Juha Savinainen

5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein–Protein Interaction-Derived Functions

Pätsi, Henri T; Kilpeläinen, Tommi P; Jumppanen, Mikael; Uhari-Väänänen, Johanna; Wielendaele, Pieter Van; De Lorenzo, Francesca; Cui, Hengjing; Auno, Samuli; Saharinen, Janne; Seppälä, Erin; Sipari, Nina; Savinainen, Juha; De Meester, Ingrid; Lambeir, Anne-Marie; Lahtela-Kakkonen, Maija; Myöhänen, Timo T; Wallén, Erik AA. 2024. Journal of medicinal chemistry. 67: 5421-5436 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

A prolyl oligopeptidase inhibitor reduces tau pathology in cellular models and in mice with tauopathy

Eteläinen, Tony S; Silva, M Catarina; Uhari-Väänänen, Johanna K; De Lorenzo, Francesca; Jäntti, Maria H; Cui, Hengjing; Chavero-Pieres, Marta; Kilpeläinen, Tommi; Mechtler, Christina; Svarcbahs, Reinis; Seppälä, Erin; Savinainen, Juha R; Puris, Elena; Fricker, Gert; Gynther, Mikko; Julku, Ulrika H; Huttunen, Henri J; Haggarty, Stephen J; Myöhänen, Timo T. 2023. Science translational medicine. 15: 1-17 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

Della Pietra, Adriana; Krivoshein, Georgii; Ivanov, Konstantin; Giniatullina, Raisa; Jyrkkänen, Henna-Kaisa; Leinonen, Ville; Lehtonen, Marko; van den Maagdenberg, Arn MJM; Savinainen, Juha; Giniatullin, Rashid. 2023. Journal of headache and pain. 24: . 38 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid α/β Hydrolase Domain 6 (ABHD6)

Mardon, Karine; Patel, Jayendra Z; Savinainen, Juha R; Stimson, Damion HR; Oyagawa, Caitlin RM; Grimsey, Natasha L; Migotto, Mary-anne; Njiru, Grace FM; Hamilton, Brett R; Cowin, Gary; Yli-Kauhaluoma, Jari; Vanduffel, Wim; Blakey, Idriss; Bhalla, Rajiv; Cawthorne, Christopher; Celen, Sofie; Bormans, Guy; Thurecht, Kristofer J; Ahamed, Muneer. 2023. Journal of medicinal chemistry. 66: 538-552 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Inhibiting Endocannabinoid Hydrolysis as Emerging Analgesic Strategy Targeting a Spectrum of Ion Channels Implicated in Migraine Pain

Della Pietra, Adriana; Savinainen, Juha; Giniatullin, Rashid. 2022. International journal of molecular sciences. 23: A2 Katsausartikkeli tieteellisessä aikakauslehdessä

Metabolomics of Synovial Fluid and Infrapatellar Fat Pad in Patients with Osteoarthritis or Rheumatoid Arthritis

Nieminen, Petteri; Hämäläinen, Wilhelmiina; Savinainen, Juha; Lehtonen, Marko; Lehtiniemi, Saara; Rinta-Paavola, Juho; Lehenkari, Petri; Kääriäinen, Tommi; Joukainen, Antti; Kröger, Heikki; Paakkonen, Tommi; Mustonen, Anne-Mari. 2022. Inflammation. 45: 1101-1117 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Distinct Activity of Endocannabinoid-Hydrolyzing Enzymes MAGL and FAAH in Key Regions of Peripheral and Central Nervous System Implicated in Migraine

Della Pietra, Adriana; Giniatullin, Rashid; Savinainen, Juha R. 2021. International journal of molecular sciences. 22: 1204 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Evaluation of FASN inhibitors by a versatile toolkit reveals differences in pharmacology between human and rodent FASN preparations and in antiproliferative efficacy in vitro vs. in situ in human cancer cells

Singha, Prosanta; Mäklin, Kiira; Vihavainen, Taina; Laitinen, Tuomo; Nevalainen, Tapio; Patil, Mahadeo; Tonduru, Arun; Poso, Antti; Laitinen, Jarmo; Savinainen, Juha. 2020. European journal of pharmaceutical sciences. 149: 105321 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections - Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils

Aaltonen, Niina; Singha, Prosanta; Jakupovic, Hermina; Wirth, Thomas; Samaranayake, Haritha; Pasonen-Seppänen, Sanna; Rilla, Kirsi; Varjosalo, Markku; Edgington-Mitchell, Laura; Kasperkiewicz, Paulina; Drag, Marcin; Kälvälä, Sara; Moisio, Eemeli; Savinainen, Juha; Laitinen, Jarmo. 2020. Biological procedures online. 22: 6 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Regulating membrane lipid levels at the synapse by small-molecule inhibitors of monoacylglycerol lipase: new developments in therapeutic and PET imaging applications

Grimsey, NL; Savinainen, JR; Attili, B; Ahamed, M. 2020. Drug discovery today. 25: 330-343 A2 Katsausartikkeli tieteellisessä aikakauslehdessä

Discovery of 12-Thiazole Abietanes as Selective Inhibitors of the Human Metabolic Serine Hydrolase hABHD16A

Ahonen, Tiina J; Savinainen, Juha R; Yli-Kauhaluoma, Jari: Kalso, Eija; Laitinen, Jarmo T; Moreira, Vânia M. 2018. Acs medicinal chemistry letters. 9: 1269-1273 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Design, Synthesis, and Biological Evaluation of 2,4-Dihydropyrano[2,3-c]pyrazole Derivatives as Autotaxin Inhibitors

Pantsar T, Singha P, Nevalainen TJ, Koshevoy I, Leppänen J, Poso A, Niskanen JMA, Pasonen-Seppänen S, Savinainen JR, Laitinen T, Laitinen JT. 2017. European journal of pharmaceutical sciences. 107: 97-111 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)

Ahamed Muneer, Attili Bala, van Veghel Daisy, Ooms Maarten, Berben Philippe, Celen Sofie, Koole Michel, Declercq Lieven, Savinainen Juha R, Laitinen Jarmo T, Verbruggen Alfons, Bormans Guy. 2017. European journal of medicinal chemistry. 136: 104-113 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

A sensitive and versatile fluorescent activity assay for ABHD12

Savinainen Juha R, Navia-Paldanius Dina, Laitinen Jarmo T. Teoksessa: Maccarrone Mauro(toim.) , 2016. Endocannabinoid Signaling: Methods and Protocols. s. 179-189. Springer A3 Kirjan tai muun kokoomateoksen osa

A sensitive and versatile fluorescent activity assay for ABHD6

Savinainen Juha R, Navia-Paldanius Dina, Laitinen Jarmo T. Teoksessa: Maccarrone Mauro(toim.) , 2016. Endocannabinoid Signaling: Methods and Protocols. s. 169-178. Springer A3 Kirjan tai muun kokoomateoksen osa

Chemoproteomic, biochemical and pharmacological approaches in the discovery of inhibitors targeting human alfa/beta-hydrolase domain containing 11 (ABHD11)

Navia-Paldanius D, Patel JZ, López Navarro M, Jakupovic H, Goffart S, Pasonen-Seppänen S, Nevalainen TJ, Jääskeläinen T, Laitinen T, Laitinen JT, Savinainen JR. 2016. European journal of pharmaceutical sciences. 93: 253-263 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

In vivo characterization of the ultrapotent monoacylglycerol lipase inhibitor {4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl} (1H-1,2,4-triazol-1-yl)methanone (JJKK-048)

Aaltonen Niina, Kedzierska Ewa, Orzelska-Gorka Jolanta, Lehtonen Marko, Navia-Paldanius Dina, Jakupovic Hermina, Savinainen Juha, Nevalainen Tapio, Laitinen Jarmo T, Parkkari Teija, Gynther Mikko. 2016. Journal of pharmacology and experimental therapeutics. 359: 62-72 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Increased tonic cannabinoid CB1R activity and brain region-specific desensitization of CB1R Gi/o signaling axis in mice with global genetic knockout of monoacylglycerol lipase

Navia-Paldanius Dina, Aaltonen Niina, Lehtonen Marko, Savinainen Juha R, Taschler Ulrike, Radner Franz PW, Zimmermann Robert, Laitinen Jarmo T. 2015. European journal of pharmaceutical sciences. 77: 180-188 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Loratadine analogues as MAGL inhibitors

Patel Jayendra Z, Ahenkorah Stephen, Vaara Miia, Staszewski Marek, Adams Yahaya, Laitinen Tuomo, Navia-Paldanius Dina, Parkkari Teija, Savinainen Juha R, Walczynski Krzysztof, Laitinen Jarmo T, Nevalainen Tapio J. 2015. Bioorganic and medicinal chemistry letters. 25: 1436-1442 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity

Manera Clementina, Malfitano Anna M, Parkkari Teija, Lucchesi Valentina, Carpi Sara, Fogli Stefano, Bertini Simone, Laezza Chiara, Ligresti Alessia, Saccomanni Giuseppe, Savinainen Juha R, Ciaglia Elena, Pisanti Simona, Gazzerro Patrizia, Di Marzo Vincenzo, Nieri Paola, Macchia Marco, Bifulco Maurizio. 2015. European journal of medicinal chemistry. 97: 10-18 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists

Yrjölä Sari, Parkkari Teija, Navia-Paldanius Dina, Laitinen Tuomo, Kaczor Agnieszka A, Kokkola Tarja, Adusei-Mensah Frank, Savinainen Juha R, Laitinen Jarmo T, Poso Antti, Alexander Amy, Penman June, Stott Lisa, Anskat Marie, Irving Andrew J, Nevalainen Tapio J. 2015. European journal of medicinal chemistry. 107 (2016): 119-132 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors

Patel Jayendra Z, van Bruchem John, Laitinen Tuomo, Kaczor Agnieszka A, Navia-Paldanius Dina, Parkkari Teija, Savinainen Juha R, Laitinen Jarmo T, Nevalainen Tapio J. 2015. Bioorganic and medicinal chemistry. 23: 6335-6345 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor

Lucchesi Valentina, Parkkari Teija, Savinainen Juha R, Malfitano Anna M, Allarà Marco, Bertini Simone, Castelli Francesca, Del Carlo Sara, Laezza Chiara, Ligresti Alessia, Saccomanni Giuseppe, Bifulco Maurizio, Di Marzo Vincenzo, Macchia Marco, Manera Clementina. 2014. European journal of medicinal chemistry. 74: 524-532 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Biochemical and Pharmacological Characterization of the Human Lymphocyte Antigen B-Associated Transcript 5 (BAT5/ABHD16A)

Savinainen Juha R, Patel Jayendra Z, Parkkari Teija, Navia-Paldanius Dina, Marjamaa Joona JT, Laitinen Tuomo, Nevalainen Tapio, Laitinen Jarmo T. 2014. PLoS ONE. 9: e109869 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Discovery of triterpenoids as reversible inhibitors of alpha/ß-hydrolase domain containing 12 (ABHD12)

Parkkari Teija, Haavikko Raisa, Laitinen Tuomo, Navia-Paldanius Dina, Rytilahti Roosa, Vaara Miia, Lehtonen Marko, Alakurtti Sami, Yli-Kauhaluoma Jari, Nevalainen Tapio, Savinainen Juha R, Laitinen Jarmo T. 2014. PLoS ONE. 9: e98286 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors

Patel Jayendra Z, Nevalainen Tapio J, Savinainen Juha R, Adams Yahaya, Laitinen Tuomo, Runyon Robert S, Vaara Miia, Ahenkorah Stephen, Kaczor Agnieszka A, Navia-Paldanius Dina, Gynther Mikko, Aaltonen Niina, Joharapurkar Amit A, Jain Mukul R, Haka Abigail S, Maxfield Frederick R, Laitinen Jarmo T, Parkkari Teija. 2014. Chemmedchem. 2015; 10: 253-265 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL)

Korhonen Jani, Kuusisto Anne, van Bruchem John, Patel Jayendra Z, Laitinen Tuomo, Navia-Paldanius Dina, Laitinen Jarmo T, Savinainen Juha R, Parkkari Teija, Nevalainen Tapio J. 2014. Bioorganic and medicinal chemistry. 22: 6694-6705 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Robust hydrolysis of prostaglandin glycerol esters by human monoacylglycerol lipase (MAGL)

Savinainen Juha R, Kansanen Emilia, Pantsar Tatu, Navia-Paldanius Dina, Parkkari Teija, Lehtonen Marko, Laitinen Tuomo, Nevalainen Tapio, Poso Antti, Levonen Anna-Liisa, Laitinen Jarmo T. 2014. Molecular pharmacology. Epub ahead of print: - A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands

Bertini Simone, Parkkari Teija, Savinainen Juha R, Arena Chiara, Saccomanni Giuseppe, Saguto Simone, Ligresti Alessia, Allarà Marco, Bruno Agostino, Marinelli Luciana, Di Marzo Vincenzo, Novellino Ettore, Manera Clementina, Macchia Marco. 2014. European journal of medicinal chemistry. 90 (2015): 526-536 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Brain regional cannabinoid CB1 receptor signalling and alternative enzymatic pathways for 2-arachidonoylglycerol generation in brain sections of diacylglycerol lipase deficient mice

Aaltonen Niina, Ribas Casandra R, Lehtonen Marko, Savinainen Juha R, Laitinen Jarmo T. 2013. European journal of pharmaceutical sciences. 2014:51: 87-95 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors

Patel Jayendra Z, Parkkari Teija, Laitinen Tuomo, Kaczor Agnieszka A, Saario Susanna M, Savinainen Juha R, Navia-Paldanius Dina, Cipriano Mariateresa, Leppänen Jukka, Koshevoy Igor O, Poso Antti, Fowler Christopher J, Laitinen Jarmo T, Nevalainen Tapio. 2013. Journal of medicinal chemistry. 56: 8484-8496 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency

Laitinen Tuomo, Navia-Paldanius Dina, Rytilahti Roosa, Marjamaa Joona J, Karizkova Julie, Parkkari Teija, Pantsar Tatu, Poso Antti, Laitinen Jarmo T, Savinainen Juha R. 2013. Molecular pharmacology. 2014:85: 510-519 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase

Aaltonen Niina, Savinainen Juha R, Ribas Casandra R, Rönkkö Jani, Kuusisto Anne, Korhonen Jani, Navia-Paldanius Dina, Häyrinen Jukka, Takabe Piia, Käsnänen Heikki, Pantsar Tatu, Laitinen Tuomo, Lehtonen Marko, Pasonen-Seppänen Sanna, Poso Antti, Nevalainen Tapio, Laitinen Jarmo T. 2013. Chemistry and biology. 20: 379-390 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Biochemical and pharmacological characterization of human &#945 /&#946 -hydrolase domain containing 6 (ABHD6) and 12 (ABHD12)

Navia-Paldanius D, Savinainen JR, Laitinen JT. 2012. Journal of lipid research. 53: 2413-2424 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

The serine hydrolases MAGL, ABHD6 and ABHD12 as guardians of 2-arachidonoylglycerol signalling through cannabinoid receptors

Savinainen JR, Saario SM, Laitinen JT. 2011. Acta physiologica. 2012 vol 204: 267-276 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescene-based technique

Savinainen JR, Megumi Y, Minkkilä A, Nevalainen T, & Laitinen JT. 2010. Analytical biochemistry. 399: 132-134 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Screening of various hormone-sensitive lipase inhibitors as endocannabinoid-hydrolyzing enzyme inhibitors

Minkkilä A, Savinainen JR, Käsnänen H, Xhaard H, Nevalainen T, Laitinen JT, Poso A, Leppänen J, Saario SM. 2009. Chemmedchem. 4: 1253-1259 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Visualization of 2-arachidonoylglycerol accumulation and cannabinoid CB1 receptor activity in rat brain cryosections by functional autoradiography

Palomäki VAB, Lehtonen M, Savinainen JR, Laitinen JT. 2007. Journal of neurochemistry. 101: 972-981 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data

Salo OMH, Savinainen JR, Parkkari T, Nevalainen T, Lahtela-Kakkonen M, Gynther J, Laitinen JT, Järvinen T, Poso A. 2006. Journal of medicinal chemistry. 49: 554-566 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Synthesis and in vitro evaluation of novel 2-oxo-1,2-dihydroquinoline CB2 receptor inverse agonists

Raitio KH, Savinainen JR, Nevalainen T, Järvinen T, Vepsäläinen J. 2006. Chemical biology and drug design. 68: 334-340 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor

Savinainen JR, Kokkola T, Salo OMH, Poso A, Järvinen T, Laitinen JT. 2005. British journal of pharmacology. 145: 636-645 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Optimized Methods to Determine Ligand Activities at the Cannabinoid CB1 and CB2 Receptors

Savinainen J. 2005. Kuopion yliopiston julkaisuja C. Luonnontieteet ja ympäristötieteet G5 Artikkeliväitöskirja

S-Nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific manner

Kokkola T, Savinainen JR, Mönkkönen KS, Retamal MD, Laitinen JT. 2005. Bmc cell biology. 6: 21 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor

Salo OMH, Raitio KH, Savinainen JR, Nevalainen T, Lahtela-Kakkonen M, Laitinen JT, Järvinen T, Poso A. 2005. Journal of medicinal chemistry. 48: 7166-7171 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Detection of cannabinoid CB1, adenosine A1, muscarinic acetylcholine, and GABAB receptor-dependent G protein activity in transducin-deactivated membranes and autoradiography sections of rat retina

Savinainen JR, Laitinen JT. 2004. Cellular and molecular neurobiology. 24: 243-256 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranes

Saario SM, Savinainen JR, Laitinen JT, Järvinen T, Niemi R. 2004. Biochemical pharmacology. 67: 1381-1387 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives

Parkkari T, Savinainen JR, Rauhala AL, Tolonen TL, Nevalainen T, Laitinen JT, Gynther J, Järvinen T. 2004. Bioorganic and medicinal chemistry letters. 14: 3231-3234 A1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä

Tarkenna hakuasi

Tutkimusryhmät

Avainsanat

5-Aminothiazoles Reveal a New Ligand-Binding Site on Prolyl Oligopeptidase Which is Important for Modulation of Its Protein–Protein Interaction-Derived Functions

A prolyl oligopeptidase inhibitor reduces tau pathology in cellular models and in mice with tauopathy

Potent dual MAGL/FAAH inhibitor AKU-005 engages endocannabinoids to diminish meningeal nociception implicated in migraine pain

Utilizing PET and MALDI Imaging for Discovery of a Targeted Probe for Brain Endocannabinoid α/β Hydrolase Domain 6 (ABHD6)

Inhibiting Endocannabinoid Hydrolysis as Emerging Analgesic Strategy Targeting a Spectrum of Ion Channels Implicated in Migraine Pain

Metabolomics of Synovial Fluid and Infrapatellar Fat Pad in Patients with Osteoarthritis or Rheumatoid Arthritis

Distinct Activity of Endocannabinoid-Hydrolyzing Enzymes MAGL and FAAH in Key Regions of Peripheral and Central Nervous System Implicated in Migraine

Evaluation of FASN inhibitors by a versatile toolkit reveals differences in pharmacology between human and rodent FASN preparations and in antiproliferative efficacy in vitro vs. in situ in human cancer cells

High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections - Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils

Regulating membrane lipid levels at the synapse by small-molecule inhibitors of monoacylglycerol lipase: new developments in therapeutic and PET imaging applications

Discovery of 12-Thiazole Abietanes as Selective Inhibitors of the Human Metabolic Serine Hydrolase hABHD16A

Design, Synthesis, and Biological Evaluation of 2,4-Dihydropyrano[2,3-c]pyrazole Derivatives as Autotaxin Inhibitors

Synthesis and preclinical evaluation of [11C]MA-PB-1 for in vivo imaging of brain monoacylglycerol lipase (MAGL)

A sensitive and versatile fluorescent activity assay for ABHD12

A sensitive and versatile fluorescent activity assay for ABHD6

Chemoproteomic, biochemical and pharmacological approaches in the discovery of inhibitors targeting human alfa/beta-hydrolase domain containing 11 (ABHD11)

In vivo characterization of the ultrapotent monoacylglycerol lipase inhibitor {4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl} (1H-1,2,4-triazol-1-yl)methanone (JJKK-048)

Increased tonic cannabinoid CB1R activity and brain region-specific desensitization of CB1R Gi/o signaling axis in mice with global genetic knockout of monoacylglycerol lipase

Loratadine analogues as MAGL inhibitors

New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity

Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists

Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors

1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor

Biochemical and Pharmacological Characterization of the Human Lymphocyte Antigen B-Associated Transcript 5 (BAT5/ABHD16A)

Discovery of triterpenoids as reversible inhibitors of alpha/ß-hydrolase domain containing 12 (ABHD12)

Optimization of 1,2,5-thiadiazole carbamates as potent and selective ABHD6 inhibitors

Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL)

Robust hydrolysis of prostaglandin glycerol esters by human monoacylglycerol lipase (MAGL)

Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands

Brain regional cannabinoid CB1 receptor signalling and alternative enzymatic pathways for 2-arachidonoylglycerol generation in brain sections of diacylglycerol lipase deficient mice

Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors

Mutation of Cys242 of human monoacylglycerol lipase disrupts balanced hydrolysis of 1- and 2-monoacylglycerols and selectively impairs inhibitor potency

Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase

Biochemical and pharmacological characterization of human &#945 /&#946 -hydrolase domain containing 6 (ABHD6) and 12 (ABHD12)

The serine hydrolases MAGL, ABHD6 and ABHD12 as guardians of 2-arachidonoylglycerol signalling through cannabinoid receptors

Characterization of binding properties of monoglyceride lipase inhibitors by a versatile fluorescene-based technique

Screening of various hormone-sensitive lipase inhibitors as endocannabinoid-hydrolyzing enzyme inhibitors

Visualization of 2-arachidonoylglycerol accumulation and cannabinoid CB1 receptor activity in rat brain cryosections by functional autoradiography

3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data

Synthesis and in vitro evaluation of novel 2-oxo-1,2-dihydroquinoline CB2 receptor inverse agonists

Identification of WIN55212-3 as a competitive neutral antagonist of the human cannabinoid CB2 receptor

Optimized Methods to Determine Ligand Activities at the Cannabinoid CB1 and CB2 Receptors

S-Nitrosothiols modulate G protein-coupled receptor signaling in a reversible and highly receptor-specific manner

Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor

Detection of cannabinoid CB1, adenosine A1, muscarinic acetylcholine, and GABAB receptor-dependent G protein activity in transducin-deactivated membranes and autoradiography sections of rat retina

Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranes

Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives