G protein-coupled receptors (GPCRs): advances in structures, …
2024年4月10日 · Considering both receptor constitutive activity and drug efficacy, GPCR ligands are categorized as (full) agonists, partial agonists, antagonists, and inverse agonists.
G protein-coupled receptors: structure- and function-based …
2021年1月8日 · As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to …
How ligands illuminate GPCR molecular pharmacology - PMC
Recent structural and molecular studies have both transformed and expanded classical concepts of receptor pharmacology and begun to illuminate the distinct mechanisms by which …
G protein-coupled receptors (GPCRs): advances in structures, …
The efficacy of diverse ligands acting on a single GPCR in terms of activation or inactivation also varies widely. Considering both receptor constitutive activity and drug efficacy, GPCR ligands …
G protein-coupled receptors: structure- and function-based …
Biased signaling, allosteric modulation, and polypharmacology are helping us better understand how GPCRs bind to numerous ligands and how they transmit diverse signals to elicit …
Mechanisms of signalling and biased agonism in G protein …
2018年8月13日 · A key advancement has been provided by the concept of biased agonism, which describes the ability of ligands acting at the same GPCR to elicit distinct cellular signalling …
Structure, function and drug discovery of GPCR signaling
2023年12月4日 · Agonists bind to GPCRs and trigger downstream G-protein or β-arrestin signaling. Antagonists occupy the agonism-associated pocket and prevent endogenous ligand …
How Ligands Illuminate GPCR Molecular Pharmacology
2017年7月27日 · G protein-coupled receptors (GPCRs), which are modulated by a variety of endogenous and synthetic ligands, represent the largest family of druggable targets in the …
Biased Ligands of G Protein-Coupled Receptors (GPCRs): …
2018年6月25日 · Biased ligands selective for either pathway are expected to regulate biological functions of GPCRs in a more precise way, therefore providing new drug molecules with …
Orphan G protein-coupled receptors (GPCRs): biological
2012年2月27日 · GPCRs are the most successful targets of modern medicine, and approximately 36% of marketed pharmaceuticals target human GPCRs. However, the endogenous ligands of …