Results 31 to 40 of about 13,221 (154)

Allosteric Modulation of the CB1 Cannabinoid Receptor by Cannabidiol—A Molecular Modeling Study of the N-Terminal Domain and the Allosteric-Orthosteric Coupling

Molecules, 2021
The CB1 cannabinoid receptor (CB1R) contains one of the longest N termini among class A G protein-coupled receptors. Mutagenesis studies suggest that the allosteric binding site of cannabidiol (CBD) involves residues from the N terminal domain.
Jakub Jakowiecki, Renata Abel, Urszula Orzeł, Paweł Pasznik, Robert Preissner, Sławomir Filipek   +5 more
doaj   +1 more source

Peptides in BioNMR Research

CHIMIA, 2021
Heteronuclear NMR in combination with isotope labelling is used to study folding of polypeptides induced by metals in the case of metallothioneins, binding of the peptidic allosteric modulator ρ-TIA to the human G-protein coupled α1b adrenergic receptor,
Oliver Zerbe, Christian Baumann, Matthias Schuster, Kerstin Moehle, Kathryn K. Oi, Erich Michel   +5 more
doaj   +1 more source

Allostery of atypical modulators at oligomeric G protein-coupled receptors

Scientific Reports, 2021
Many G protein-coupled receptors (GPCRs) are therapeutic targets, with most drugs acting at the orthosteric site. Some GPCRs also possess allosteric sites, which have become a focus of drug discovery.
Rabindra V. Shivnaraine, Brendan Kelly, Gwendolynne Elmslie, Xi-Ping Huang, Yue John Dong, Margaret Seidenberg, James W. Wells, John Ellis   +7 more
doaj   +1 more source

Correction: Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator

eLife, 2018
Joan Font, Marc López-Cano, Serena Notartomaso, Pamela Scarselli, Paola Di Prieto, Roger Bresolí-Obach, Giuseppe Battaglia, Fanny Malhaire, Xavier Rovira, Juanlo Catena, Jesús Giraldo, Jean-Philippe Pin, Víctor Fernández-Dueñas, Cyril Goudet, Santi Nonell, Ferdinando Nicoletti, Amadeu Llebaria, Francisco Ciruela   +17 more
doaj   +2 more sources

Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer

eLife, 2017
GPCRs play critical roles in cell communication. Although GPCRs can form heteromers, their role in signaling remains elusive. Here we used rat metabotropic glutamate (mGlu) receptors as prototypical dimers to study the functional interaction between each
Junke Liu, Zongyong Zhang, David Moreno-Delgado, James AR Dalton, Xavier Rovira, Ana Trapero, Cyril Goudet, Amadeu Llebaria, Jesús Giraldo, Qilin Yuan, Philippe Rondard, Siluo Huang, Jianfeng Liu, Jean-Philippe Pin   +13 more
doaj   +1 more source

Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]

Bioorganic & Medicinal Chemistry Letters, 2016
Les modulateurs allostériques négatifs (MNA) CB1 existants appartiennent à une gamme limitée de classes structurelles. Malgré le potentiel théorique des NAM CB1, les études in vivo publiées n'ont généralement pas été en mesure de démontrer les effets thérapeutiques attendus médiés par CB1.
Iain R. Greig, Gemma L. Baillie, Mostafa H. Abdelrahman, Laurent Trembleau, Ruth A. Ross   +4 more
openaire   +3 more sources

Dataset for Phase I randomized clinical trial for safety and tolerability of GET 73 in single and repeated ascending doses including preliminary pharmacokinetic parameters

Data in Brief, 2017
The data in this article outline the methods used for the administration of GET 73 in the first time-in-human manuscript entitled “Phase I randomized clinical trial for the safety, tolerability and preliminary pharmacokinetics of the mGluR5 negative ...
Carolina L. Haass-Koffler, Kimberly Goodyear, Victoria M. Long, Harrison H. Tran, Antonella Loche, Roberto Cacciaglia, Robert M. Swift, Lorenzo Leggio   +7 more
doaj   +1 more source

Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition

Communications Biology, 2020
Kennedy et al. report the pharmacological and in vivo profiling of two small molecule PAR2 inhibitors and an agonist. They conclude that while the small molecule agonist and one of the inhibitors bind to the orthosteric PAR2 binding site, the other ...
Amanda J. Kennedy, Linda Sundström, Stefan Geschwindner, Eunice K. Y. Poon, Yuhong Jiang, Rongfeng Chen, Rob Cooke, Shawn Johnstone, Andrew Madin, Junxian Lim, Qingqi Liu, Rink-Jan Lohman, Anneli Nordqvist, Maria Fridén-Saxin, Wenzhen Yang, Dean G. Brown, David P. Fairlie, Niek Dekker   +17 more
doaj   +1 more source

Negative Allosteric Modulators That Target Human α4β2 Neuronal Nicotinic Receptors [PDF]

The Journal of Pharmacology and Experimental Therapeutics, 2010
Allosteric modulation of neuronal nicotinic acetylcholine receptors (nAChRs) is considered to be one of the most promising approaches for therapeutics. We have previously reported on the pharmacological activity of several compounds that act as negative allosteric modulators (NAMs) of nAChRs.
Brandon J, Henderson, Ryan E, Pavlovicz, Jerad D, Allen, Tatiana F, González-Cestari, Crina M, Orac, Andrew B, Bonnell, Michael X, Zhu, R Thomas, Boyd, Chenglong, Li, Stephen C, Bergmeier, Dennis B, McKay   +10 more
openaire   +2 more sources

Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine [v1; ref status: indexed, http://f1000r.es/o0]

F1000Research, 2013
We investigated the role of metabotropic glutamate receptor type 5 (mGluR5) in methamphetamine-induced behavioral sensitization. The mGluR5 positive allosteric modulator (3-cyano-N-(1,3-diphenyl-1H-pyrazol-5-yl) benzamide (CDPPB) and negative allosteric ...
Peter R Kufahl, Natali E Nemirovsky, Lucas R Watterson, Nicholas Zautra, M Foster Olive   +4 more
doaj   +1 more source