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 : Assay of Monoacylglycerol Lipase Activity - Jung_2023_Methods.Mol.Biol_2576_285 |
Author(s) : Jung KM , Piomelli D |
Ref : Methods Mol Biol , 2576 :285 , 2023 |
Abstract : |
PubMedSearch : Jung_2023_Methods.Mol.Biol_2576_285 |
PubMedID: 36152196 |
Title : Benzisothiazolinone derivatives as potent allosteric monoacylglycerol lipase inhibitors that functionally mimic sulfenylation of regulatory cysteines - Castelli_2020_J.Med.Chem_63_1261 |
Author(s) : Castelli R , Scalvini L , Vacondio F , Lodola A , Anselmi M , Vezzosi S , Carmi C , Bassi M , Ferlenghi F , Rivara S , Moller IR , Rand KD , Daglian J , Wei D , Dotsey EY , Ahmed F , Jung KM , Stella N , Singh S , Mor M , Piomelli D |
Ref : Journal of Medicinal Chemistry , 63 :1261 , 2020 |
Abstract : |
PubMedSearch : Castelli_2020_J.Med.Chem_63_1261 |
PubMedID: 31714779 |
Title : Cannabinoid CB2 receptors mediate the anxiolytic-like effects of monoacylglycerol lipase inhibition in a rat model of predator-induced fear - Ivy_2020_Neuropsychopharmacology__ |
Author(s) : Ivy D , Palese F , Vozella V , Fotio Y , Yalcin A , Ramirez G , Mears D , Wynn G , Piomelli D |
Ref : Neuropsychopharmacology , : , 2020 |
Abstract : |
PubMedSearch : Ivy_2020_Neuropsychopharmacology__ |
PubMedID: 32375160 |
Title : Inhibition of monoacylglycerol lipase: Another signalling pathway for potential therapeutic targets in migraine? - Greco_2017_Cephalalgia__333102417727537 |
Author(s) : Greco R , Demartini C , Zanaboni AM , Berliocchi L , Piomelli D , Tassorelli C |
Ref : Cephalalgia , :333102417727537 , 2017 |
Abstract : |
PubMedSearch : Greco_2017_Cephalalgia__333102417727537 |
PubMedID: 28816506 |
Title : Monoglyceride lipase: Structure and inhibitors - Scalvini_2016_Chem.Phys.Lipids_197_13 |
Author(s) : Scalvini L , Piomelli D , Mor M |
Ref : Chemistry & Physic of Lipids , 197 :13 , 2016 |
Abstract : |
PubMedSearch : Scalvini_2016_Chem.Phys.Lipids_197_13 |
PubMedID: 26216043 |
Title : Free-energy studies reveal a possible mechanism for oxidation-dependent inhibition of MGL - Scalvini_2016_Sci.Rep_6_31046 |
Author(s) : Scalvini L , Vacondio F , Bassi M , Pala D , Lodola A , Rivara S , Jung KM , Piomelli D , Mor M |
Ref : Sci Rep , 6 :31046 , 2016 |
Abstract : |
PubMedSearch : Scalvini_2016_Sci.Rep_6_31046 |
PubMedID: 27499063 |
Title : Effects of fatty acid amide hydrolase (FAAH) inhibitors on working memory in rats - Panlilio_2016_Psychopharmacology.(Berl)_233_1879 |
Author(s) : Panlilio LV , Thorndike EB , Nikas SP , Alapafuja SO , Bandiera T , Cravatt BF , Makriyannis A , Piomelli D , Goldberg SR , Justinova Z |
Ref : Psychopharmacology (Berl) , 233 :1879 , 2016 |
Abstract : |
PubMedSearch : Panlilio_2016_Psychopharmacology.(Berl)_233_1879 |
PubMedID: 26558620 |
Title : Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain - Brindisi_2016_J.Med.Chem_59_2612 |
Author(s) : Brindisi M , Maramai S , Gemma S , Brogi S , Grillo A , Di Cesare Mannelli L , Gabellieri E , Lamponi S , Saponara S , Gorelli B , Tedesco D , Bonfiglio T , Landry C , Jung KM , Armirotti A , Luongo L , Ligresti A , Piscitelli F , Bertucci C , Dehouck MP , Campiani G , Maione S , Ghelardini C , Pittaluga A , Piomelli D , Di Marzo V , Butini S |
Ref : Journal of Medicinal Chemistry , 59 :2612 , 2016 |
Abstract : |
PubMedSearch : Brindisi_2016_J.Med.Chem_59_2612 |
PubMedID: 26888301 |
Title : Endocannabinoid Modulation of Predator Stress-Induced Long-Term Anxiety in Rats - Lim_2016_Neuropsychopharmacology_41_1329 |
Author(s) : Lim J , Igarashi M , Jung KM , Butini S , Campiani G , Piomelli D |
Ref : Neuropsychopharmacology , 41 :1329 , 2016 |
Abstract : |
PubMedSearch : Lim_2016_Neuropsychopharmacology_41_1329 |
PubMedID: 26361059 |
Title : Deficiency of Lipoprotein Lipase in Neurons Decreases AMPA Receptor Phosphorylation and Leads to Neurobehavioral Abnormalities in Mice - Yu_2015_PLoS.One_10_e0135113 |
Author(s) : Yu T , Taussig MD , DiPatrizio NV , Astarita G , Piomelli D , Bergman BC , Dell'Acqua ML , Eckel RH , Wang H |
Ref : PLoS ONE , 10 :e0135113 , 2015 |
Abstract : |
PubMedSearch : Yu_2015_PLoS.One_10_e0135113 |
PubMedID: 26263173 |
Title : Peripheral FAAH and soluble epoxide hydrolase inhibitors are synergistically antinociceptive - Sasso_2015_Pharmacol.Res_97_7 |
Author(s) : Sasso O , Wagner K , Morisseau C , Inceoglu B , Hammock BD , Piomelli D |
Ref : Pharmacol Res , 97 :7 , 2015 |
Abstract : |
PubMedSearch : Sasso_2015_Pharmacol.Res_97_7 |
PubMedID: 25882247 |
Title : Pharmacological characterization of memoquin, a multi-target compound for the treatment of Alzheimer's disease - Capurro_2013_PLoS.One_8_e56870 |
Author(s) : Capurro V , Busquet P , Lopes JP , Bertorelli R , Tarozzo G , Bolognesi ML , Piomelli D , Reggiani A , Cavalli A |
Ref : PLoS ONE , 8 :e56870 , 2013 |
Abstract : |
PubMedSearch : Capurro_2013_PLoS.One_8_e56870 |
PubMedID: 23441223 |
Title : Galantamine potentiates the neuroprotective effect of memantine against NMDA-induced excitotoxicity - Lopes_2013_Brain.Behav_3_67 |
Author(s) : Lopes JP , Tarozzo G , Reggiani A , Piomelli D , Cavalli A |
Ref : Brain Behav , 3 :67 , 2013 |
Abstract : |
PubMedSearch : Lopes_2013_Brain.Behav_3_67 |
PubMedID: 23532860 |
Title : Combining galantamine and memantine in multitargeted, new chemical entities potentially useful in Alzheimer's disease - Simoni_2012_J.Med.Chem_55_9708 |
Author(s) : Simoni E , Daniele S , Bottegoni G , Pizzirani D , Trincavelli ML , Goldoni L , Tarozzo G , Reggiani A , Martini C , Piomelli D , Melchiorre C , Rosini M , Cavalli A |
Ref : Journal of Medicinal Chemistry , 55 :9708 , 2012 |
Abstract : |
PubMedSearch : Simoni_2012_J.Med.Chem_55_9708 |
PubMedID: 23033965 |
Title : Activation of type 5 metabotropic glutamate receptors and diacylglycerol lipase-alpha initiates 2-arachidonoylglycerol formation and endocannabinoid-mediated analgesia - Gregg_2012_J.Neurosci_32_9457 |
Author(s) : Gregg LC , Jung KM , Spradley JM , Nyilas R , Suplita RL, 2nd , Zimmer A , Watanabe M , Mackie K , Katona I , Piomelli D , Hohmann AG |
Ref : Journal of Neuroscience , 32 :9457 , 2012 |
Abstract : |
PubMedSearch : Gregg_2012_J.Neurosci_32_9457 |
PubMedID: 22787031 |
Gene_locus related to this paper: human-DAGLA |
Title : Uncoupling of the endocannabinoid signalling complex in a mouse model of fragile X syndrome - Jung_2012_Nat.Commun_3_1080 |
Author(s) : Jung KM , Sepers M , Henstridge CM , Lassalle O , Neuhofer D , Martin H , Ginger M , Frick A , DiPatrizio NV , Mackie K , Katona I , Piomelli D , Manzoni OJ |
Ref : Nat Commun , 3 :1080 , 2012 |
Abstract : |
PubMedSearch : Jung_2012_Nat.Commun_3_1080 |
PubMedID: 23011134 |
Title : Pretreatment with the monoacylglycerol lipase inhibitor URB602 protects from the long-term consequences of neonatal hypoxic-ischemic brain injury in rats - Carloni_2012_Pediatr.Res_72_400 |
Author(s) : Carloni S , Alonso-Alconada D , Girelli S , Duranti A , Tontini A , Piomelli D , Hilario E , Alvarez A , Balduini W |
Ref : Pediatr Res , 72 :400 , 2012 |
Abstract : |
PubMedSearch : Carloni_2012_Pediatr.Res_72_400 |
PubMedID: 22821058 |
Title : Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain - Guindon_2011_Br.J.Pharmacol_163_1464 |
Author(s) : Guindon J , Guijarro A , Piomelli D , Hohmann AG |
Ref : British Journal of Pharmacology , 163 :1464 , 2011 |
Abstract : |
PubMedSearch : Guindon_2011_Br.J.Pharmacol_163_1464 |
PubMedID: 21198549 |
Title : Deficiency of lipoprotein lipase in neurons modifies the regulation of energy balance and leads to obesity - Wang_2011_Cell.Metab_13_105 |
Author(s) : Wang H , Astarita G , Taussig MD , Bharadwaj KG , DiPatrizio NV , Nave KA , Piomelli D , Goldberg IJ , Eckel RH |
Ref : Cell Metab , 13 :105 , 2011 |
Abstract : |
PubMedSearch : Wang_2011_Cell.Metab_13_105 |
PubMedID: 21195353 |
Title : Complementary synaptic distribution of enzymes responsible for synthesis and inactivation of the endocannabinoid 2-arachidonoylglycerol in the human hippocampus - Ludanyi_2011_Neurosci_174_50 |
Author(s) : Ludanyi A , Hu SS , Yamazaki M , Tanimura A , Piomelli D , Watanabe M , Kano M , Sakimura K , Magloczky Z , Mackie K , Freund TF , Katona I |
Ref : Neuroscience , 174 :50 , 2011 |
Abstract : |
PubMedSearch : Ludanyi_2011_Neurosci_174_50 |
PubMedID: 21035522 |
Title : Diacylglycerol lipase-alpha and -beta control neurite outgrowth in neuro-2a cells through distinct molecular mechanisms - Jung_2011_Mol.Pharmacol_80_60 |
Author(s) : Jung KM , Astarita G , Thongkham D , Piomelli D |
Ref : Molecular Pharmacology , 80 :60 , 2011 |
Abstract : |
PubMedSearch : Jung_2011_Mol.Pharmacol_80_60 |
PubMedID: 21493725 |
Title : Discovery of potent and reversible monoacylglycerol lipase inhibitors - King_2009_Chem.Biol_16_1045 |
Author(s) : King AR , Dotsey EY , Lodola A , Jung KM , Ghomian A , Qiu Y , Fu J , Mor M , Piomelli D |
Ref : Chemical Biology , 16 :1045 , 2009 |
Abstract : |
PubMedSearch : King_2009_Chem.Biol_16_1045 |
PubMedID: 19875078 |
Title : The endocannabinoid system as a target for novel anxiolytic and antidepressant drugs - Gaetani_2009_Int.Rev.Neurobiol_85_57 |
Author(s) : Gaetani S , Dipasquale P , Romano A , Righetti L , Cassano T , Piomelli D , Cuomo V |
Ref : International Review of Neurobiology , 85 :57 , 2009 |
Abstract : |
PubMedSearch : Gaetani_2009_Int.Rev.Neurobiol_85_57 |
PubMedID: 19607961 |
Title : A critical cysteine residue in monoacylglycerol lipase is targeted by a new class of isothiazolinone-based enzyme inhibitors - King_2009_Br.J.Pharmacol_157_974 |
Author(s) : King AR , Lodola A , Carmi C , Fu J , Mor M , Piomelli D |
Ref : British Journal of Pharmacology , 157 :974 , 2009 |
Abstract : |
PubMedSearch : King_2009_Br.J.Pharmacol_157_974 |
PubMedID: 19486005 |
Gene_locus related to this paper: human-ABHD6 |
Title : Distribution and function of monoacylglycerol lipase in the gastrointestinal tract - Duncan_2008_Am.J.Physiol.Gastrointest.Liver.Physiol_295_G1255 |
Author(s) : Duncan M , Thomas AD , Cluny NL , Patel A , Patel KD , Lutz B , Piomelli D , Alexander SP , Sharkey KA |
Ref : American Journal of Physiology Gastrointest Liver Physiol , 295 :G1255 , 2008 |
Abstract : |
PubMedSearch : Duncan_2008_Am.J.Physiol.Gastrointest.Liver.Physiol_295_G1255 |
PubMedID: 18948437 |
Title : A key role for diacylglycerol lipase-alpha in metabotropic glutamate receptor-dependent endocannabinoid mobilization - Jung_2007_Mol.Pharmacol_72_612 |
Author(s) : Jung KM , Astarita G , Zhu C , Wallace M , Mackie K , Piomelli D |
Ref : Molecular Pharmacology , 72 :612 , 2007 |
Abstract : |
PubMedSearch : Jung_2007_Mol.Pharmacol_72_612 |
PubMedID: 17584991 |
Title : Hydrolysis of prostaglandin glycerol esters by the endocannabinoid-hydrolyzing enzymes, monoacylglycerol lipase and fatty acid amide hydrolase - Vila_2007_Biochemistry_46_9578 |
Author(s) : Vila A , Rosengarth A , Piomelli D , Cravatt B , Marnett LJ |
Ref : Biochemistry , 46 :9578 , 2007 |
Abstract : |
PubMedSearch : Vila_2007_Biochemistry_46_9578 |
PubMedID: 17649977 |
Gene_locus related to this paper: human-MGLL , mouse-MGLL |
Title : URB602 inhibits monoacylglycerol lipase and selectively blocks 2-arachidonoylglycerol degradation in intact brain slices - King_2007_Chem.Biol_14_1357 |
Author(s) : King AR , Duranti A , Tontini A , Rivara S , Rosengarth A , Clapper JR , Astarita G , Geaga JA , Luecke H , Mor M , Tarzia G , Piomelli D |
Ref : Chemical Biology , 14 :1357 , 2007 |
Abstract : |
PubMedSearch : King_2007_Chem.Biol_14_1357 |
PubMedID: 18096504 |
Title : The fatty-acid amide hydrolase inhibitor URB597 does not affect triacylglycerol hydrolysis in rat tissues - Clapper_2006_Pharmacol.Res_54_341 |
Author(s) : Clapper JR , Duranti A , Tontini A , Mor M , Tarzia G , Piomelli D |
Ref : Pharmacol Res , 54 :341 , 2006 |
Abstract : |
PubMedSearch : Clapper_2006_Pharmacol.Res_54_341 |
PubMedID: 16935521 |
Title : Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597) - Piomelli_2006_CNS.Drug.Rev_12_21 |
Author(s) : Piomelli D , Tarzia G , Duranti A , Tontini A , Mor M , Compton TR , Dasse O , Monaghan EP , Parrott JA , Putman D |
Ref : CNS Drug Rev , 12 :21 , 2006 |
Abstract : |
PubMedSearch : Piomelli_2006_CNS.Drug.Rev_12_21 |
PubMedID: 16834756 |
Title : Molecular composition of the endocannabinoid system at glutamatergic synapses - Katona_2006_J.Neurosci_26_5628 |
Author(s) : Katona I , Urban GM , Wallace M , Ledent C , Jung KM , Piomelli D , Mackie K , Freund TF |
Ref : Journal of Neuroscience , 26 :5628 , 2006 |
Abstract : |
PubMedSearch : Katona_2006_J.Neurosci_26_5628 |
PubMedID: 16723519 |
Gene_locus related to this paper: mouse-q6wqj1 |
Title : Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors - Jung_2005_Mol.Pharmacol_68_1196 |
Author(s) : Jung KM , Mangieri R , Stapleton C , Kim J , Fegley D , Wallace M , Mackie K , Piomelli D |
Ref : Molecular Pharmacology , 68 :1196 , 2005 |
Abstract : |
PubMedSearch : Jung_2005_Mol.Pharmacol_68_1196 |
PubMedID: 16051747 |
Gene_locus related to this paper: rat-dglb |
Title : Design, synthesis, and structure-activity relationships of alkylcarbamic acid aryl esters, a new class of fatty acid amide hydrolase inhibitors - Tarzia_2003_J.Med.Chem_46_2352 |
Author(s) : Tarzia G , Duranti A , Tontini A , Piersanti G , Mor M , Rivara S , Plazzi PV , Park C , Kathuria S , Piomelli D |
Ref : Journal of Medicinal Chemistry , 46 :2352 , 2003 |
Abstract : |
PubMedSearch : Tarzia_2003_J.Med.Chem_46_2352 |
PubMedID: 12773040 |
Title : Brain monoglyceride lipase participating in endocannabinoid inactivation - Dinh_2002_Proc.Natl.Acad.Sci.U.S.A_99_10819 |
Author(s) : Dinh TP , Carpenter D , Leslie FM , Freund TF , Katona I , Sensi SL , Kathuria S , Piomelli D |
Ref : Proceedings of the National Academy of Sciences of the United States of America , 99 :10819 , 2002 |
Abstract : |
PubMedSearch : Dinh_2002_Proc.Natl.Acad.Sci.U.S.A_99_10819 |
PubMedID: 12136125 |
Gene_locus related to this paper: ratno-MGLL |
Title : Lipoxygenase metabolites of arachidonic acid as second messengers for presynaptic inhibition of Aplysia sensory cells - Piomelli_1987_Nature_328_38 |
Author(s) : Piomelli D , Volterra A , Dale N , Siegelbaum SA , Kandel ER , Schwartz JH , Belardetti F |
Ref : Nature , 328 :38 , 1987 |
Abstract : |
PubMedSearch : Piomelli_1987_Nature_328_38 |
PubMedID: 2439918 |