenosine deaminase complexing protein 2. The novel emerging coronavirus Middle East respiratory syndrome coronavirus (MERS-CoV) binds cells through DPP4. Inhibition of CD26\/DPP4 ameliorates lipopolysaccharide (LPS)-induced lung injury in mice, with anti-inflammatory effects on the lungs endothelial cells. CD26\/DPP4 mediates inflammatory responses in the pulmonary endothelium
Family : DPP4N_Peptidase_S9
Block : X
Position in NCBI Life Tree : Homo sapiens
(Below N is a link to NCBI taxonomic web page and E link to ESTHER at designed phylum.)
> cellular organisms N E > Eukaryota N E > Opisthokonta N E > Metazoa N E > Eumetazoa N E > Bilateria N E > Deuterostomia N E > Chordata N E > Craniata N E > Vertebrata N E > Gnathostomata N E > Teleostomi N E > Euteleostomi N E > Sarcopterygii N E > Dipnotetrapodomorpha N E > Tetrapoda N E > Amniota N E > Mammalia N E > Theria N E > Eutheria N E > Boreoeutheria N E > Euarchontoglires N E > Primates N E > Haplorrhini N E > Simiiformes N E > Catarrhini N E > Hominoidea N E > Hominidae N E > Homininae N E > Homo N E > Homo sapiens N EMKTPWRVLLG LLGAAALVTI ITVPVVLLNK GTDDATADSR KTYTLTDYLK NTYRLKLYSL RWISDHEYLY KQENNILVFN AEYGNSSVFL ENSTFDEFGH SINDYSISPD GQFILLEYNY VKQWRHSYTA SYDIYDLNKR QLITEERIPN NTQWVTWSPV GHKLAYVWNN DIYVKIEPNL PSYRITWTGK EDIIYNGITD WVYEEEVFSA YSALWWSPNG TFLAYAQFND TEVPLIEYSF YSDESLQYPK TVRVPYPKAG AVNPTVKFFV VNTDSLSSVT NATSIQITAP ASMLIGDHYL CDVTWATQER ISLQWLRRIQ NYSVMDICDY DESSGRWNCL VARQHIEMST TGWVGRFRPS EPHFTLDGNS FYKIISNEEG YRHICYFQID KKDCTFITKG TWEVIGIEAL TSDYLYYISN EYKGMPGGRN LYKIQLSDYT KVTCLSCELN PERCQYYSVS FSKEAKYYQL RCSGPGLPLY TLHSSVNDKG LRVLEDNSAL DKMLQNVQMP SKKLDFIILN ETKFWYQMIL PPHFDKSKKY PLLLDVYAGP CSQKADIVFR LNWATYLAST ENIIVASFDG RGSGYQGDKI MHAINRRLGT FEVEDQIEAA RQFSKMGFVD NKRIAIWGWS YGGYVTSMVL GSGSGVFKCG IAVAPVSRWE YYESVYTERY MGLPTPEDNL DHYRNSTVMS RAENFKQVEY LLIHGTADDN VHFQQSAQIS KALVDVGVDF QAMWYTDEDH GIASSTAHQH IYTHMSHFIK QCFSLP
Title : CAR-macrophages targets CD26 to eliminate chronic myeloid leukemia stem cells - Guoyun_2025_Exp.Hematol.Oncol_14_14 |
Author(s) : Guoyun J , Yuefeng Q , Zhenglan H , Zuowei Y , Hongyan Z , Ying Y , Wenli F |
Ref : Experimental Hematology Oncol , 14 :14 , 2025 |
Abstract : |
PubMedSearch : Guoyun_2025_Exp.Hematol.Oncol_14_14 |
PubMedID: 39948620 |
Gene_locus related to this paper: human-DPP4 |
Title : alpha-chaconine increases the sensitivity of HER2+ breast cancer cells to trastuzumab by targeting acetylcholinesterase - Hermawan_2025_Comput.Biol.Med_188_109809 |
Author(s) : Hermawan A , Pamungkas Putri DD , Fatimah N , Rhamandana Putra IM , Lestari IA |
Ref : Computers in Biology & Medicine , 188 :109809 , 2025 |
Abstract : |
PubMedSearch : Hermawan_2025_Comput.Biol.Med_188_109809 |
PubMedID: 39955879 |
Gene_locus related to this paper: human-DPP4 |
Title : Macrocyclic phage display for identification of selective protease substrates - Faucher_2025_bioRxiv__ |
Author(s) : Faucher FF , Lovell S , Bertolini M , Blazkova K , Cosco ED , Bogyo M , Barniol-Xicota M |
Ref : Biorxiv , : , 2025 |
Abstract : |
PubMedSearch : Faucher_2025_bioRxiv__ |
PubMedID: 40161698 |
Gene_locus related to this paper: human-DPP4 , human-FAP |
Title : Sulphostin-inspired N-phosphonopiperidones as selective covalent DPP8 and DPP9 inhibitors - Sewald_2025_Nat.Commun_16_3208 |
Author(s) : Sewald L , Tabak WWA , Fehr L , Zolg S , Najdzion M , Verhoef CJA , Podlesainski D , Geiss-Friedlander R , Lammens A , Kaschani F , Hellerschmied D , Huber R , Kaiser M |
Ref : Nat Commun , 16 :3208 , 2025 |
Abstract : |
PubMedSearch : Sewald_2025_Nat.Commun_16_3208 |
PubMedID: 40180908 |
Gene_locus related to this paper: human-DPP4 , human-DPP8 , human-DPP9 |
Title : Contribution of amino acids in the active site of dipeptidyl peptidase 4 to the catalytic action of the enzyme - Gnoth_2024_PLoS.One_19_e0289239 |
Author(s) : Gnoth K , Bar JW , Rosche F , Rahfeld JU , Demuth HU |
Ref : PLoS ONE , 19 :e0289239 , 2024 |
Abstract : |
PubMedSearch : Gnoth_2024_PLoS.One_19_e0289239 |
PubMedID: 38625918 |
Gene_locus related to this paper: human-DPP4 |
Title : A novel bifunctional peptide VAMP mined from hemp seed protein hydrolysates improves glucose homeostasis by inhibiting intestinal DPP-IV and increasing the abundance of Akkermansia muciniphila - Chen_2024_Biorxiv__ |
Author(s) : Chen H , Li W , Hu W , Xu B , Wang Y , Liu J , Zhang C , Zhang X , Nie Q , Xing XH |
Ref : Biorxiv , : , 2024 |
Abstract : |
PubMedSearch : Chen_2024_Biorxiv__ |
PubMedID: |
Gene_locus related to this paper: human-DPP4 |
Title : Dipeptidyl Peptidase 4 (DPP4) Exacerbates Osteoarthritis Progression in an Enzyme-Independent Manner - Li_2024_Adv.Sci.(Weinh)__e2410525 |
Author(s) : Li X , Zhang Z , Jiang W , Ju Y , Guo W , Huang Z |
Ref : Adv Sci (Weinh) , :e2410525 , 2024 |
Abstract : |
PubMedSearch : Li_2024_Adv.Sci.(Weinh)__e2410525 |
PubMedID: 39680708 |
Gene_locus related to this paper: human-DPP4 |
Title : Transcriptome Analysis of Fibroblasts in Hypoxia-Induced Vascular Remodeling: Functional Roles of CD26\/DPP4 - Suzuki_2024_Int.J.Mol.Sci_25_12599 |
Author(s) : Suzuki Y , Kawasaki T , Tatsumi K , Okaya T , Sato S , Shimada A , Misawa T , Hatano R , Morimoto C , Kasuya Y , Hasegawa Y , Ohara O , Suzuki T |
Ref : Int J Mol Sci , 25 : , 2024 |
Abstract : |
PubMedSearch : Suzuki_2024_Int.J.Mol.Sci_25_12599 |
PubMedID: 39684311 |
Gene_locus related to this paper: human-DPP4 |
Title : High-Throughput Screening of DPPIV Inhibitors Antagonizing GLP-1 Degradation Using an Enzymatic Activated Fluorescent Probe - Zhang_2024_Anal.Chem__ |
Author(s) : Zhang M , He S , Han C , Wu Y , Cui J , Feng L , Huo X , Li D , Chen Q , Ma X , Wang C |
Ref : Analytical Chemistry , : , 2024 |
Abstract : |
PubMedSearch : Zhang_2024_Anal.Chem__ |
PubMedID: 39733350 |
Gene_locus related to this paper: human-DPP4 |
Title : Molecular insights on the coronavirus MERS-CoV interaction with the CD26 receptor - Failayev_2024_Virus.Res__199330 |
Author(s) : Failayev H , Ganoth A , Tsfadia Y |
Ref : Virus Res , :199330 , 2024 |
Abstract : |
PubMedSearch : Failayev_2024_Virus.Res__199330 |
PubMedID: 38272241 |
Gene_locus related to this paper: human-DPP4 |
Title : Deep quantification of substrate turnover defines protease subsite cooperativity - Gudipati_2024_Mol.Syst.Biol__ |
Author(s) : Gudipati RK , Gaidatzis D , Seebacher J , Muehlhaeusser S , Kempf G , Cavadini S , Hess D , Soneson C , Grosshans H |
Ref : Mol Syst Biol , : , 2024 |
Abstract : |
PubMedSearch : Gudipati_2024_Mol.Syst.Biol__ |
PubMedID: 39468329 |
Gene_locus related to this paper: caeel-K02F2.1 , human-DPP4 |
Title : Targeting DPP4-RBD interactions by sitagliptin and linagliptin delivers a potential host-directed therapy against pan-SARS-CoV-2 infections - Mani_2023_Int.J.Biol.Macromol_245_125444 |
Author(s) : Mani S , Kaur A , Jakhar K , Kumari G , Sonar S , Kumar A , Das S , Kumar S , Kumar V , Kundu R , Pandey AK , Singh UP , Majumdar T |
Ref : Int J Biol Macromol , 245 :125444 , 2023 |
Abstract : |
PubMedSearch : Mani_2023_Int.J.Biol.Macromol_245_125444 |
PubMedID: 37385308 |
Gene_locus related to this paper: human-DPP4 |
Title : A review upon medicinal perspective and designing rationale of DPP-4 inhibitors - Kumar_2021_Bioorg.Med.Chem_46_116354 |
Author(s) : Kumar S , Mittal A |
Ref : Bioorganic & Medicinal Chemistry , 46 :116354 , 2021 |
Abstract : |
PubMedSearch : Kumar_2021_Bioorg.Med.Chem_46_116354 |
PubMedID: 34428715 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes - Li_2019_J.Med.Chem_62_2348 |
Author(s) : Li S , Qin C , Cui S , Xu H , Wu F , Wang J , Su M , Fang X , Li D , Jiao Q , Zhang M , Xia C , Zhu L , Wang R , Li J , Jiang H , Zhao Z , Li H |
Ref : Journal of Medicinal Chemistry , 62 :2348 , 2019 |
Abstract : |
PubMedSearch : Li_2019_J.Med.Chem_62_2348 |
PubMedID: 30694668 |
Gene_locus related to this paper: human-DPP4 |
Title : A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice - Berger_2018_Endocrinol.Diabetes.Metab_1_e00002 |
Author(s) : Berger JP , SinhaRoy R , Pocai A , Kelly TM , Scapin G , Gao YD , Pryor KAD , Wu JK , Eiermann GJ , Xu SS , Zhang X , Tatosian DA , Weber AE , Thornberry NA , Carr RD |
Ref : Endocrinol Diabetes Metab , 1 :e00002 , 2018 |
Abstract : |
PubMedSearch : Berger_2018_Endocrinol.Diabetes.Metab_1_e00002 |
PubMedID: 30815539 |
Gene_locus related to this paper: human-DPP4 |
Title : Unique binding mode of Evogliptin with human dipeptidyl peptidase IV - Lee_2017_Biochem.Biophys.Res.Commun_494_452 |
Author(s) : Lee HK , Kim MK , Kim HD , Kim HJ , Kim JW , Lee JO , Kim CW , Kim EE |
Ref : Biochemical & Biophysical Research Communications , 494 :452 , 2017 |
Abstract : |
PubMedSearch : Lee_2017_Biochem.Biophys.Res.Commun_494_452 |
PubMedID: 29061303 |
Gene_locus related to this paper: human-DPP4 |
Title : Mapping the Specific Amino Acid Residues That Make Hamster DPP4 Functional as a Receptor for Middle East Respiratory Syndrome Coronavirus - van Doremalen_2016_J.Virol_90_5499 |
Author(s) : van Doremalen N , Miazgowicz KL , Munster VJ |
Ref : J Virol , 90 :5499 , 2016 |
Abstract : |
PubMedSearch : van Doremalen_2016_J.Virol_90_5499 |
PubMedID: 27030263 |
Gene_locus related to this paper: human-DPP4 |
Title : The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors - Cox_2016_Bioorg.Med.Chem.Lett_26_2622 |
Author(s) : Cox JM , Chu HD , Kuethe JT , Gao YD , Scapin G , Eiermann G , He H , Li X , Lyons KA , Metzger J , Petrov A , Wu JK , Xu S , Sinha-Roy R , Weber AE , Biftu T |
Ref : Bioorganic & Medicinal Chemistry Lett , 26 :2622 , 2016 |
Abstract : |
PubMedSearch : Cox_2016_Bioorg.Med.Chem.Lett_26_2622 |
PubMedID: 27106708 |
Gene_locus related to this paper: human-DPP4 |
Title : Scaffold-hopping from xanthines to tricyclic guanines: A case study of dipeptidyl peptidase 4 (DPP4) inhibitors - Pissarnitski_2016_Bioorg.Med.Chem_24_5534 |
Author(s) : Pissarnitski DA , Zhao Z , Cole D , Wu WL , Domalski M , Clader JW , Scapin G , Voigt J , Soriano A , Kelly T , Powles MA , Yao Z , Burnett DA |
Ref : Bioorganic & Medicinal Chemistry , 24 :5534 , 2016 |
Abstract : |
PubMedSearch : Pissarnitski_2016_Bioorg.Med.Chem_24_5534 |
PubMedID: 27670099 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes - Li_2016_J.Med.Chem_59_6772 |
Author(s) : Li S , Xu H , Cui S , Wu F , Zhang Y , Su M , Gong Y , Qiu S , Jiao Q , Qin C , Shan J , Zhang M , Wang J , Yin Q , Xu M , Liu X , Wang R , Zhu L , Li J , Xu Y , Jiang H , Zhao Z , Li H |
Ref : Journal of Medicinal Chemistry , 59 :6772 , 2016 |
Abstract : |
PubMedSearch : Li_2016_J.Med.Chem_59_6772 |
PubMedID: 27396490 |
Gene_locus related to this paper: human-DPP4 |
Title : Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism - Grimshaw_2016_PLoS.One_11_e0157509 |
Author(s) : Grimshaw CE , Jennings A , Kamran R , Ueno H , Nishigaki N , Kosaka T , Tani A , Sano H , Kinugawa Y , Koumura E , Shi L , Takeuchi K |
Ref : PLoS ONE , 11 :e0157509 , 2016 |
Abstract : |
PubMedSearch : Grimshaw_2016_PLoS.One_11_e0157509 |
PubMedID: 27328054 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes - Wu_2016_ACS.Med.Chem.Lett_7_498 |
Author(s) : Wu WL , Hao J , Domalski M , Burnett DA , Pissarnitski D , Zhao Z , Stamford A , Scapin G , Gao YD , Soriano A , Kelly TM , Yao Z , Powles MA , Chen S , Mei H , Hwa J |
Ref : ACS Med Chem Lett , 7 :498 , 2016 |
Abstract : |
PubMedSearch : Wu_2016_ACS.Med.Chem.Lett_7_498 |
PubMedID: 27190600 |
Gene_locus related to this paper: human-DPP4 |
Title : Anagliptin, a potent dipeptidyl peptidase IV inhibitor: its single-crystal structure and enzyme interactions - Watanabe_2015_J.Enzyme.Inhib.Med.Chem_30_981 |
Author(s) : Watanabe YS , Yasuda Y , Kojima Y , Okada S , Motoyama T , Takahashi R , Oka M |
Ref : J Enzyme Inhib Med Chem , 30 :981 , 2015 |
Abstract : |
PubMedSearch : Watanabe_2015_J.Enzyme.Inhib.Med.Chem_30_981 |
PubMedID: 26147347 |
Gene_locus related to this paper: human-DPP4 |
Title : Identification of residues on human receptor DPP4 critical for MERS-CoV binding and entry - Song_2014_Virology_471-473C_49 |
Author(s) : Song W , Wang Y , Wang N , Wang D , Guo J , Fu L , Shi X |
Ref : Virology , 471-473C :49 , 2014 |
Abstract : |
PubMedSearch : Song_2014_Virology_471-473C_49 |
PubMedID: 25461530 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold - Xiao_2014_Chin.Chem.Lett_25_673 |
Author(s) : Xiao P , Guo R , Huang S , Cui H , Ye S , Zhang Z |
Ref : Chin Chem Lett , 25 :673 , 2014 |
Abstract : |
PubMedSearch : Xiao_2014_Chin.Chem.Lett_25_673 |
PubMedID: |
Gene_locus related to this paper: human-DPP4 |
Title : Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes - Biftu_2014_J.Med.Chem_57_3205 |
Author(s) : Biftu T , Sinha-Roy R , Chen P , Qian X , Feng D , Kuethe JT , Scapin G , Gao YD , Yan Y , Krueger D , Bak A , Eiermann G , He J , Cox J , Hicks J , Lyons K , He H , Salituro G , Tong S , Patel S , Doss G , Petrov A , Wu J , Xu SS , Sewall C , Zhang X , Zhang B , Thornberry NA , Weber AE |
Ref : Journal of Medicinal Chemistry , 57 :3205 , 2014 |
Abstract : |
PubMedSearch : Biftu_2014_J.Med.Chem_57_3205 |
PubMedID: 24660890 |
Gene_locus related to this paper: human-DPP4 |
Title : Bat origins of MERS-CoV supported by bat coronavirus HKU4 usage of human receptor CD26 - Wang_2014_Cell.Host.Microbe_16_328 |
Author(s) : Wang Q , Qi J , Yuan Y , Xuan Y , Han P , Wan Y , Ji W , Li Y , Wu Y , Wang J , Iwamoto A , Woo PC , Yuen KY , Yan J , Lu G , Gao GF |
Ref : Cell Host Microbe , 16 :328 , 2014 |
Abstract : |
PubMedSearch : Wang_2014_Cell.Host.Microbe_16_328 |
PubMedID: 25211075 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV - Namoto_2014_Bioorg.Med.Chem.Lett_24_731 |
Author(s) : Namoto K , Sirockin F , Ostermann N , Gessier F , Flohr S , Sedrani R , Gerhartz B , Trappe J , Hassiepen U , Duttaroy A , Ferreira S , Sutton JM , Clark DE , Fenton G , Beswick M , Baeschlin DK |
Ref : Bioorganic & Medicinal Chemistry Lett , 24 :731 , 2014 |
Abstract : |
PubMedSearch : Namoto_2014_Bioorg.Med.Chem.Lett_24_731 |
PubMedID: 24439847 |
Gene_locus related to this paper: human-DPP4 |
Title : Molecular basis of binding between novel human coronavirus MERS-CoV and its receptor CD26 - Lu_2013_Nature_500_227 |
Author(s) : Lu G , Hu Y , Wang Q , Qi J , Gao F , Li Y , Zhang Y , Zhang W , Yuan Y , Bao J , Zhang B , Shi Y , Yan J , Gao GF |
Ref : Nature , 500 :227 , 2013 |
Abstract : |
PubMedSearch : Lu_2013_Nature_500_227 |
PubMedID: 23831647 |
Gene_locus related to this paper: human-DPP4 |
Title : Structure of MERS-CoV spike receptor-binding domain complexed with human receptor DPP4 - Wang_2013_Cell.Res_23_986 |
Author(s) : Wang N , Shi X , Jiang L , Zhang S , Wang D , Tong P , Guo D , Fu L , Cui Y , Liu X , Arledge KC , Chen YH , Zhang L , Wang X |
Ref : Cell Res , 23 :986 , 2013 |
Abstract : |
PubMedSearch : Wang_2013_Cell.Res_23_986 |
PubMedID: 23835475 |
Gene_locus related to this paper: human-DPP4 |
Title : Design and synthesis of 4-(2,4,5-trifluorophenyl)butane-1,3-diamines as dipeptidyl peptidase IV inhibitors - Zhu_2013_ChemMedChem_8_1104 |
Author(s) : Zhu L , Li Y , Qiu L , Su M , Wang X , Xia C , Qu Y , Li J , Xiong B , Shen J |
Ref : ChemMedChem , 8 :1104 , 2013 |
Abstract : |
PubMedSearch : Zhu_2013_ChemMedChem_8_1104 |
PubMedID: 23671024 |
Gene_locus related to this paper: human-DPP4 |
Title : A Comparative Study of the Binding Modes of Recently Launched Dipeptidyl Peptidase IV Inhibitors in the Active Site - Nabeno_2013_Biochem.Biophys.Res.Commun_434_191 |
Author(s) : Nabeno M , Akahoshi F , Kishida H , Miyaguchi I , Tanaka Y , Ishii S , Kadowaki T |
Ref : Biochemical & Biophysical Research Communications , 434 :191 , 2013 |
Abstract : |
PubMedSearch : Nabeno_2013_Biochem.Biophys.Res.Commun_434_191 |
PubMedID: 23501107 |
Gene_locus related to this paper: human-DPP4 |
Title : Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]py ridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778) - Devasthale_2013_J.Med.Chem_56_7343 |
Author(s) : Devasthale P , Wang Y , Wang W , Fevig J , Feng J , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Moulin F , Li YX , Zahler R , Kirby MS , Hamann LG |
Ref : Journal of Medicinal Chemistry , 56 :7343 , 2013 |
Abstract : |
PubMedSearch : Devasthale_2013_J.Med.Chem_56_7343 |
PubMedID: 23964740 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-y lcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Yoshida_2012_Bioorg.Med.Chem_20_5705 |
Author(s) : Yoshida T , Akahoshi F , Sakashita H , Kitajima H , Nakamura M , Sonda S , Takeuchi M , Tanaka Y , Ueda N , Sekiguchi S , Ishige T , Shima K , Nabeno M , Abe Y , Anabuki J , Soejima A , Yoshida K , Takashina Y , Ishii S , Kiuchi S , Fukuda S , Tsutsumiuchi R , Kosaka K , Murozono T , Nakamaru Y , Utsumi H , Masutomi N , Kishida H , Miyaguchi I , Hayashi Y |
Ref : Bioorganic & Medicinal Chemistry , 20 :5705 , 2012 |
Abstract : |
PubMedSearch : Yoshida_2012_Bioorg.Med.Chem_20_5705 |
PubMedID: 22959556 |
Gene_locus related to this paper: human-DPP4 |
Title : Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors - Lam_2012_Bioorg.Med.Chem.Lett_22_6628 |
Author(s) : Lam B , Zhang Z , Stafford JA , Skene RJ , Shi L , Gwaltney SL, 2nd |
Ref : Bioorganic & Medicinal Chemistry Lett , 22 :6628 , 2012 |
Abstract : |
PubMedSearch : Lam_2012_Bioorg.Med.Chem.Lett_22_6628 |
PubMedID: 23025999 |
Gene_locus related to this paper: human-DPP4 |
Title : Fused bicyclic heteroarylpiperazine-substituted L-prolylthiazolidines as highly potent DPP-4 inhibitors lacking the electrophilic nitrile group - Yoshida_2012_Bioorg.Med.Chem_20_5033 |
Author(s) : Yoshida T , Akahoshi F , Sakashita H , Sonda S , Takeuchi M , Tanaka Y , Nabeno M , Kishida H , Miyaguchi I , Hayashi Y |
Ref : Bioorganic & Medicinal Chemistry , 20 :5033 , 2012 |
Abstract : |
PubMedSearch : Yoshida_2012_Bioorg.Med.Chem_20_5033 |
PubMedID: 22824762 |
Gene_locus related to this paper: human-DPP4 |
Title : Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes. - Sutton_2012_Bioorg.Med.Chem.Lett_22_1464 |
Author(s) : Sutton JM , Clark DE , Dunsdon SJ , Fenton G , Fillmore A , Harris NV , Higgs C , Hurley CA , Krintel SL , Mackenzie RE , Duttaroy A , Gangl E , Maniara W , Sedrani R , Namoto K , Ostermann N , Gerhartz B , Sirockin F , Trappe J , Hassiepen U , Baeschlin DK |
Ref : Bioorganic & Medicinal Chemistry Lett , 22 :1464 , 2012 |
Abstract : |
PubMedSearch : Sutton_2012_Bioorg.Med.Chem.Lett_22_1464 |
PubMedID: 22177783 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of beta-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors - Park_2011_Bioorg.Med.Chem.Lett_21_1366 |
Author(s) : Park WS , Kang SK , Jun MA , Shin MS , Kim KY , Rhee SD , Bae MA , Kim MS , Kim KR , Kang NS , Yoo SE , Lee JO , Song DH , Silinski P , Schneider SE , Ahn JH , Kim SS |
Ref : Bioorganic & Medicinal Chemistry Lett , 21 :1366 , 2011 |
Abstract : |
PubMedSearch : Park_2011_Bioorg.Med.Chem.Lett_21_1366 |
PubMedID: 21306895 |
Gene_locus related to this paper: human-DPP4 |
Title : Role of a propeller loop in the quaternary structure and enzymatic activity of prolyl dipeptidases DPP-IV and DPP9 - Tang_2011_FEBS.Lett_585_3409 |
Author(s) : Tang HK , Chen KC , Liou GG , Cheng SC , Chien CH , Tang HY , Huang LH , Chang HP , Chou CY , Chen X |
Ref : FEBS Letters , 585 :3409 , 2011 |
Abstract : |
PubMedSearch : Tang_2011_FEBS.Lett_585_3409 |
PubMedID: 22001206 |
Gene_locus related to this paper: human-DPP4 , human-DPP9 |
Title : Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV - Zhang_2011_J.Med.Chem_54_510 |
Author(s) : Zhang Z , Wallace MB , Feng J , Stafford JA , Skene RJ , Shi L , Lee B , Aertgeerts K , Jennings A , Xu R , Kassel DB , Kaldor SW , Navre M , Webb DR , Gwaltney SL |
Ref : Journal of Medicinal Chemistry , 54 :510 , 2011 |
Abstract : |
PubMedSearch : Zhang_2011_J.Med.Chem_54_510 |
PubMedID: 21186796 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor - Miyamoto_2011_J.Med.Chem_54_831 |
Author(s) : Miyamoto Y , Banno Y , Yamashita T , Fujimoto T , Oi S , Moritoh Y , Asakawa T , Kataoka O , Yashiro H , Takeuchi K , Suzuki N , Ikedo K , Kosaka T , Tsubotani S , Tani A , Sasaki M , Funami M , Amano M , Yamamoto Y , Aertgeerts K , Yano J , Maezaki H |
Ref : Journal of Medicinal Chemistry , 54 :831 , 2011 |
Abstract : |
PubMedSearch : Miyamoto_2011_J.Med.Chem_54_831 |
PubMedID: 21218817 |
Gene_locus related to this paper: human-DPP4 |
Title : 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site - Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
Author(s) : Wang W , Devasthale P , Wang A , Harrity T , Egan D , Morgan N , Cap M , Fura A , Klei HE , Kish K , Weigelt C , Sun L , Levesque P , Li YX , Zahler R , Kirby MS , Hamann LG |
Ref : Bioorganic & Medicinal Chemistry Lett , 21 :6646 , 2011 |
Abstract : |
PubMedSearch : Wang_2011_Bioorg.Med.Chem.Lett_21_6646 |
PubMedID: 21996520 |
Gene_locus related to this paper: human-DPP4 |
Title : Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554 - Banno_2011_Bioorg.Med.Chem_19_4953 |
Author(s) : Banno Y , Miyamoto Y , Sasaki M , Oi S , Asakawa T , Kataoka O , Takeuchi K , Suzuki N , Ikedo K , Kosaka T , Tsubotani S , Tani A , Funami M , Tawada M , Yamamoto Y , Aertgeerts K , Yano J , Maezaki H |
Ref : Bioorganic & Medicinal Chemistry , 19 :4953 , 2011 |
Abstract : |
PubMedSearch : Banno_2011_Bioorg.Med.Chem_19_4953 |
PubMedID: 21764322 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554 - Maezaki_2011_Bioorg.Med.Chem_19_4482 |
Author(s) : Maezaki H , Banno Y , Miyamoto Y , Moritoh Y , Asakawa T , Kataoka O , Takeuchi K , Suzuki N , Ikedo K , Kosaka T , Sasaki M , Tsubotani S , Tani A , Funami M , Yamamoto Y , Tawada M , Aertgeerts K , Yano J , Oi S |
Ref : Bioorganic & Medicinal Chemistry , 19 :4482 , 2011 |
Abstract : |
PubMedSearch : Maezaki_2011_Bioorg.Med.Chem_19_4482 |
PubMedID: 21741847 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxa mides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors - Meng_2010_J.Med.Chem_53_5620 |
Author(s) : Meng W , Brigance RP , Chao HJ , Fura A , Harrity T , Marcinkeviciene J , O'Connor SP , Tamura JK , Xie D , Zhang Y , Klei HE , Kish K , Weigelt CA , Turdi H , Wang A , Zahler R , Kirby MS , Hamann LG |
Ref : Journal of Medicinal Chemistry , 53 :5620 , 2010 |
Abstract : |
PubMedSearch : Meng_2010_J.Med.Chem_53_5620 |
PubMedID: 20684603 |
Gene_locus related to this paper: human-DPP4 |
Title : Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors - Boehringer_2010_Bioorg.Med.Chem.Lett_20_1106 |
Author(s) : Boehringer M , Fischer H , Hennig M , Hunziker D , Huwyler J , Kuhn B , Loeffler BM , Luebbers T , Mattei P , Narquizian R , Sebokova E , Sprecher U , Wessel HP |
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :1106 , 2010 |
Abstract : |
PubMedSearch : Boehringer_2010_Bioorg.Med.Chem.Lett_20_1106 |
PubMedID: 20031408 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Mattei_2010_Bioorg.Med.Chem.Lett_20_1109 |
Author(s) : Mattei P , Boehringer M , Di Giorgio P , Fischer H , Hennig M , Huwyler J , Kocer B , Kuhn B , Loeffler BM , Macdonald A , Narquizian R , Rauber E , Sebokova E , Sprecher U |
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :1109 , 2010 |
Abstract : |
PubMedSearch : Mattei_2010_Bioorg.Med.Chem.Lett_20_1109 |
PubMedID: 20031405 |
Gene_locus related to this paper: human-DPP4 |
Title : (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrr olidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor - Ammirati_2009_Bioorg.Med.Chem.Lett_19_1991 |
Author(s) : Ammirati MJ , Andrews KM , Boyer DD , Brodeur AM , Danley DE , Doran SD , Hulin B , Liu S , McPherson RK , Orena SJ , Parker JC , Polivkova J , Qiu X , Soglia CB , Treadway JL , VanVolkenburg MA , Wilder DC , Piotrowski DW |
Ref : Bioorganic & Medicinal Chemistry Lett , 19 :1991 , 2009 |
Abstract : |
PubMedSearch : Ammirati_2009_Bioorg.Med.Chem.Lett_19_1991 |
PubMedID: 19275964 |
Gene_locus related to this paper: human-DPP4 |
Title : Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors - Edmondson_2009_Bioorg.Med.Chem.Lett_19_4097 |
Author(s) : Edmondson SD , Mastracchio A , Cox JM , Eiermann GJ , He H , Lyons KA , Patel RA , Patel SB , Petrov A , Scapin G , Wu JK , Xu S , Zhu B , Thornberry NA , Roy RS , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 19 :4097 , 2009 |
Abstract : |
PubMedSearch : Edmondson_2009_Bioorg.Med.Chem.Lett_19_4097 |
PubMedID: 19539471 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV - Nordhoff_2009_Bioorg.Med.Chem.Lett_19_4201 |
Author(s) : Nordhoff S , Cerezo-Galvez S , Deppe H , Hill O , Lopez-Canet M , Rummey C , Thiemann M , Matassa VG , Edwards PJ , Feurer A |
Ref : Bioorganic & Medicinal Chemistry Lett , 19 :4201 , 2009 |
Abstract : |
PubMedSearch : Nordhoff_2009_Bioorg.Med.Chem.Lett_19_4201 |
PubMedID: 19515557 |
Gene_locus related to this paper: human-DPP4 |
Title : Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors - Wallace_2008_Bioorg.Med.Chem.Lett_18_2362 |
Author(s) : Wallace MB , Feng J , Zhang Z , Skene RJ , Shi L , Caster CL , Kassel DB , Xu R , Gwaltney SL, 2nd |
Ref : Bioorganic & Medicinal Chemistry Lett , 18 :2362 , 2008 |
Abstract : |
PubMedSearch : Wallace_2008_Bioorg.Med.Chem.Lett_18_2362 |
PubMedID: 18346892 |
Gene_locus related to this paper: human-DPP4 |
Title : Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors - Ahn_2008_Bioorg.Med.Chem.Lett_18_6525 |
Author(s) : Ahn JH , Park WS , Jun MA , Shin MS , Kang SK , Kim KY , Rhee SD , Bae MA , Kim KR , Kim SG , Kim SY , Sohn SK , Kang NS , Lee JO , Lee DH , Cheon HG , Kim SS |
Ref : Bioorganic & Medicinal Chemistry Lett , 18 :6525 , 2008 |
Abstract : |
PubMedSearch : Ahn_2008_Bioorg.Med.Chem.Lett_18_6525 |
PubMedID: 18996694 |
Gene_locus related to this paper: human-DPP4 |
Title : Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors - Edmondson_2008_Bioorg.Med.Chem.Lett_18_2409 |
Author(s) : Edmondson SD , Wei L , Xu J , Shang J , Xu S , Pang J , Chaudhary A , Dean DC , He H , Leiting B , Lyons KA , Patel RA , Patel SB , Scapin G , Wu JK , Beconi MG , Thornberry NA , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 18 :2409 , 2008 |
Abstract : |
PubMedSearch : Edmondson_2008_Bioorg.Med.Chem.Lett_18_2409 |
PubMedID: 18331795 |
Gene_locus related to this paper: human-DPP4 |
Title : Synthesis and biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors - Jun_2008_Eur.J.Med.Chem_43_1889 |
Author(s) : Jun MA , Park WS , Kang SK , Kim KY , Kim KR , Rhee SD , Bae MA , Kang NS , Sohn SK , Kim SG , Lee JO , Lee DH , Cheon HG , Kim SS , Ahn JH |
Ref : Eur Journal of Medicinal Chemistry , 43 :1889 , 2008 |
Abstract : |
PubMedSearch : Jun_2008_Eur.J.Med.Chem_43_1889 |
PubMedID: 18243422 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design - Liang_2008_Bioorg.Med.Chem.Lett_18_3706 |
Author(s) : Liang GB , Qian X , Biftu T , Singh S , Gao YD , Scapin G , Patel S , Leiting B , Patel R , Wu J , Zhang X , Thornberry NA , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 18 :3706 , 2008 |
Abstract : |
PubMedSearch : Liang_2008_Bioorg.Med.Chem.Lett_18_3706 |
PubMedID: 18524582 |
Gene_locus related to this paper: human-DPP4 |
Title : Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation - Metzler_2008_Protein.Sci_17_240 |
Author(s) : Metzler WJ , Yanchunas J , Weigelt C , Kish K , Klei HE , Xie D , Zhang Y , Corbett M , Tamura JK , He B , Hamann LG , Kirby MS , Marcinkeviciene J |
Ref : Protein Science , 17 :240 , 2008 |
Abstract : |
PubMedSearch : Metzler_2008_Protein.Sci_17_240 |
PubMedID: 18227430 |
Gene_locus related to this paper: human-DPP4 |
Title : (3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization - Wright_2007_Bioorg.Med.Chem.Lett_17_5638 |
Author(s) : Wright SW , Ammirati MJ , Andrews KM , Brodeur AM , Danley DE , Doran SD , Lillquist JS , Liu S , McClure LD , McPherson RK , Olson TV , Orena SJ , Parker JC , Rocke BN , Soeller WC , Soglia CB , Treadway JL , VanVolkenburg MA , Zhao Z , Cox ED |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :5638 , 2007 |
Abstract : |
PubMedSearch : Wright_2007_Bioorg.Med.Chem.Lett_17_5638 |
PubMedID: 17822893 |
Gene_locus related to this paper: human-DPP4 |
Title : [(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors - Yoshida_2007_Bioorg.Med.Chem.Lett_17_2618 |
Author(s) : Yoshida T , Sakashita H , Akahoshi F , Hayashi Y |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2618 , 2007 |
Abstract : |
PubMedSearch : Yoshida_2007_Bioorg.Med.Chem.Lett_17_2618 |
PubMedID: 17317162 |
Gene_locus related to this paper: human-DPP4 |
Title : Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors - Kowalchick_2007_Bioorg.Med.Chem.Lett_17_5934 |
Author(s) : Kowalchick JE , Leiting B , Pryor KD , Marsilio F , Wu JK , He H , Lyons KA , Eiermann GJ , Petrov A , Scapin G , Patel RA , Thornberry NA , Weber AE , Kim D |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :5934 , 2007 |
Abstract : |
PubMedSearch : Kowalchick_2007_Bioorg.Med.Chem.Lett_17_5934 |
PubMedID: 17827003 |
Gene_locus related to this paper: human-DPP4 |
Title : 4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV - Kaelin_2007_Bioorg.Med.Chem.Lett_17_5806 |
Author(s) : Kaelin DE , Smenton AL , Eiermann GJ , He H , Leiting B , Lyons KA , Patel RA , Patel SB , Petrov A , Scapin G , Wu JK , Thornberry NA , Weber AE , Duffy JL |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :5806 , 2007 |
Abstract : |
PubMedSearch : Kaelin_2007_Bioorg.Med.Chem.Lett_17_5806 |
PubMedID: 17851076 |
Gene_locus related to this paper: human-DPP4 |
Title : 1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors - Lubbers_2007_Bioorg.Med.Chem.Lett_17_2966 |
Author(s) : Lubbers T , Bohringer M , Gobbi L , Hennig M , Hunziker D , Kuhn B , Loffler B , Mattei P , Narquizian R , Peters JU , Ruff Y , Wessel HP , Wyss P |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2966 , 2007 |
Abstract : |
PubMedSearch : Lubbers_2007_Bioorg.Med.Chem.Lett_17_2966 |
PubMedID: 17418568 |
Gene_locus related to this paper: human-DPP4 |
Title : Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors - Ahn_2007_Bioorg.Med.Chem.Lett_17_2622 |
Author(s) : Ahn JH , Shin MS , Jun MA , Jung SH , Kang SK , Kim KR , Rhee SD , Kang NS , Kim SY , Sohn SK , Kim SG , Jin MS , Lee JO , Cheon HG , Kim SS |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2622 , 2007 |
Abstract : |
PubMedSearch : Ahn_2007_Bioorg.Med.Chem.Lett_17_2622 |
PubMedID: 17331715 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site - Sheehan_2007_Bioorg.Med.Chem.Lett_17_1765 |
Author(s) : Sheehan SM , Mest HJ , Watson BM , Klimkowski VJ , Timm DE , Cauvin A , Parsons SH , Shi Q , Canada EJ , Wiley MR , Ruehter G , Evers B , Petersen S , Blaszczak LC , Pulley SR , Margolis BJ , Wishart GN , Renson B , Hankotius D , Mohr M , Zechel JC , Michael Kalbfleisch J , Dingess-Hammond EA , Boelke A , Weichert AG |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :1765 , 2007 |
Abstract : |
PubMedSearch : Sheehan_2007_Bioorg.Med.Chem.Lett_17_1765 |
PubMedID: 17239592 |
Gene_locus related to this paper: human-DPP4 |
Title : (3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)- 1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Biftu_2007_Bioorg.Med.Chem.Lett_17_49 |
Author(s) : Biftu T , Feng D , Qian X , Liang GB , Kieczykowski G , Eiermann G , He H , Leiting B , Lyons K , Petrov A , Sinha-Roy R , Zhang B , Scapin G , Patel S , Gao YD , Singh S , Wu J , Zhang X , Thornberry NA , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :49 , 2007 |
Abstract : |
PubMedSearch : Biftu_2007_Bioorg.Med.Chem.Lett_17_49 |
PubMedID: 17055272 |
Gene_locus related to this paper: human-DPP4 |
Title : Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit - Backes_2007_Bioorg.Med.Chem.Lett_17_2005 |
Author(s) : Backes BJ , Longenecker K , Hamilton GL , Stewart K , Lai C , Kopecka H , von Geldern TW , Madar DJ , Pei Z , Lubben TH , Zinker BA , Tian Z , Ballaron SJ , Stashko MA , Mika AK , Beno DW , Kempf-Grote AJ , Black-Schaefer C , Sham HL , Trevillyan JM |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2005 , 2007 |
Abstract : |
PubMedSearch : Backes_2007_Bioorg.Med.Chem.Lett_17_2005 |
PubMedID: 17276063 |
Gene_locus related to this paper: ratno-dpp4 , human-DPP4 |
Title : Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin - Biftu_2007_Bioorg.Med.Chem.Lett_17_3384 |
Author(s) : Biftu T , Scapin G , Singh S , Feng D , Becker JW , Eiermann G , He H , Lyons K , Patel S , Petrov A , Sinha-Roy R , Zhang B , Wu J , Zhang X , Doss GA , Thornberry NA , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :3384 , 2007 |
Abstract : |
PubMedSearch : Biftu_2007_Bioorg.Med.Chem.Lett_17_3384 |
PubMedID: 17433672 |
Gene_locus related to this paper: human-DPP4 |
Title : Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors - Corbett_2007_Bioorg.Med.Chem.Lett_17_6707 |
Author(s) : Corbett JW , Dirico K , Song W , Boscoe BP , Doran SD , Boyer D , Qiu X , Ammirati M , VanVolkenburg MA , McPherson RK , Parker JC , Cox ED |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :6707 , 2007 |
Abstract : |
PubMedSearch : Corbett_2007_Bioorg.Med.Chem.Lett_17_6707 |
PubMedID: 17977724 |
Gene_locus related to this paper: human-DPP4 |
Title : 4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV - Duffy_2007_Bioorg.Med.Chem.Lett_17_2879 |
Author(s) : Duffy JL , Kirk BA , Wang L , Eiermann GJ , He H , Leiting B , Lyons KA , Patel RA , Patel SB , Petrov A , Scapin G , Wu JK , Thornberry NA , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2879 , 2007 |
Abstract : |
PubMedSearch : Duffy_2007_Bioorg.Med.Chem.Lett_17_2879 |
PubMedID: 17350841 |
Gene_locus related to this paper: human-DPP4 |
Title : 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylme thyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes - Eckhardt_2007_J.Med.Chem_50_6450 |
Author(s) : Eckhardt M , Langkopf E , Mark M , Tadayyon M , Thomas L , Nar H , Pfrengle W , Guth B , Lotz R , Sieger P , Fuchs H , Himmelsbach F |
Ref : Journal of Medicinal Chemistry , 50 :6450 , 2007 |
Abstract : |
PubMedSearch : Eckhardt_2007_J.Med.Chem_50_6450 |
PubMedID: 18052023 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV - Feng_2007_J.Med.Chem_50_2297 |
Author(s) : Feng J , Zhang Z , Wallace MB , Stafford JA , Kaldor SW , Kassel DB , Navre M , Shi L , Skene RJ , Asakawa T , Takeuchi K , Xu R , Webb DR , Gwaltney SL, 2nd |
Ref : Journal of Medicinal Chemistry , 50 :2297 , 2007 |
Abstract : |
PubMedSearch : Feng_2007_J.Med.Chem_50_2297 |
PubMedID: 17441705 |
Gene_locus related to this paper: human-DPP4 |
Title : Crystal structures of human dipeptidyl peptidase IV in its apo and diprotin B-complexed forms - Hiramatsu_2007_Acta.Biochim.Biophys.Sin.(Shanghai)_39_335 |
Author(s) : Hiramatsu H , Kyono K , Yamamoto A , Saeki K , Shima H , Sugiyama S , Inaka K , Shimizu R |
Ref : Acta Biochim Biophys Sin (Shanghai) , 39 :335 , 2007 |
Abstract : |
PubMedSearch : Hiramatsu_2007_Acta.Biochim.Biophys.Sin.(Shanghai)_39_335 |
PubMedID: 17492130 |
Gene_locus related to this paper: human-DPP4 |
Title : Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones - Koo_2007_Bioorg.Med.Chem.Lett_17_4167 |
Author(s) : Koo KD , Kim MJ , Kim S , Kim KH , Hong SY , Hur GC , Yim HJ , Kim GT , Han HO , Kwon OH , Kwon TS , Koh JS , Lee CS |
Ref : Bioorganic & Medicinal Chemistry Lett , 17 :4167 , 2007 |
Abstract : |
PubMedSearch : Koo_2007_Bioorg.Med.Chem.Lett_17_4167 |
PubMedID: 17544668 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors - Pei_2007_J.Med.Chem_50_1983 |
Author(s) : Pei Z , Li X , von Geldern TW , Longenecker K , Pireh D , Stewart KD , Backes BJ , Lai C , Lubben TH , Ballaron SJ , Beno DW , Kempf-Grote AJ , Sham HL , Trevillyan JM |
Ref : Journal of Medicinal Chemistry , 50 :1983 , 2007 |
Abstract : |
PubMedSearch : Pei_2007_J.Med.Chem_50_1983 |
PubMedID: 17367123 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors - Xu_2006_Bioorg.Med.Chem.Lett_16_5373 |
Author(s) : Xu J , Wei L , Mathvink RJ , Edmondson SD , Eiermann GJ , He H , Leone JF , Leiting B , Lyons KA , Marsilio F , Patel RA , Patel SB , Petrov A , Scapin G , Wu JK , Thornberry NA , Weber AE |
Ref : Bioorganic & Medicinal Chemistry Lett , 16 :5373 , 2006 |
Abstract : |
PubMedSearch : Xu_2006_Bioorg.Med.Chem.Lett_16_5373 |
PubMedID: 16919457 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Pei_2006_J.Med.Chem_49_6439 |
Author(s) : Pei Z , Li X , von Geldern TW , Madar DJ , Longenecker K , Yong H , Lubben TH , Stewart KD , Zinker BA , Backes BJ , Judd AS , Mulhern M , Ballaron SJ , Stashko MA , Mika AK , Beno DW , Reinhart GA , Fryer RM , Preusser LC , Kempf-Grote AJ , Sham HL , Trevillyan JM |
Ref : Journal of Medicinal Chemistry , 49 :6439 , 2006 |
Abstract : |
PubMedSearch : Pei_2006_J.Med.Chem_49_6439 |
PubMedID: 17064063 |
Gene_locus related to this paper: human-DPP4 |
Title : [(S)-gamma-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors - Sakashita_2006_Bioorg.Med.Chem_14_3662 |
Author(s) : Sakashita H , Akahoshi F , Kitajima H , Tsutsumiuchi R , Hayashi Y |
Ref : Bioorganic & Medicinal Chemistry , 14 :3662 , 2006 |
Abstract : |
PubMedSearch : Sakashita_2006_Bioorg.Med.Chem_14_3662 |
PubMedID: 16460948 |
Gene_locus related to this paper: human-DPP4 |
Title : (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]tr iazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Edmondson_2006_J.Med.Chem_49_3614 |
Author(s) : Edmondson SD , Mastracchio A , Mathvink RJ , He J , Harper B , Park YJ , Beconi M , Di Salvo J , Eiermann GJ , He H , Leiting B , Leone JF , Levorse DA , Lyons K , Patel RA , Patel SB , Petrov A , Scapin G , Shang J , Roy RS , Smith A , Wu JK , Xu S , Zhu B , Thornberry NA , Weber AE |
Ref : Journal of Medicinal Chemistry , 49 :3614 , 2006 |
Abstract : |
PubMedSearch : Edmondson_2006_J.Med.Chem_49_3614 |
PubMedID: 16759103 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes - Madar_2006_J.Med.Chem_49_6416 |
Author(s) : Madar DJ , Kopecka H , Pireh D , Yong H , Pei Z , Li X , Wiedeman PE , Djuric SW , von Geldern TW , Fickes MG , Bhagavatula L , McDermott T , Wittenberger S , Richards SJ , Longenecker KL , Stewart KD , Lubben TH , Ballaron SJ , Stashko MA , Long MA , Wells H , Zinker BA , Mika AK , Beno DW , Kempf-Grote AJ , Polakowski J , Segreti J , Reinhart GA , Fryer RM , Sham HL , Trevillyan JM |
Ref : Journal of Medicinal Chemistry , 49 :6416 , 2006 |
Abstract : |
PubMedSearch : Madar_2006_J.Med.Chem_49_6416 |
PubMedID: 17034148 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors - Pei_2006_J.Med.Chem_49_3520 |
Author(s) : Pei Z , Li X , Longenecker K , von Geldern TW , Wiedeman PE , Lubben TH , Zinker BA , Stewart K , Ballaron SJ , Stashko MA , Mika AK , Beno DW , Long M , Wells H , Kempf-Grote AJ , Madar DJ , McDermott TS , Bhagavatula L , Fickes MG , Pireh D , Solomon LR , Lake MR , Edalji R , Fry EH , Sham HL , Trevillyan JM |
Ref : Journal of Medicinal Chemistry , 49 :3520 , 2006 |
Abstract : |
PubMedSearch : Pei_2006_J.Med.Chem_49_3520 |
PubMedID: 16759095 |
Gene_locus related to this paper: human-DPP4 |
Title : Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors - Qiao_2006_Bioorg.Med.Chem.Lett_16_123 |
Author(s) : Qiao L , Baumann CA , Crysler CS , Ninan NS , Abad MC , Spurlino JC , Desjarlais RL , Kervinen J , Neeper MP , Bayoumy SS , Williams R , Deckman IC , Dasgupta M , Reed RL , Huebert ND , Tomczuk BE , Moriarty KJ |
Ref : Bioorganic & Medicinal Chemistry Lett , 16 :123 , 2006 |
Abstract : |
PubMedSearch : Qiao_2006_Bioorg.Med.Chem.Lett_16_123 |
PubMedID: 16236500 |
Gene_locus related to this paper: human-DPP4 |
Title : Crystal structures of HIV-1 Tat-derived nonapeptides Tat-(1-9) and Trp2-Tat-(1-9) bound to the active site of dipeptidyl-peptidase IV (CD26) - Weihofen_2005_J.Biol.Chem_280_14911 |
Author(s) : Weihofen WA , Liu J , Reutter W , Saenger W , Fan H |
Ref : Journal of Biological Chemistry , 280 :14911 , 2005 |
Abstract : |
PubMedSearch : Weihofen_2005_J.Biol.Chem_280_14911 |
PubMedID: 15695814 |
Gene_locus related to this paper: human-DPP4 |
Title : (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)- yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes - Kim_2005_J.Med.Chem_48_141 |
Author(s) : Kim D , Wang L , Beconi M , Eiermann GJ , Fisher MH , He H , Hickey GJ , Kowalchick JE , Leiting B , Lyons K , Marsilio F , McCann ME , Patel RA , Petrov A , Scapin G , Patel SB , Roy RS , Wu JK , Wyvratt MJ , Zhang BB , Zhu L , Thornberry NA , Weber AE |
Ref : Journal of Medicinal Chemistry , 48 :141 , 2005 |
Abstract : |
PubMedSearch : Kim_2005_J.Med.Chem_48_141 |
PubMedID: 15634008 |
Gene_locus related to this paper: human-DPP4 |
Title : Crystal structure of CD26\/dipeptidyl-peptidase IV in complex with adenosine deaminase reveals a highly amphiphilic interface - Weihofen_2004_J.Biol.Chem_279_43330 |
Author(s) : Weihofen WA , Liu J , Reutter W , Saenger W , Fan H |
Ref : Journal of Biological Chemistry , 279 :43330 , 2004 |
Abstract : |
PubMedSearch : Weihofen_2004_J.Biol.Chem_279_43330 |
PubMedID: 15213224 |
Gene_locus related to this paper: human-DPP4 |
Title : Crystal structure of human dipeptidyl peptidase IV in complex with a decapeptide reveals details on substrate specificity and tetrahedral intermediate formation - Aertgeerts_2004_Protein.Sci_13_412 |
Author(s) : Aertgeerts K , Ye S , Tennant MG , Kraus ML , Rogers J , Sang BC , Skene RJ , Webb DR , Prasad GS |
Ref : Protein Science , 13 :412 , 2004 |
Abstract : |
PubMedSearch : Aertgeerts_2004_Protein.Sci_13_412 |
PubMedID: 14718659 |
Gene_locus related to this paper: human-DPP4 |
Title : Tyrosine 547 constitutes an essential part of the catalytic mechanism of dipeptidyl peptidase IV - Bjelke_2004_J.Biol.Chem_279_34691 |
Author(s) : Bjelke JR , Christensen J , Branner S , Wagtmann N , Olsen C , Kanstrup AB , Rasmussen HB |
Ref : Journal of Biological Chemistry , 279 :34691 , 2004 |
Abstract : |
PubMedSearch : Bjelke_2004_J.Biol.Chem_279_34691 |
PubMedID: 15175333 |
Gene_locus related to this paper: human-DPP4 |
Title : The crystal structure of human dipeptidyl peptidase IV (DPPIV) complex with diprotin A - Hiramatsu_2004_Biol.Chem_385_561 |
Author(s) : Hiramatsu H , Yamamoto A , Kyono K , Higashiyama Y , Fukushima C , Shima H , Sugiyama S , Inaka K , Shimizu R |
Ref : Biol Chem , 385 :561 , 2004 |
Abstract : |
PubMedSearch : Hiramatsu_2004_Biol.Chem_385_561 |
PubMedID: 15255191 |
Gene_locus related to this paper: human-DPP4 |
Title : Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents - Peters_2004_Bioorg.Med.Chem.Lett_14_1491 |
Author(s) : Peters JU , Weber S , Kritter S , Weiss P , Wallier A , Boehringer M , Hennig M , Kuhn B , Loeffler BM |
Ref : Bioorganic & Medicinal Chemistry Lett , 14 :1491 , 2004 |
Abstract : |
PubMedSearch : Peters_2004_Bioorg.Med.Chem.Lett_14_1491 |
PubMedID: 15006388 |
Gene_locus related to this paper: human-DPP4 |
Title : Crystal structure of human dipeptidyl peptidase IV\/CD26 in complex with a substrate analog - Rasmussen_2003_Nat.Struct.Biol_10_19 |
Author(s) : Rasmussen HB , Branner S , Wiberg FC , Wagtmann N |
Ref : Nat Struct Biol , 10 :19 , 2003 |
Abstract : |
PubMedSearch : Rasmussen_2003_Nat.Struct.Biol_10_19 |
PubMedID: 12483204 |
Gene_locus related to this paper: human-DPP4 |
Title : Structural basis of proline-specific exopeptidase activity as observed in human dipeptidyl peptidase-IV - Thoma_2003_Structure_11_947 |
Author(s) : Thoma R , Loffler B , Stihle M , Huber W , Ruf A , Hennig M |
Ref : Structure , 11 :947 , 2003 |
Abstract : |
PubMedSearch : Thoma_2003_Structure_11_947 |
PubMedID: 12906826 |
Gene_locus related to this paper: human-DPP4 |
Title : 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties - Villhauer_2003_J.Med.Chem_46_2774 |
Author(s) : Villhauer EB , Brinkman JA , Naderi GB , Burkey BF , Dunning BE , Prasad K , Mangold BL , Russell ME , Hughes TE |
Ref : Journal of Medicinal Chemistry , 46 :2774 , 2003 |
Abstract : |
PubMedSearch : Villhauer_2003_J.Med.Chem_46_2774 |
PubMedID: 12801240 |
Gene_locus related to this paper: human-DPP4 |
Title : The structure and function of human dipeptidyl peptidase IV, possessing a unique eight-bladed beta-propeller fold - Hiramatsu_2003_Biochem.Biophys.Res.Commun_302_849 |
Author(s) : Hiramatsu H , Kyono K , Higashiyama Y , Fukushima C , Shima H , Sugiyama S , Inaka K , Yamamoto A , Shimizu R |
Ref : Biochemical & Biophysical Research Communications , 302 :849 , 2003 |
Abstract : |
PubMedSearch : Hiramatsu_2003_Biochem.Biophys.Res.Commun_302_849 |
PubMedID: 12646248 |
Gene_locus related to this paper: human-DPP4 |
Title : High-resolution structure of human apo dipeptidyl peptidase IV\/CD26 and its complex with 1-[([2-[(5-iodopyridin-2-yl)amino]-ethyl]amino)-acetyl]-2-cyano-(S)-pyrrolidine - Oefner_2003_Acta.Crystallogr.D.Biol.Crystallogr_59_1206 |
Author(s) : Oefner C , D'Arcy A , Mac Sweeney A , Pierau S , Gardiner R , Dale GE |
Ref : Acta Crystallographica D Biol Crystallogr , 59 :1206 , 2003 |
Abstract : |
PubMedSearch : Oefner_2003_Acta.Crystallogr.D.Biol.Crystallogr_59_1206 |
PubMedID: 12832764 |
Gene_locus related to this paper: human-DPP4 |
Title : Human dipeptidyl peptidase IV gene promoter: tissue-specific regulation from a TATA-less GC-rich sequence characteristic of a housekeeping gene promoter - Bohm_1995_Biochem.J_311 ( Pt 3)_835 |
Author(s) : Bohm SK , Gum JR, Jr. , Erickson RH , Hicks JW , Kim YS |
Ref : Biochemical Journal , 311 ( Pt 3) :835 , 1995 |
Abstract : |
PubMedSearch : Bohm_1995_Biochem.J_311 ( Pt 3)_835 |
PubMedID: 7487939 |
Gene_locus related to this paper: human-DPP4 |
Title : Genomic organization, exact localization, and tissue expression of the human CD26 (dipeptidyl peptidase IV) gene - Abbott_1994_Immunogenetics_40_331 |
Author(s) : Abbott CA , Baker E , Sutherland GR , McCaughan GW |
Ref : Immunogenetics , 40 :331 , 1994 |
Abstract : |
PubMedSearch : Abbott_1994_Immunogenetics_40_331 |
PubMedID: 7927537 |
Gene_locus related to this paper: human-DPP4 |
Title : Cloning and functional expression of the T cell activation antigen CD26 - |
Author(s) : Tanaka T |
Ref : J Immunol , 150 :2090 , 1993 |
PubMedID: 8094732 |
Gene_locus related to this paper: human-DPP4 |
Title : Dipeptidyl peptidase IV (CD 26) gene expression in enterocyte-like colon cancer cell lines HT-29 and Caco-2. Cloning of the complete human coding sequence and changes of dipeptidyl peptidase IV mRNA levels during cell differentiation - Darmoul_1992_J.Biol.Chem_267_4824 |
Author(s) : Darmoul D , Lacasa M , Baricault L , Marguet D , Sapin C |
Ref : Journal of Biological Chemistry , 267 :4824 , 1992 |
Abstract : |
PubMedSearch : Darmoul_1992_J.Biol.Chem_267_4824 |
PubMedID: 1347043 |
Gene_locus related to this paper: human-DPP4 |
Title : Cloning and functional expression of the T cell activation antigen CD26 - Tanaka_1992_J.Immunol_149_481 |
Author(s) : Tanaka T , Camerini D , Seed B , Torimoto Y , Dang NH , Kameoka J , Dahlberg HN , Schlossman SF , Morimoto C |
Ref : J Immunol , 149 :481 , 1992 |
Abstract : |
PubMedSearch : Tanaka_1992_J.Immunol_149_481 |
PubMedID: 1352530 |
Gene_locus related to this paper: human-DPP4 |
Title : Molecular cloning and sequence analysis of human dipeptidyl peptidase IV, a serine proteinase on the cell surface - Misumi_1992_Biochim.Biophys.Acta_1131_333 |
Author(s) : Misumi Y , Hayashi Y , Arakawa F , Ikehara Y |
Ref : Biochimica & Biophysica Acta , 1131 :333 , 1992 |
Abstract : |
PubMedSearch : Misumi_1992_Biochim.Biophys.Acta_1131_333 |
PubMedID: 1352704 |
Gene_locus related to this paper: human-DPP4 |
Title : Isolation of a cDNA probe for the human intestinal dipeptidylpeptidase IV and assignment of the gene locus DPP4 to chromosome 2 - Darmoul_1990_Ann.Hum.Genet_54_191 |
Author(s) : Darmoul D , Lacasa M , Chantret I , Swallow DM , Trugnan G |
Ref : Ann Hum Genet , 54 :191 , 1990 |
Abstract : |
PubMedSearch : Darmoul_1990_Ann.Hum.Genet_54_191 |
PubMedID: 1977364 |
Gene_locus related to this paper: human-DPP4 |