Results 141 to 150 of about 22,949 (304)

The study of allosteric modulator sites at the cannabinoid CB1 receptor [PDF]

, 2009
Org 27569, Org 27759 and Org 29647 are the first discovered allosteric modulators of the cannabinoid CB1 receptor. These ligands are thought to bind to "accessory binding sites" at the receptor . Binding of the Org allosteric modulators has been shown to
Barber, Teresa S., NC DOCKS at The University of North Carolina at Greensboro   +1 more
core  

Structural pharmacology of SV2A reveals an allosteric modulation mechanism in the major facilitator superfamily

Nature Communications
The synaptic vesicle glycoprotein 2A (SV2A), a member of the major facilitator superfamily (MFS), is a key target for antiseizure medications and a biomarker for synaptic density imaging.
Shabareesh Pidathala, Xiao Chen, Yaxin Dai, Long N. Nguyen, Christoph Gorgulla, Yiming Niu, Fangyu Liu, Chia-Hsueh Lee   +7 more
doaj   +1 more source

Computational analysis of negative and positive allosteric modulator binding and function in metabotropic glutamate receptor 5 (in)activation

, 2014
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets because of their involvement in several neurological disease states, and mGluR5 in particular is a subtype whose controlled allosteric modulation, both ...
Dalton, James A. R., Gómez-Santacana, Xavier, Llebaria, Amadeu, Giraldo, Jesús   +3 more
core   +1 more source

Direct activation of M1 muscarinic receptors by the positive allosteric modulator, BQCA

, 2014
BQCA (Benzyl quinolone carboxylic acid) was recently identified as a positive allosteric modulator of the M1 muscarinic receptor. We studied the nature of this effect on muscarinic signaling at the single cell level in Chinese Hamster Ovary (CHO) cells ...
Brinker, Katherine
core  

Zinc as Allosteric Ion Channel Modulator: Ionotropic Receptors as Metalloproteins

, 2016
Zinc is an essential metal to life. This transition metal is a structural component of many proteins and is actively involved in the catalytic activity of cell enzymes. In either case, these zinc-containing proteins are metalloproteins.
Francisco Peralta, Juan Huidobro-Toro
core   +1 more source

Allosteric activation of the glutamate receptor mGlu2 by the serotonin receptor 5-HT2A

Nature Communications
G protein-coupled receptor (GPCR) dimers and higher-order oligomers are the subject of intense debates. The complexes formed between two or more different GPCRs enable the cell to integrate several signals.
Siyu Gai, Li Lin, Jiyong Meng, Yichen Wu, Li Xue, Chanjuan Xu, Qian Sun, Adrià Ricarte, James Dalton, Pedro Renault, Jesús Giraldo, Jean-Philippe Pin, Philippe Rondard, Jianfeng Liu   +13 more
doaj   +1 more source

Protein allosteric site identification using machine learning and per amino acid residue reported internal protein nanoenvironment descriptors

Computational and Structural Biotechnology Journal
Allosteric regulation plays a crucial role in modulating protein functions and represents a promising strategy in drug development, offering enhanced specificity and reduced toxicity compared to traditional active site inhibition.
Folorunsho Bright Omage, José Augusto Salim, Ivan Mazoni, Inácio Henrique Yano, Luiz Borro, Jorge Enrique Hernández Gonzalez, Fabio Rogerio de Moraes, Poliana Fernanda Giachetto, Ljubica Tasic, Raghuvir Krishnaswamy Arni, Goran Neshich   +10 more
doaj   +1 more source

Computational Analysis of Negative and Positive Allosteric Modulator Binding and Function in Metabotropic Glutamate Receptor 5 (In)Activation

, 2016
Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets because of their involvement in several neurological disease states, and mGluR5 in particular is a subtype whose controlled allosteric modulation, both ...
Xavier Gómez-Santacana (2106892), Amadeu Llebaria (1626844), Jesús Giraldo (1558987), James A. R. Dalton (2106895)   +3 more
core   +1 more source

An Agonist/Antagonist Photo‐Switchable Vitamin D Mimetic Enables Bidirectional Optical Control of VDR

Angewandte Chemie International Edition, EarlyView.
Vitamin D exhibits complex and cell‐specific biological effects in multiple tissues via activation of the ligand‐sensing transcription factor vitamin D receptor (VDR). The photo‐switchable vitamin D mimetic 10 transitions between VDR antagonist (E) and agonist (Z) activity upon illumination and offers unprecedented bidirectional optical control over ...
Xiu Ge, Sabine Willems, Francesco Melfi, Tufan Mukhopadhyay, Johannes Morstein, Jordan Artzy, Loris Knümann, Giorgia Sbriccoli, Jörg Pabel, Julian A. Marschner, Dirk Trauner, Daniel Merk   +11 more
wiley   +1 more source

Zuranolone: A case study in (regulatory) rush to judgement?

British Journal of Clinical Pharmacology, EarlyView.
Abstract Sage, in collaboration with Biogen, submitted a new drug approval for zuranolone for postpartum depression (PPD) and major depressive disorder (MDD) in December 2022. In August 2023, the US Food and Drug Administration granted approval for PPD but denied approval for MDD.
Lisa Cosgrove, Milutin Kostic, Barbara Mintzes, Gianna D'Ambrozio, Allen Shaughnessy   +4 more
wiley   +1 more source