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Gene_locus Report for: human-DPP4

Homo sapiens (Human) dipeptidyl peptidase IV (DPP4), T-cell activation antigen CD26

Comment
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


Relationship
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 E


Molecular evidence
Database
1 mutation: human-DPP4
104 structures (e.g. : 1J2E, 1N1M, 1NU6... more)
No kinetic





2 substrates: GP-BAN, tNPY
96 inhibitors (e.g. : 1,3,4-oxadiazolyl-ketone-18h, 1-valylpyrrolidine, 2-phenylbenzylamine... more)
>3 Genbank links 28 more: M80536, M74777, X60708
1 UniProt : P27487
1 Ncbi-nid : 181569
1 Ncbi-pid : 181570
>3 Structure links 101 more: 5ZID, 6B1O, 6B1E
1 UniProt : P27487
1 Interpro : P27487
1 Prodom : P27487
1 Pfam : P27487
1 PIRSF : P27487
1 SUPERFAM : P27487
1 EntrezGene : 1803
1 SNP : 1803
1 UniGene : 368912
1 HUGO HGNC : 3009
1 IUPHAR : 1612
1 OMIM : 102720
1 Ensembl : ENSG00000197635
Sequence
Graphical view for this peptide sequence: human-DPP4
Colored MSA for DPP4N_Peptidase_S9 (raw)
MKTPWRVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLK
NTYRLKLYSLRWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGH
SINDYSISPDGQFILLEYNYVKQWRHSYTASYDIYDLNKRQLITEERIPN
NTQWVTWSPVGHKLAYVWNNDIYVKIEPNLPSYRITWTGKEDIIYNGITD
WVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSFYSDESLQYPK
TVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMST
TGWVGRFRPSEPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKG
TWEVIGIEALTSDYLYYISNEYKGMPGGRNLYKIQLSDYTKVTCLSCELN
PERCQYYSVSFSKEAKYYQLRCSGPGLPLYTLHSSVNDKGLRVLEDNSAL
DKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKYPLLLDVYAGP
CSQKADIVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCG
IAVAPVSRWEYYESVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEY
LLIHGTADDNVHFQQSAQISKALVDVGVDFQAMWYTDEDHGIASSTAHQH
IYTHMSHFIKQCFSLP
Legend This sequence has been compared to family alignement (MSA)
red => minority aminoacid
blue => majority aminoacid
color intensity => conservation rate
title => sequence position(MSA position)aminoacid rate
Catalytic site
Catalytic site in the MSA

MKTPWRVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLK
NTYRLKLYSLRWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGH
SINDYSISPDGQFILLEYNYVKQWRHSYTASYDIYDLNKRQLITEERIPN
NTQWVTWSPVGHKLAYVWNNDIYVKIEPNLPSYRITWTGKEDIIYNGITD
WVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSFYSDESLQYPK
TVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMST
TGWVGRFRPSEPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKG
TWEVIGIEALTSDYLYYISNEYKGMPGGRNLYKIQLSDYTKVTCLSCELN
PERCQYYSVSFSKEAKYYQLRCSGPGLPLYTLHSSVNDKGLRVLEDNSAL
DKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKYPLLLDVYAGP
CSQKADIVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCG
IAVAPVSRWEYYESVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEY
LLIHGTADDNVHFQQSAQISKALVDVGVDFQAMWYTDEDHGIASSTAHQH
IYTHMSHFIKQCFSLP


References
82 more
    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 S, Xu H, Cui S, Wu F, Zhang Y, Su M, Gong Y, Qiu S, Jiao Q and Li H <13 more author(s)>
    Ref: Journal of Medicinal Chemistry, 59:6772, 2016 : PubMed

            

    Title: Design and synthesis of 4-(2,4,5-trifluorophenyl)butane-1,3-diamines as dipeptidyl peptidase IV inhibitors
    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 : PubMed

            

    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 T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N and Hayashi Y <20 more author(s)>
    Ref: Bioorganic & Medicinal Chemistry, 20:5705, 2012 : PubMed

            


Other Papers


Send your questions or comments to :
Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.
Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
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