Results 41 to 50 of about 131,252 (300)

Allosteric modulators targeting CNS muscarinic receptors [PDF]

, 2018
Muscarinic acetylcholine receptors are G protein-coupled receptors (GPCRs) which are broadly expressed in the central nervous system (CNS) and other tissues in the periphery.
Mohr, K., Andreas Bock, Schrage, R., Ramona Schrage, Klaus Mohr, Bock, A.   +5 more
core   +1 more source

Deconstructing Allostery: Computational Assessment of the Binding Determinants of Allosteric PTP1B Modulators [PDF]

, 2023
It is currently challenging to predict whether fragment hits that do not bind to an orthosteric site could be elaborated into allosteric modulators, as in these cases binding does not necessarily translate into a functional effect.
Silvia, Lovera, Adele, Hardie, Benjamin P, Cossins, Julien, Michel   +3 more
core   +2 more sources

Allosteric modulation of adenosine receptors [PDF]

Purinergic Signalling, 2008
Allosteric ligands for G protein-coupled receptors (GPCRs) may alter receptor conformations induced by an orthosteric ligand. These modulators can thus fine-tune classical pharmacological responses. In this review we will describe efforts to synthesize and characterize allosteric modulators for one particular GPCR subfamily, the adenosine receptors ...
Göblyös, Anikó, IJzerman, Ad P.
openaire   +3 more sources

Allosteric modulation of gonadotropin receptors

Frontiers in Endocrinology, 2023
Gonadotropins regulate reproductive functions by binding to G protein-coupled receptors (FSHR and LHCGR) expressed in the gonads. They activate multiple, cell-specific signalling pathways, consisting of ligand-dependent intracellular events. Signalling cascades may be modulated by synthetic compounds which bind allosteric sites of FSHR and LHCGR or by ...
Clara Lazzaretti, Manuela Simoni, Manuela Simoni, Manuela Simoni, Livio Casarini, Livio Casarini, Elia Paradiso   +6 more
openaire   +3 more sources

Design, Synthesis and Characterization of a New Series of Fluorescent Metabotropic Glutamate Receptor Type 5 Negative Allosteric Modulators

Molecules, 2020
In recent years, new drug discovery approaches based on novel pharmacological concepts have emerged. Allosteric modulators, for example, target receptors at sites other than the orthosteric binding sites and can modulate agonist-mediated activation ...
Víctor Fernández-Dueñas, Mingcheng Qian, Josep Argerich, Carolina Amaral, Martijn D.P. Risseeuw, Serge Van Calenbergh, Francisco Ciruela   +6 more
doaj   +1 more source

Pharmacological hallmarks of allostery at the M4 muscarinic receptor elucidated through structure and dynamics

eLife, 2023
Allosteric modulation of G protein-coupled receptors (GPCRs) is a major paradigm in drug discovery. Despite decades of research, a molecular-level understanding of the general principles that govern the myriad pharmacological effects exerted by GPCR ...
Ziva Vuckovic, Jinan Wang, Vi Pham, Jesse I Mobbs, Matthew J Belousoff, Apurba Bhattarai, Wessel AC Burger, Geoff Thompson, Mahmuda Yeasmin, Vindhya Nawaratne, Katie Leach, Emma T van der Westhuizen, Elham Khajehali, Yi-Lynn Liang, Alisa Glukhova, Denise Wootten, Craig W Lindsley, Andrew Tobin, Patrick Sexton, Radostin Danev, Celine Valant, Yinglong Miao, Arthur Christopoulos, David M Thal   +23 more
doaj   +1 more source

The Action of Positive Allosteric Modulators of the GABAAR Can Be Reversed by Novel Spiro Barbiturates [PDF]

GABAARs are pentameric ligand-gated ion channels that play a major role in mediating inhibition in the CNS. They are the target of many widely used positive allosteric modulators (PAMs) of GABAARs such as general anesthetics, sedatives, antiepileptics ...
Keith W., Miller, Karol S., Bruzik, Dimosthenis, Koinas, Xiaojuan, Zhou, Bo, Wu   +4 more
core   +2 more sources

Modulation of Allosteric Control and Evolution of Hemoglobin

Biomolecules, 2023
Allostery arises when a ligand-induced change in shape of a binding site of a protein is coupled to a tertiary/quaternary conformational change with a consequent modulation of functional properties. The two-state allosteric model of Monod, Wyman and Changeux [J. Mol. Biol.
Maurizio Brunori, Adriana Erica Miele
openaire   +4 more sources

Allosteric modulation of glycine receptors [PDF]

British Journal of Pharmacology, 2011
Inhibitory (or strychnine-sensitive) glycine receptors (GlyRs) are anion-selective transmitter-gated ion channels of the cys-loop superfamily, which includes among others also the inhibitory γ-aminobutyric acid receptors (GABA(A) receptors). While GABA mediates fast inhibitory neurotransmission throughout the CNS, the action of glycine as a fast ...
Yévenes, G E, Zeilhofer, Hanns Ulrich
openaire   +4 more sources

Synthesis of Novel Nicotinic Ligands with Multimodal Action: Targeting Acetylcholine α4β2, Dopamine and Serotonin Transporters

Molecules, 2019
Nicotinic acetylcholine receptors (nAChRs), serotonin transporters (SERT) and dopamine transporters (DAT) represent targets for the development of novel nicotinic derivatives acting as multiligands associated with different health conditions, such as ...
Juan Pablo González-Gutiérrez, Hernán Armando Pessoa-Mahana, Patricio Ernesto Iturriaga-Vásquez, Miguel Iván Reyes-Parada, Nicolas Esteban Guerra-Díaz, Martin Hodar-Salazar, Franco Viscarra, Pablo Paillali, Gabriel Núñez-Vivanco, Marcos Antonio Lorca-Carvajal, Jaime Mella-Raipán, María Carolina Zúñiga   +11 more
doaj   +1 more source