| 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 |
| Gene_locus related to this paper: human-MGLL |
| Title : Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors - Di Stefano_2023_Eur.J.Med.Chem_263_115916 |
| Author(s) : Di Stefano M , Masoni S , Bononi G , Poli G , Galati S , Gado F , Manzi S , Vagaggini C , Brai A , Caligiuri I , Asif K , Rizzolio F , Macchia M , Chicca A , Sodi A , Di Bussolo V , Minutolo F , Meier P , Gertsch J , Granchi C , Dreassi E , Tuccinardi T |
| Ref : Eur Journal of Medicinal Chemistry , 263 :115916 , 2023 |
| Abstract : |
| PubMedSearch : Di Stefano_2023_Eur.J.Med.Chem_263_115916 |
| PubMedID: 37976705 |
| Gene_locus related to this paper: human-ABHD6 |
| Title : Reversible Monoacylglycerol Lipase Inhibitors: Discovery of a New Class of Benzylpiperidine Derivatives - Bononi_2022_J.Med.Chem__ |
| Author(s) : Bononi G , Di Stefano M , Poli G , Ortore G , Meier P , Masetto F , Caligiuri I , Rizzolio F , Macchia M , Chicca A , Avan A , Giovannetti E , Vagaggini C , Brai A , Dreassi E , Valoti M , Minutolo F , Granchi C , Gertsch J , Tuccinardi T |
| Ref : Journal of Medicinal Chemistry , : , 2022 |
| Abstract : |
| PubMedSearch : Bononi_2022_J.Med.Chem__ |
| PubMedID: 35522977 |
| Title : Insights into the Phytochemical and Multifunctional Biological Profile of Spices from the Genus Piper - Luca_2021_Antioxidants.(Basel)_10_ |
| Author(s) : Luca SV , Gawel-Beben K , Strzepek-Gomolka M , Czech K , Trifan A , Zengin G , Korona-Glowniak I , Minceva M , Gertsch J , Skalicka-Wozniak K |
| Ref : Antioxidants (Basel) , 10 : , 2021 |
| Abstract : |
| PubMedSearch : Luca_2021_Antioxidants.(Basel)_10_ |
| PubMedID: 34679776 |
| Title : Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors - Granchi_2020_Eur.J.Med.Chem_209_112857 |
| Author(s) : Granchi C , Bononi G , Ferrisi R , Gori E , Mantini G , Glasmacher S , Poli G , Palazzolo S , Caligiuri I , Rizzolio F , Canzonieri V , Perin T , Gertsch J , Sodi A , Giovannetti E , Macchia M , Minutolo F , Tuccinardi T , Chicca A |
| Ref : Eur Journal of Medicinal Chemistry , 209 :112857 , 2020 |
| Abstract : |
| PubMedSearch : Granchi_2020_Eur.J.Med.Chem_209_112857 |
| PubMedID: 33045662 |
| Gene_locus related to this paper: human-MGLL |
| Title : Endocannabinoid metabolism and transport as targets to regulate intraocular pressure - Miller_2020_Exp.Eye.Res__108266 |
| Author(s) : Miller S , Daily L , Dharla V , Gertsch J , Malamas MS , Ojima I , Kaczocha M , Ogasawara D , Straiker A |
| Ref : Experimental Eye Research , :108266 , 2020 |
| Abstract : |
| PubMedSearch : Miller_2020_Exp.Eye.Res__108266 |
| PubMedID: 32979397 |
| Title : Paradoxical effects of JZL184, an inhibitor of monoacylglycerol lipase, on bone remodelling in healthy and cancer-bearing mice - Marino_2019_EBioMedicine_44_452 |
| Author(s) : Marino S , de Ridder D , Bishop RT , Renema N , Ponzetti M , Sophocleous A , Capulli M , Aljeffery A , Carrasco G , Gens MD , Khogeer A , Ralston SH , Gertsch J , Lamoureux F , Heymann D , Rucci N , Idris AI |
| Ref : EBioMedicine , 44 :452 , 2019 |
| Abstract : |
| PubMedSearch : Marino_2019_EBioMedicine_44_452 |
| PubMedID: 31151929 |
| Title : Modification on the 1,2-dihydro-2-oxo-pyridine-3-carboxamide core to obtain multi-target modulators of endocannabinoid system - Gado_2019_Bioorg.Chem__103353 |
| Author(s) : Gado F , Arena C , Fauci C , Reynoso-Moreno I , Bertini S , Digiacomo M , Meini S , Poli G , Macchia M , Tuccinardi T , Gertsch J , Chicca A , Manera C |
| Ref : Bioorg Chem , :103353 , 2019 |
| Abstract : |
| PubMedSearch : Gado_2019_Bioorg.Chem__103353 |
| PubMedID: 31668465 |
| Title : Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor - Granchi_2019_J.Med.Chem_62_1932 |
| Author(s) : Granchi C , Lapillo M , Glasmacher S , Bononi G , Licari C , Poli G , El Boustani M , Caligiuri I , Rizzolio F , Gertsch J , Macchia M , Minutolo F , Tuccinardi T , Chicca A |
| Ref : Journal of Medicinal Chemistry , 62 :1932 , 2019 |
| Abstract : |
| PubMedSearch : Granchi_2019_J.Med.Chem_62_1932 |
| PubMedID: 30715876 |
| Title : New cycloartane-type ester triterpenes from Euphorbia pterococca and biological evaluation - Benabdelaziz_2018_Fitoterapia_127_271 |
| Author(s) : Benabdelaziz I , Gomez-Ruiz S , Benkhaled M , Carralero S , Schenker P , Salm A , Gertsch J , Haba H |
| Ref : Fitoterapia , 127 :271 , 2018 |
| Abstract : |
| PubMedSearch : Benabdelaziz_2018_Fitoterapia_127_271 |
| PubMedID: 29524564 |
| Title : Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system - Chicca_2018_Eur.J.Med.Chem_154_155 |
| Author(s) : Chicca A , Arena C , Bertini S , Gado F , Ciaglia E , Abate M , Digiacomo M , Lapillo M , Poli G , Bifulco M , Macchia M , Tuccinardi T , Gertsch J , Manera C |
| Ref : Eur Journal of Medicinal Chemistry , 154 :155 , 2018 |
| Abstract : |
| PubMedSearch : Chicca_2018_Eur.J.Med.Chem_154_155 |
| PubMedID: 29793210 |
| Title : Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors - Aghazadeh Tabrizi_2018_J.Med.Chem_61_1340 |
| Author(s) : Aghazadeh Tabrizi M , Baraldi PG , Baraldi S , Ruggiero E , De Stefano L , Rizzolio F , Di Cesare Mannelli L , Ghelardini C , Chicca A , Lapillo M , Gertsch J , Manera C , Macchia M , Martinelli A , Granchi C , Minutolo F , Tuccinardi T |
| Ref : Journal of Medicinal Chemistry , 61 :1340 , 2018 |
| Abstract : |
| PubMedSearch : Aghazadeh Tabrizi_2018_J.Med.Chem_61_1340 |
| PubMedID: 29309142 |
| 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 : Guineensine is a novel inhibitor of endocannabinoid uptake showing cannabimimetic behavioral effects in BALB\/c mice - Nicolussi_2014_Pharmacol.Res_80_52 |
| Author(s) : Nicolussi S , Viveros-Paredes JM , Gachet MS , Rau M , Flores-Soto ME , Blunder M , Gertsch J |
| Ref : Pharmacol Res , 80 :52 , 2014 |
| Abstract : |
| PubMedSearch : Nicolussi_2014_Pharmacol.Res_80_52 |
| PubMedID: 24412246 |
| Title : Discovery of potent positive allosteric modulators of the alpha3beta2 nicotinic acetylcholine receptor by a chemical space walk in ChEMBL - Burgi_2014_ACS.Chem.Neurosci_5_346 |
| Author(s) : Burgi JJ , Awale M , Boss SD , Schaer T , Marger F , Viveros-Paredes JM , Bertrand S , Gertsch J , Bertrand D , Reymond JL |
| Ref : ACS Chem Neurosci , 5 :346 , 2014 |
| Abstract : |
| PubMedSearch : Burgi_2014_ACS.Chem.Neurosci_5_346 |
| PubMedID: 24593915 |
| Title : Functionalization of beta-Caryophyllene Generates Novel Polypharmacology in the Endocannabinoid System - Chicca_2014_ACS.Chem.Biol_9_1499 |
| Author(s) : Chicca A , Caprioglio D , Minassi A , Petrucci V , Appendino G , Taglialatela-Scafati O , Gertsch J |
| Ref : ACS Chemical Biology , 9 :1499 , 2014 |
| Abstract : |
| PubMedSearch : Chicca_2014_ACS.Chem.Biol_9_1499 |
| PubMedID: 24831513 |
| Title : The antinociceptive triterpene beta-amyrin inhibits 2-arachidonoylglycerol (2-AG) hydrolysis without directly targeting cannabinoid receptors - Chicca_2012_Br.J.Pharmacol_167_1596 |
| Author(s) : Chicca A , Marazzi J , Gertsch J |
| Ref : British Journal of Pharmacology , 167 :1596 , 2012 |
| Abstract : |
| PubMedSearch : Chicca_2012_Br.J.Pharmacol_167_1596 |
| PubMedID: 22646533 |
| Title : In silico target fishing for rationalized ligand discovery exemplified on constituents of Ruta graveolens - Rollinger_2009_Planta.Med_75_195 |
| Author(s) : Rollinger JM , Schuster D , Danzl B , Schwaiger S , Markt P , Schmidtke M , Gertsch J , Raduner S , Wolber G , Langer T , Stuppner H |
| Ref : Planta Med , 75 :195 , 2009 |
| Abstract : |
| PubMedSearch : Rollinger_2009_Planta.Med_75_195 |
| PubMedID: 19096995 |