Title : Structure-Guided Discovery of cis-Hexahydro-pyrido-oxazinones as Reversible, Drug-like Monoacylglycerol Lipase Inhibitors - Kuhn_2024_J.Med.Chem__ |
Author(s) : Kuhn B , Ritter M , Hornsperger B , Bell C , Kocer B , Rombach D , Lutz MDR , Gobbi L , Kuratli M , Bartelmus C , Burkler M , Koller R , Tosatti P , Ruf I , Guerard M , Pavlovic A , Stephanus J , O'Hara F , Wetzl D , Saal W , Stihle M , Roth D , Hug M , Huber S , Heer D , Kroll C , Topp A , Schneider M , Gertsch J , Glasmacher S , van der Stelt M , Martella A , Wittwer MB , Collin L , Benz J , Richter H , Grether U |
Ref : Journal of Medicinal Chemistry , : , 2024 |
Abstract : |
PubMedSearch : Kuhn_2024_J.Med.Chem__ |
PubMedID: 39360636 |
Title : P2X(7) receptor-dependent increase in endocannabinoid 2-arachidonoyl glycerol production by neuronal cells in culture: Dynamics and mechanism - Singh_2024_Br.J.Pharmacol__ |
Author(s) : Singh S , Sarroza D , English A , Whittington D , Dong A , Malamas M , Makriyannis A , van der Stelt M , Li Y , Zweifel L , Bruchas MR , Land BB , Stella N |
Ref : British Journal of Pharmacology , : , 2024 |
Abstract : |
PubMedSearch : Singh_2024_Br.J.Pharmacol__ |
PubMedID: 38581262 |
Title : Structure-Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors - Jiang_2024_J.Med.Chem__ |
Author(s) : Jiang M , Huizenga MCW , Mohr F , Amedi A , Bakker R , van den Berg R , Deng H , van der Wel T , van Boeckel CAA , van der Stelt M |
Ref : Journal of Medicinal Chemistry , : , 2024 |
Abstract : |
PubMedSearch : Jiang_2024_J.Med.Chem__ |
PubMedID: 38988250 |
Title : Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization - Butini_2024_J.Med.Chem__ |
Author(s) : Butini S , Grether U , Jung KM , Ligresti A , Allara M , Postmus AGJ , Maramai S , Brogi S , Papa A , Carullo G , Sykes D , Veprintsev D , Federico S , Grillo A , Di Guglielmo B , Ramunno A , Stevens AF , Heer D , Lamponi S , Gemma S , Benz J , Di Marzo V , van der Stelt M , Piomelli D , Campiani G |
Ref : Journal of Medicinal Chemistry , : , 2024 |
Abstract : |
PubMedSearch : Butini_2024_J.Med.Chem__ |
PubMedID: 38241614 |
Gene_locus related to this paper: human-MGLL |
Title : Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects - Aebi_2024_Chimia.(Aarau)_78_499 |
Author(s) : Aebi J , Atz K , Ametamey SM , Benz J , Blaising J , Butini S , Campiani G , Carreira EM , Collin L , De Lago E , Gazzi T , Gertsch J , Gobbi L , Guba W , Fernandez-Ruiz J , Fingerle J , Haider A , He Y , Heitman LH , Honer M , Hunziker D , Kuhn B , Maccarrone M , Marki HP , Martin RE , Mohr P , Mu L , Nazare M , Nippa DF , Oddi S , O'Hara F , Pacher P , Romero J , Rover S , Rufer AC , Schibli R , Schneider G , Stepan AF , Sykes DA , Ullmer C , van der Stelt M , Veprintsev DB , Wittwer MB , Grether U |
Ref : Chimia (Aarau) , 78 :499 , 2024 |
Abstract : |
PubMedSearch : Aebi_2024_Chimia.(Aarau)_78_499 |
PubMedID: 39221845 |
Title : Chemical Proteomics Reveals Antibiotic Targets of Oxadiazolones in MRSA - Bakker_2023_J.Am.Chem.Soc_145_1136 |
Author(s) : Bakker AT , Kotsogianni I , Mirenda L , Straub VM , Avalos M , van den Berg R , Florea BI , van Wezel GP , Janssen APA , Martin NI , van der Stelt M |
Ref : Journal of the American Chemical Society , 145 :1136 , 2023 |
Abstract : |
PubMedSearch : Bakker_2023_J.Am.Chem.Soc_145_1136 |
PubMedID: 36584241 |
Gene_locus related to this paper: staa3-q2fkj0 , staau-MW0741 , staau-MW2456 , staau-SA1143 , staau-SA2367 , staau-SAV0321 , staau-SAV0655 |
Title : Inhibition of diacylglycerol lipase beta modulates lipid and endocannabinoid levels in the ex vivo human placenta - Berger_2023_Front.Endocrinol.(Lausanne)_14_1092024 |
Author(s) : Berger N , van der Wel T , Hirschmugl B , Baernthaler T , Gindlhuber J , Fawzy N , Eichmann T , Birner-Gruenberger R , Zimmermann R , van der Stelt M , Wadsack C |
Ref : Front Endocrinol (Lausanne) , 14 :1092024 , 2023 |
Abstract : |
PubMedSearch : Berger_2023_Front.Endocrinol.(Lausanne)_14_1092024 |
PubMedID: 36864832 |
Gene_locus related to this paper: human-DAGLA , human-DAGLB |
Title : Oxygenation of Anandamide by Lipoxygenases - van Zadelhoff_2023_Methods.Mol.Biol_2576_307 |
Author(s) : van Zadelhoff G , van der Stelt M |
Ref : Methods Mol Biol , 2576 :307 , 2023 |
Abstract : |
PubMedSearch : van Zadelhoff_2023_Methods.Mol.Biol_2576_307 |
PubMedID: 36152198 |
Title : A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence - Jiang_2023_Nat.Commun_14_8039 |
Author(s) : Jiang M , Huizenga MCW , Wirt JL , Paloczi J , Amedi A , van den Berg R , Benz J , Collin L , Deng H , Di X , Driever WF , Florea BI , Grether U , Janssen APA , Hankemeier T , Heitman LH , Lam TW , Mohr F , Pavlovic A , Ruf I , van den Hurk H , Stevens AF , van der Vliet D , van der Wel T , Wittwer MB , van Boeckel CAA , Pacher P , Hohmann AG , van der Stelt M |
Ref : Nat Commun , 14 :8039 , 2023 |
Abstract : |
PubMedSearch : Jiang_2023_Nat.Commun_14_8039 |
PubMedID: 38052772 |
Title : Biochemical and Cellular Characterization of the Function of Fluorophosphonate-Binding Hydrolase H (FphH) in Staphylococcus aureus Support a Role in Bacterial Stress Response - Fellner_2023_ACS.Infect.Dis__ |
Author(s) : Fellner M , Walsh A , Dela Ahator S , Aftab N , Sutherland B , Tan EW , Bakker AT , Martin NI , van der Stelt M , Lentz CS |
Ref : ACS Infect Dis , : , 2023 |
Abstract : |
PubMedSearch : Fellner_2023_ACS.Infect.Dis__ |
PubMedID: 37824340 |
Gene_locus related to this paper: staau-MW0741 |
Title : Multi-parameter optimization: Development of a morpholin-3-one derivative with an improved kinetic profile for imaging monoacylglycerol lipase in the brain - He_2022_Eur.J.Med.Chem_243_114750 |
Author(s) : He Y , Grether U , Taddio MF , Meier C , Keller C , Edelmann MR , Honer M , Huber S , Wittwer MB , Heer D , Richter H , Collin L , Hug MN , Hilbert M , Postmus AGJ , Stevens AF , van der Stelt M , Kramer SD , Schibli R , Mu L , Gobbi LC |
Ref : Eur Journal of Medicinal Chemistry , 243 :114750 , 2022 |
Abstract : |
PubMedSearch : He_2022_Eur.J.Med.Chem_243_114750 |
PubMedID: 36137365 |
Gene_locus related to this paper: human-MGLL , mouse-MGLL |
Title : Chemical Probes to Control and Visualize Lipid Metabolism in the Brain - Punt_2022_Acc.Chem.Res_55_3205 |
Author(s) : Punt JM , van der Vliet D , van der Stelt M |
Ref : Acc Chem Res , 55 :3205 , 2022 |
Abstract : |
PubMedSearch : Punt_2022_Acc.Chem.Res_55_3205 |
PubMedID: 36283077 |
Gene_locus related to this paper: human-MGLL |
Title : Targeting Endocannabinoid Signaling: FAAH and MAG Lipase Inhibitors - van Egmond_2021_Annu.Rev.Pharmacol.Toxicol_61_441 |
Author(s) : van Egmond N , Straub VM , van der Stelt M |
Ref : Annual Review of Pharmacology & Toxicology , 61 :441 , 2021 |
Abstract : |
PubMedSearch : van Egmond_2021_Annu.Rev.Pharmacol.Toxicol_61_441 |
PubMedID: 32867595 |
Title : ABHD2 Inhibitor Identified by Activity-Based Protein Profiling Reduces Acrosome Reaction - Baggelaar_2019_ACS.Chem.Biol_14_2295 |
Author(s) : Baggelaar MP , den Dulk H , Florea BI , Fazio D , Perruzza D , Bernabo N , Raspa M , Janssen APA , Scavizzi F , Barboni B , Overkleeft HS , Maccarrone M , van der Stelt M |
Ref : ACS Chemical Biology , 14 :2295 , 2019 |
Abstract : |
PubMedSearch : Baggelaar_2019_ACS.Chem.Biol_14_2295 |
PubMedID: 31525885 |
Gene_locus related to this paper: human-ABHD2 , human-ABHD3 |
Title : Identification of alpha,beta-Hydrolase Domain Containing Protein 6 as a Diacylglycerol Lipase in Neuro-2a Cells - van Esbroeck_2019_Front.Mol.Neurosci_12_286 |
Author(s) : van Esbroeck ACM , Kantae V , Di X , van der Wel T , den Dulk H , Stevens AF , Singh S , Bakker AT , Florea BI , Stella N , Overkleeft HS , Hankemeier T , van der Stelt M |
Ref : Front Mol Neurosci , 12 :286 , 2019 |
Abstract : |
PubMedSearch : van Esbroeck_2019_Front.Mol.Neurosci_12_286 |
PubMedID: 31849602 |
Gene_locus related to this paper: human-ABHD6 |
Title : Activity-Based Protein Profiling Identifies alpha-Ketoamides as Inhibitors for Phospholipase A2 Group XVI - Zhou_2019_ACS.Chem.Biol_14_164 |
Author(s) : Zhou J , Mock ED , Martella A , Kantae V , Di X , Burggraaff L , Baggelaar MP , Al-Ayed K , Bakker A , Florea BI , Grimm SH , den Dulk H , Li CT , Mulder L , Overkleeft HS , Hankemeier T , van Westen GJP , van der Stelt M |
Ref : ACS Chemical Biology , 14 :164 , 2019 |
Abstract : |
PubMedSearch : Zhou_2019_ACS.Chem.Biol_14_164 |
PubMedID: 30620559 |
Title : Design and Synthesis of Quenched Activity-based Probes for Diacylglycerol Lipase and alpha,beta-Hydrolase Domain Containing Protein 6 - van Rooden_2018_Chem.Asian.J_13_3491 |
Author(s) : van Rooden EJ , Kohsiek M , Kreekel R , van Esbroeck ACM , van den Nieuwendijk A , Janssen APA , van den Berg R , Overkleeft HS , van der Stelt M |
Ref : Chem Asian J , 13 :3491 , 2018 |
Abstract : |
PubMedSearch : van Rooden_2018_Chem.Asian.J_13_3491 |
PubMedID: 29901868 |
Title : Chemical Proteomic Analysis of Serine Hydrolase Activity in Niemann-Pick Type C Mouse Brain - van Rooden_2018_Front.Neurosci_12_440 |
Author(s) : van Rooden EJ , van Esbroeck ACM , Baggelaar MP , Deng H , Florea BI , Marques ARA , Ottenhoff R , Boot RG , Overkleeft HS , Aerts J , van der Stelt M |
Ref : Front Neurosci , 12 :440 , 2018 |
Abstract : |
PubMedSearch : van Rooden_2018_Front.Neurosci_12_440 |
PubMedID: 30018533 |
Title : Activity-Based Protein Profiling Delivers Selective Drug Candidate ABX-1431, a Monoacylglycerol Lipase Inhibitor, To Control Lipid Metabolism in Neurological Disorders - Jiang_2018_J.Med.Chem_61_9059 |
Author(s) : Jiang M , van der Stelt M |
Ref : Journal of Medicinal Chemistry , 61 :9059 , 2018 |
Abstract : |
PubMedSearch : Jiang_2018_J.Med.Chem_61_9059 |
PubMedID: 30354159 |
Title : Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors - Janssen_2018_ACS.Chem.Biol_13_2406 |
Author(s) : Janssen APA , van der Vliet D , Bakker AT , Jiang M , Grimm SH , Campiani G , Butini S , van der Stelt M |
Ref : ACS Chemical Biology , 13 :2406 , 2018 |
Abstract : |
PubMedSearch : Janssen_2018_ACS.Chem.Biol_13_2406 |
PubMedID: 30199617 |
Title : Mapping in vivo target interaction profiles of covalent inhibitors using chemical proteomics with label-free quantification - van Rooden_2018_Nat.Protoc_13_752 |
Author(s) : van Rooden EJ , Florea BI , Deng H , Baggelaar MP , van Esbroeck ACM , Zhou J , Overkleeft HS , van der Stelt M |
Ref : Nat Protoc , 13 :752 , 2018 |
Abstract : |
PubMedSearch : van Rooden_2018_Nat.Protoc_13_752 |
PubMedID: 29565900 |
Title : Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding - Deng_2017_J.Med.Chem_60_428 |
Author(s) : Deng H , Kooijman S , van den Nieuwendijk AM , Ogasawara D , van der Wel T , van Dalen F , Baggelaar MP , Janssen FJ , van den Berg RJ , den Dulk H , Cravatt BF , Overkleeft HS , Rensen PC , van der Stelt M |
Ref : Journal of Medicinal Chemistry , 60 :428 , 2017 |
Abstract : |
PubMedSearch : Deng_2017_J.Med.Chem_60_428 |
PubMedID: 27992221 |
Title : Competitive ABPP of Serine Hydrolases: A Case Study on DAGL-Alpha - Baggelaar_2017_Methods.Mol.Biol_1491_161 |
Author(s) : Baggelaar MP , van der Stelt M |
Ref : Methods Mol Biol , 1491 :161 , 2017 |
Abstract : |
PubMedSearch : Baggelaar_2017_Methods.Mol.Biol_1491_161 |
PubMedID: 27778288 |
Title : Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474 - van Esbroeck_2017_Science_356_1084 |
Author(s) : van Esbroeck ACM , Janssen APA , Cognetta AB, 3rd , Ogasawara D , Shpak G , van der Kroeg M , Kantae V , Baggelaar MP , de Vrij FMS , Deng H , Allara M , Fezza F , Lin Z , van der Wel T , Soethoudt M , Mock ED , den Dulk H , Baak IL , Florea BI , Hendriks G , De Petrocellis L , Overkleeft HS , Hankemeier T , De Zeeuw CI , Di Marzo V , Maccarrone M , Cravatt BF , Kushner SA , van der Stelt M |
Ref : Science , 356 :1084 , 2017 |
Abstract : |
PubMedSearch : van Esbroeck_2017_Science_356_1084 |
PubMedID: 28596366 |
Title : Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity - Soethoudt_2017_Nat.Commun_8_13958 |
Author(s) : Soethoudt M , Grether U , Fingerle J , Grim TW , Fezza F , De Petrocellis L , Ullmer C , Rothenhausler B , Perret C , van Gils N , Finlay D , MacDonald C , Chicca A , Gens MD , Stuart J , de Vries H , Mastrangelo N , Xia L , Alachouzos G , Baggelaar MP , Martella A , Mock ED , Deng H , Heitman LH , Connor M , Di Marzo V , Gertsch J , Lichtman AH , Maccarrone M , Pacher P , Glass M , van der Stelt M |
Ref : Nat Commun , 8 :13958 , 2017 |
Abstract : |
PubMedSearch : Soethoudt_2017_Nat.Commun_8_13958 |
PubMedID: 28045021 |
Title : Chemical Proteomics Maps Brain Region Specific Activity of Endocannabinoid Hydrolases - Baggelaar_2017_ACS.Chem.Biol_12_852 |
Author(s) : Baggelaar MP , van Esbroeck AC , van Rooden EJ , Florea BI , Overkleeft HS , Marsicano G , Chaouloff F , van der Stelt M |
Ref : ACS Chemical Biology , 12 :852 , 2017 |
Abstract : |
PubMedSearch : Baggelaar_2017_ACS.Chem.Biol_12_852 |
PubMedID: 28106377 |
Gene_locus related to this paper: human-ABHD4 , human-ABHD6 , human-ABHD12 , human-DAGLA , human-MGLL |
Title : Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-alpha and ABHD6 inhibitors - Deng_2017_Medchemcomm_8_982 |
Author(s) : Deng H , van der Wel T , van den Berg R , van den Nieuwendijk A , Janssen FJ , Baggelaar MP , Overkleeft HS , van der Stelt M |
Ref : Medchemcomm , 8 :982 , 2017 |
Abstract : |
PubMedSearch : Deng_2017_Medchemcomm_8_982 |
PubMedID: 30108813 |
Gene_locus related to this paper: human-ABHD6 |
Title : Oxygenation of Anandamide by Lipoxygenases - van Zadelhoff_2016_Methods.Mol.Biol_1412_217 |
Author(s) : van Zadelhoff G , van der Stelt M |
Ref : Methods Mol Biol , 1412 :217 , 2016 |
Abstract : |
PubMedSearch : van Zadelhoff_2016_Methods.Mol.Biol_1412_217 |
PubMedID: 27245907 |
Title : Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition - Ogasawara_2016_Proc.Natl.Acad.Sci.U.S.A_113_26 |
Author(s) : Ogasawara D , Deng H , Viader A , Baggelaar MP , Breman A , den Dulk H , van den Nieuwendijk AM , Soethoudt M , van der Wel T , Zhou J , Overkleeft HS , Sanchez-Alavez M , Mori S , Nguyen W , Conti B , Liu X , Chen Y , Liu QS , Cravatt BF , van der Stelt M |
Ref : Proc Natl Acad Sci U S A , 113 :26 , 2016 |
Abstract : |
PubMedSearch : Ogasawara_2016_Proc.Natl.Acad.Sci.U.S.A_113_26 |
PubMedID: 26668358 |
Gene_locus related to this paper: human-DAGLA , human-DAGLB |
Title : A natural substrate-based fluorescence assay for inhibitor screening on diacylglycerol lipase alpha - van der Wel_2015_J.Lipid.Res_56_927 |
Author(s) : van der Wel T , Janssen FJ , Baggelaar MP , Deng H , den Dulk H , Overkleeft HS , van der Stelt M |
Ref : J Lipid Res , 56 :927 , 2015 |
Abstract : |
PubMedSearch : van der Wel_2015_J.Lipid.Res_56_927 |
PubMedID: 25684760 |
Title : Highly Selective, Reversible Inhibitor Identified by Comparative Chemoproteomics Modulates Diacylglycerol Lipase Activity in Neurons - Baggelaar_2015_J.Am.Chem.Soc_137_8851 |
Author(s) : Baggelaar MP , Chameau PJ , Kantae V , Hummel J , Hsu KL , Janssen F , van der Wel T , Soethoudt M , Deng H , den Dulk H , Allara M , Florea BI , Di Marzo V , Wadman WJ , Kruse CG , Overkleeft HS , Hankemeier T , Werkman TR , Cravatt BF , van der Stelt M |
Ref : Journal of the American Chemical Society , 137 :8851 , 2015 |
Abstract : |
PubMedSearch : Baggelaar_2015_J.Am.Chem.Soc_137_8851 |
PubMedID: 26083464 |
Gene_locus related to this paper: human-DAGLA , human-DAGLB |
Title : Comprehensive Analysis of Structure-Activity Relationships of alpha-Ketoheterocycles as sn-1-Diacylglycerol Lipase alpha Inhibitors - Janssen_2015_J.Med.Chem_58_9742 |
Author(s) : Janssen FJ , Baggelaar MP , Hummel JJ , Overkleeft HS , Cravatt BF , Boger DL , van der Stelt M |
Ref : Journal of Medicinal Chemistry , 58 :9742 , 2015 |
Abstract : |
PubMedSearch : Janssen_2015_J.Med.Chem_58_9742 |
PubMedID: 26584396 |
Title : Discovery of Glycine Sulfonamides as Dual Inhibitors of sn-1-Diacylglycerol Lipase alpha and alpha\/beta-Hydrolase Domain 6 - Janssen_2014_J.Med.Chem_57_6610 |
Author(s) : Janssen FJ , Deng H , Baggelaar MP , Allara M , van der Wel T , den Dulk H , Ligresti A , van Esbroeck AC , McGuire R , Di Marzo V , Overkleeft HS , van der Stelt M |
Ref : Journal of Medicinal Chemistry , 57 :6610 , 2014 |
Abstract : |
PubMedSearch : Janssen_2014_J.Med.Chem_57_6610 |
PubMedID: 24988361 |
Title : Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-alpha in brain - |
Author(s) : Baggelaar MP , Janssen FJ , van Esbroeck AC , den Dulk H , Allara M , Hoogendoorn S , McGuire R , Florea BI , Meeuwenoord N , van den Elst H , van der Marel GA , Brouwer J , Di Marzo V , Overkleeft HS , van der Stelt M |
Ref : Angew Chem Int Ed Engl , 52 :12081 , 2013 |
PubMedID: 24173880 |
Gene_locus related to this paper: human-DAGLA |