Results 141 to 150 of about 61,856 (262)

Decoding functional specialization in G protein‐coupled receptors (GPCRs) through evolution‐guided residue profiling

British Journal of Pharmacology, EarlyView.
Background and Purpose G protein‐coupled receptors (GPCRs) are integral membrane proteins that mediate physiological processes by enabling cells to detect and respond to diverse stimuli. Although many subfamily‐specific functional hotspots have been described, the family‐wide determinants of common and subfamily‐specific functions remain incomplete ...
Berkay Selçuk, Gunnar Schulte, Igor B. Zhulin, Ogün Adebali   +3 more
wiley   +1 more source

GPCR systems coordinate cellular resilience against aging-associated stress. [PDF]

Front Mol Biosci
Boeringer T, Pardo M, Craig CJ, Gutierrez AN, Duckett DR, McDonald P, Maudsley S.   +6 more
europepmc   +1 more source

Peripheral targets for neuropathic pain

British Journal of Pharmacology, EarlyView.
Neuropathic pain represents a significant clinical challenge, with still limited pharmacological approaches to symptomatic relief. This review focuses on molecular targets implicated in neuropathic pain, particularly those involved in peripheral mechanisms. Using the IUPHAR/BPS database of biological targets, their occurrence together with ‘neuropathic
Amirhossein Afsharipour, Cosmin I. Ciotu, Felix J. Resch, Michael J. M. Fischer   +3 more
wiley   +1 more source

Recent Advances in GPCR Ligand Discovery Using DNA-Encoded Library Technology: From Affinity Binding to Functional Bias and Allosteric Modulation. [PDF]

ACS Med Chem Lett
Zhou R, Wang J, Li X, An Y.
europepmc   +1 more source

The chemokine receptor‐like fourth extracellular loop of the apelin receptor differentially regulates apelin and elabela binding and signalling

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Apelin and Elabela are endogenous ligands of the apelin receptor (apelin receptor/APJ), a GPCR involved in cardiovascular regulation and body fluid homeostasis. The human receptor contains a conserved disulfide bridge linking the N‐terminal domain to extracellular loop 3 (ECL3) via Cys19 and Cys281, forming a structural ...
Chloé Bonef, Hela Bouhsine, Carine Huynh, Marion Chaigneau, Steven Dubois, Mikel Garcia‐Marcos, Catherine Llorens‐Cortes, Denis Servent, Philippe Robin, Hervé Nozach, Isabel Alves, Xavier Iturrioz   +11 more
wiley   +1 more source

The GPCR Connection: Linking Alzheimer's Disease and Glioblastoma. [PDF]

J Cell Mol Med
Caniceiro AB, Agostinho SP, Piochi LF, Rosário-Ferreira N, Moreira IS.   +4 more
europepmc   +1 more source

Dualsteric and dual‐acting modulation of muscarinic receptors by antagonist KH‐5

British Journal of Pharmacology, EarlyView.
Abstract Background and purpose Muscarinic acetylcholine receptors are key therapeutic targets, and ligands engaging both orthosteric and allosteric sites may offer improved selectivity and efficacy. Here, we investigated whether the muscarinic antagonist KH‐5 acts as a dualsteric antagonist and defined its mode of interaction with muscarinic receptors.
Alena Janoušková‐Randáková, Eva Dolejší, Nikolai Chetverikov, Jan Jakubík   +3 more
wiley   +1 more source

Host GPCR-cAMP signaling balances Gαs and Gαi activity to control intracellular <i>Brucella</i> infection. [PDF]

mBio
Kang Y-S, Kirby JE.
europepmc   +1 more source

Cannabinoid CB1 allosteric ligands suppress inflammatory pain in male mice without tolerance, motor impairment, memory deficits or respiratory depression

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Positive allosteric modulators (PAMs) engage sites distinct from the orthosteric CB1 cannabinoid receptor binding site. GAT211, a racemic ligand, contains GAT228 (R) and GAT229 (S) enantiomers. Whether enantiomer‐mediated differences in allosteric activation or positive allosteric modulation translate into differences in
Ifeoluwa D. Solomon, Sumanta Garai, Ganesh A. Thakur, Andrea G. Hohmann   +3 more
wiley   +1 more source

Novel roles of GPCRs in the renal collecting duct. [PDF]

Physiology (Bethesda)
Kui MK, Zhang JJ, Pluznick JL.
europepmc   +1 more source