Progress on the development of Class A GPCR-biased ligands

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F25%3A00636707" target="_blank" >RIV/67985823:_____/25:00636707 - isvavai.cz</a>

Result on the web

<a href="https://doi.org/10.1111/bph.17301" target="_blank" >https://doi.org/10.1111/bph.17301</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1111/bph.17301" target="_blank" >10.1111/bph.17301</a>

Result language

angličtina

Original language name

Progress on the development of Class A GPCR-biased ligands

Original language description

Class A G protein-coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and therapeutic value. In this context, the elucidation of biased signalling has opened up new pharmacological avenues holding promise for safer therapeutics. Functionally selective ligands favour receptor conformations facilitating the recruitment of specific effectors and the modulation of the associated pathways. This review surveys the current drug discovery landscape of GPCR-biased modulators with a focus on recent advances. Understanding the biological effects of this preferential coupling is at different stages depending on the Class A GPCR family. Therefore, with a focus on individual GPCR families, we present a compilation of the functionally selective modulators reported over the past few years. In doing so, we dissect their therapeutic relevance, molecular determinants and potential clinical applications.

Czech name

—

Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

30104 - Pharmacology and pharmacy

Project

<a href="/en/project/GA23-04670S" target="_blank" >GA23-04670S: Structure-activity guided design of novel long-acting antagonists of muscarinic receptors</a><br>

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2025

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

British Journal of Pharmacology

ISSN

0007-1188

e-ISSN

1476-5381

Volume of the periodical

182

Issue of the periodical within the volume

14

Country of publishing house

US - UNITED STATES

Number of pages

52

Pages from-to

3249-3300

UT code for WoS article

001309737800001

EID of the result in the Scopus database

2-s2.0-85203714534