TY - JOUR AU - Pándy-Szekeres, Gáspár AU - Esguerra, Mauricio AU - Hauser, Alexander S AU - Caroli, Jimmy AU - Munk, Christian AU - Pilger, Steven AU - Keserű, György Miklós AU - Kooistra, Albert J AU - Gloriam, David E TI - The G protein database, GproteinDb JF - NUCLEIC ACIDS RESEARCH J2 - NUCLEIC ACIDS RES VL - 50 PY - 2022 IS - D1 SP - 518 EP - 525 PG - 8 SN - 0305-1048 DO - 10.1093/nar/gkab852 UR - https://m2.mtmt.hu/api/publication/32544494 ID - 32544494 LA - English DB - MTMT ER - TY - JOUR AU - Bajusz, Dávid AU - Wade, Warren S. AU - Satała, Grzegorz AU - Bojarski, Andrzej J. AU - Ilaš, Janez AU - Ebner, Jessica AU - Grebien, Florian AU - Papp, Henrietta AU - Jakab, Ferenc AU - Douangamath, Alice AU - Fearon, Daren AU - von Delft, Frank AU - Schuller, Marion AU - Ahel, Ivan AU - Wakefield, Amanda AU - Vajda, Sándor AU - Gerencsér, János AU - Pallai, Péter AU - Keserű, György Miklós TI - Exploring protein hotspots by optimized fragment pharmacophores JF - NATURE COMMUNICATIONS J2 - NAT COMMUN VL - 12 PY - 2021 IS - 1 PG - 10 SN - 2041-1723 DO - 10.1038/s41467-021-23443-y UR - https://m2.mtmt.hu/api/publication/32044302 ID - 32044302 LA - English DB - MTMT ER - TY - JOUR AU - Egyed, Attila AU - Kelemen, Ádám Andor AU - Vass, Márton AU - Visegrády, András AU - Thee, Stephanie A. AU - Wang, Zhiyong AU - de Graaf, Chris AU - Brea, Jose AU - Loza, Maria Isabel AU - Leurs, Rob AU - Keserű, György Miklós TI - Controlling the selectivity of aminergic GPCR ligands from the extracellular vestibule JF - BIOORGANIC CHEMISTRY J2 - BIOORG CHEM VL - 111 PY - 2021 SN - 0045-2068 DO - 10.1016/j.bioorg.2021.104832 UR - https://m2.mtmt.hu/api/publication/31997728 ID - 31997728 LA - English DB - MTMT ER - TY - JOUR AU - Kooistra, Albert J AU - Mordalski, Stefan AU - Pándy-Szekeres, Gáspár AU - Esguerra, Mauricio AU - Mamyrbekov, Alibek AU - Munk, Christian AU - Keserű, György Miklós AU - Gloriam, David E TI - GPCRdb in 2021: integrating GPCR sequence, structure and function JF - NUCLEIC ACIDS RESEARCH J2 - NUCLEIC ACIDS RES VL - 49 PY - 2021 IS - D1 SP - D335 EP - D343 SN - 0305-1048 DO - 10.1093/nar/gkaa1080 UR - https://m2.mtmt.hu/api/publication/31817126 ID - 31817126 N1 - Funding Agency and Grant Number: Lundbeck FoundationLundbeckfonden [R218-2016-1266, R163-2013-16327]; EU Horizon 2020, Innovative Training Network SAFER [765657]; Independent Research Fund Denmark | Natural Sciences [8021-00173B]; Novo Nordisk FoundationNovo Nordisk FoundationNovocure Limited [NNF18OC0031226]; Alfred Benzon Foundation [ABF-0-0-312]; Polish National Science Center [HARMONIA 2015/18/M/NZ2/00423]; National Research, Development and Innovation Office, Hungary [National Brain Research Program]National Research, Development & Innovation Office (NRDIO) - Hungary [2017-1.2.1-NKP-201700002] Funding text: Lundbeck Foundation [R218-2016-1266] to C.M.; EU Horizon 2020, Innovative Training Network SAFER [765657], Independent Research Fund Denmark | Natural Sciences [8021-00173B], Lundbeck Foundation [R163-2013-16327], Novo Nordisk Foundation [NNF18OC0031226] to D.E.G.; Alfred Benzon Foundation [ABF-0-0-312], Polish National Science Center [HARMONIA 2015/18/M/NZ2/00423] to S.M.; National Research, Development and Innovation Office, Hungary [National Brain Research Program, 2017-1.2.1-NKP-201700002 to G.M.K.]. Funding for open access charge: the Novo Nordisk Foundation [NNF18OC0031226]. LA - English DB - MTMT ER - TY - JOUR AU - Orgován, Zoltán AU - Ferenczy, György AU - Keserű, György Miklós TI - Allosteric Molecular Switches in Metabotropic Glutamate Receptors JF - CHEMMEDCHEM J2 - CHEMMEDCHEM VL - 16 PY - 2021 IS - 1 SP - 81 EP - 93 PG - 14 SN - 1860-7179 DO - 10.1002/cmdc.202000444 UR - https://m2.mtmt.hu/api/publication/31698584 ID - 31698584 AB - Metabotropic glutamate receptors (mGlu) are class C G protein-coupled receptors of eight subtypes that are omnipresently expressed in the central nervous system. mGlus have relevance in several psychiatric and neurological disorders, therefore they raise considerable interest as drug targets. Allosteric modulators of mGlus offer advantages over orthosteric ligands owing to their increased potential to achieve subtype selectivity, and this has prompted discovery programs that have produced a large number of reported allosteric mGlu ligands. However, the optimization of allosteric ligands into drug candidates has proved to be challenging owing to induced-fit effects, flat or steep structure-activity relationships and unexpected changes in theirpharmacology. Subtle structural changes identified as molecular switches might modulate the functional activity of allosteric ligands. Here we review these switches discovered in the metabotropic glutamate receptor family.. LA - English DB - MTMT ER - TY - JOUR AU - Prokop, Susanne Clara AU - Ábrányi-Balogh, Péter AU - Barti, Benjámin AU - Vámosi, Márton György AU - Zöldi, Miklós AU - Barna, László AU - Katona-Urbán, Gabriella AU - Tóth, András AU - Dudok, Barna AU - Egyed, Attila AU - Deng, Hui AU - Leggio, Gian Marco AU - Hunyady, László AU - van der Stelt, Mario AU - Keserű, György Miklós AU - Katona, István TI - PharmacoSTORM nanoscale pharmacology reveals cariprazine binding on Islands of Calleja granule cells JF - NATURE COMMUNICATIONS J2 - NAT COMMUN VL - 12 PY - 2021 IS - 1 PG - 19 SN - 2041-1723 DO - 10.1038/s41467-021-26757-z UR - https://m2.mtmt.hu/api/publication/32491765 ID - 32491765 N1 - Momentum Laboratory of Molecular Neurobiology, Institute of Experimental Medicine, Budapest, Hungary School of Ph.D. Studies, Semmelweis University, Budapest, Hungary Medicinal Chemistry Research Group, Research Centre for Natural Sciences, Budapest, Hungary Department of Psychological and Brain Sciences, Indiana University, Bloomington, IN, United States Nikon Center of Excellence for Neuronal Imaging, Institute of Experimental Medicine, Budapest, Hungary Department of Physiology, Faculty of Medicine, Semmelweis University, Budapest, Hungary MTA-SE Laboratory of Molecular Physiology, Eötvös Loránd Research Network, Budapest, Hungary Department of Neurosurgery, Stanford University, Stanford, CA, United States Department of Molecular Physiology, Leiden Institute of Chemistry, Leiden University & Oncode Institute, Leiden, Netherlands Department of Biomedical and Biotechnological Sciences, Section of Pharmacology, University of Catania, Catania, Italy Cited By :3 Export Date: 18 May 2022 Correspondence Address: Katona, I.; Momentum Laboratory of Molecular Neurobiology, Hungary; email: katona@koki.hu Chemicals/CAS: cariprazine, 839712-12-8, 1083076-69-0, 955400-75-6; cariprazine; Piperazines; Receptors, Dopamine D2; Receptors, Dopamine D3 Funding details: National Institutes of Health, NIH, R01DA044925, R01NS099457 Funding details: Nederlandse Organisatie voor Wetenschappelijk Onderzoek, NWO Funding details: Ministero dell’Istruzione, dell’Università e della Ricerca, MIUR, 201779W93T Funding details: Università di Catania, UNICT Funding details: Innovációs és Technológiai Minisztérium, ÚNKP-19-3-III-SE-16, ÚNKP-20-3-II-SE-33 Funding details: National Research, Development and Innovation Office, 129961, PD124598, VEKOP-2.3.3-15-2016-00013 Funding text 1: The authors are grateful to B. Pintér and E. Tischler for their laboratory support. The authors thank Drs. J. Brunner, K. Mackie, P. Somogyi, and J. Szabadics for valuable discussions and comments on the manuscript. The help of Drs. P. Vági, C. Pongor, the Nikon Microscopy Center at the Institute of Experimental Medicine, Nikon Europe B.V., Nikon Austria GmbH, and Auro-Science Consulting is acknowledged for kindly providing microscopy support. The authors are also grateful to Drs. E. Horváth, K. Kenesei, M. Kisfali, Z. Lele, Z. László, G. Balla, F. Mógor, and J. Glavinics for their experimental advice in laboratory work. The authors are indebted to Dr. B. Gereben for providing the Grenier Luminometer and HEK 293 cells. The authors also thank the help of D. Kiss and Á. Kelemen for their help in chemical modeling and synthesis, and M. Jiang for performing the docking studies with DH-463. This study was supported by the National Brain Research Program (2017-1.2.1-NKP-2017-00002 for I.K. and G.M.K.), by the National Research, Development and Innovation Office, Hungary (VEKOP-2.3.3-15-2016-00013 for super-resolution microscopy development for I.K.; Frontier Program 129961 for cannabinoid research for I.K.; postdoctoral fellowship PD124598 for P.Á.-B., EFOP-3.6.3-VEKOP-16-2017-00009 scholarship for M.V.). I.K. holds the Naus Family Chair in Addiction Sciences in the Department of Psychological and Brain Sciences at Indiana University Bloomington and his work is also supported by the National Institutes of Health (R01NS099457 and R01DA044925). This study was also supported by the New National Excellence Program of the Ministry for Innovation and Technology (ÚNKP-20-3-II-SE-33 and ÚNKP-19-3-III-SE-16 to S.P. and B.B.); by the VICI-grant from the Netherlands Organization for Scientific Research and funding from Oncode Institute to M.v.d.S.; the Italian Ministry of University and Research (PRIN 2017-Prot. 201779W93T to G.M.L.) and the University of Catania Intramural Funds (Starting Grant 2020 to G.M.L.). LA - English DB - MTMT ER - TY - JOUR AU - Egyed, Attila AU - Domány-Kovács, Katalin AU - Koványi, Bence AU - Horti, Ferenc AU - Kurko, Dalma AU - Kiss, Dóra Judit AU - Pándy-Szekeres, Gáspár AU - Greiner, István AU - Keserű, György Miklós TI - Controlling receptor function from the extracellular vestibule of G-protein coupled receptors JF - CHEMICAL COMMUNICATIONS J2 - CHEM COMMUN VL - 56 PY - 2020 IS - 91 SP - 14167 EP - 14170 PG - 4 SN - 1359-7345 DO - 10.1039/D0CC05532H UR - https://m2.mtmt.hu/api/publication/31799297 ID - 31799297 N1 - Cited By :11 Export Date: 7 April 2024 CODEN: CHCOF LA - English DB - MTMT ER - TY - JOUR AU - Jójárt, Balázs AU - Orgován, Zoltán AU - Márki, Árpád AU - Pándy-Szekeres, Gáspár AU - Ferenczy, György AU - Keserű, György Miklós TI - Allosteric activation of metabotropic glutamate receptor 5 JF - JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS J2 - J BIOMOL STRUCT DYN VL - 38 PY - 2020 IS - 9 SP - 2624 EP - 2632 PG - 10 SN - 0739-1102 DO - 10.1080/07391102.2019.1638302 UR - https://m2.mtmt.hu/api/publication/30834454 ID - 30834454 LA - English DB - MTMT ER - TY - JOUR AU - Wakefield, Amanda E. AU - Mason, Jonathan S. AU - Vajda, Sandor AU - Keserű, György Miklós TI - Analysis of tractable allosteric sites in G protein-coupled receptors JF - SCIENTIFIC REPORTS J2 - SCI REP VL - 9 PY - 2019 IS - 1 SN - 2045-2322 DO - 10.1038/s41598-019-42618-8 UR - https://m2.mtmt.hu/api/publication/30763480 ID - 30763480 LA - English DB - MTMT ER -