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 : 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 : 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 : Preclinical Evaluation of the Reversible Monoacylglycerol Lipase PET Tracer (R)-[(11) C]YH132: Application in Drug Development and Neurodegenerative Diseases - He_2024_Chembiochem__e202300819 |
Author(s) : He Y , Delparente A , Jie C , Keller C , Humm R , Heer D , Collin L , Schibli R , Gobbi L , Grether U , Mu L |
Ref : Chembiochem , :e202300819 , 2024 |
Abstract : |
PubMedSearch : He_2024_Chembiochem__e202300819 |
PubMedID: 38441502 |
Title : Identification of (R)-[(18)F]YH134 for Monoacylglycerol Lipase Neuroimaging and Exploration of Its Use for Central Nervous System and Peripheral Drug Development - He_2023_J.Nucl.Med__ |
Author(s) : He Y , Kramer SD , Grether U , Wittwer MB , Collin L , Kuhn B , Topp A , Heer D , O'Hara F , Honer M , Pavlovic A , Richter H , Ritter M , Rombach D , Keller C , Gobbi L , Mu L |
Ref : J Nucl Med , : , 2023 |
Abstract : |
PubMedSearch : He_2023_J.Nucl.Med__ |
PubMedID: 38164615 |
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 : 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 : Development of High Brain-Penetrant and Reversible Monoacylglycerol Lipase PET Tracers for Neuroimaging - He_2022_J.Med.Chem_65_2191 |
Author(s) : He Y , Schild M , Grether U , Benz J , Leibrock L , Heer D , Topp A , Collin L , Kuhn B , Wittwer M , Keller C , Gobbi LC , Schibli R , Mu L |
Ref : Journal of Medicinal Chemistry , 65 :2191 , 2022 |
Abstract : |
PubMedSearch : He_2022_J.Med.Chem_65_2191 |
PubMedID: 35089028 |
Gene_locus related to this paper: human-MGLL |
Title : A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature - Kemble_2022_PLoS.One_17_e0268590 |
Author(s) : Kemble AM , Hornsperger B , Ruf I , Richter H , Benz J , Kuhn B , Heer D , Wittwer M , Engelhardt B , Grether U , Collin L |
Ref : PLoS ONE , 17 :e0268590 , 2022 |
Abstract : |
PubMedSearch : Kemble_2022_PLoS.One_17_e0268590 |
PubMedID: 36084029 |
Gene_locus related to this paper: human-MGLL |
Title : Discovery, synthesis and evaluation of novel reversible monoacylglycerol lipase radioligands bearing a morpholine-3-one scaffold - He_2022_Nucl.Med.Biol_108-109_24 |
Author(s) : He Y , Gobbi LC , Herde AM , Rombach D , Ritter M , Kuhn B , Wittwer MB , Heer D , Hornsperger B , Bell C , O'Hara F , Benz J , Honer M , Keller C , Collin L , Richter H , Schibli R , Grether U , Mu L |
Ref : Nucl Med Biol , 108-109 :24 , 2022 |
Abstract : |
PubMedSearch : He_2022_Nucl.Med.Biol_108-109_24 |
PubMedID: 35248850 |
Title : Development of reversible monoacylglycerol lipase PET tracers with improved brain uptake - He_2021_Nucl.Med.Biol_96-97_S36 |
Author(s) : He Y , Schild M , Grether U , Humm R , Keller C , Schibli R , Gobbi L , Mu L |
Ref : Nucl Med Biol , 96-97 :S36 , 2021 |
Abstract : |
PubMedSearch : He_2021_Nucl.Med.Biol_96-97_S36 |
PubMedID: |
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 |