CC chemokine receptor 9 (CCR9), an organ-specific chemokine receptor, interacts with its exclusive ligand

The structure demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies

In his collaboration with David Hodson, every major leap—from early ligand design to GPCR visualization

While the receptor with the crystal ligand (i.e. antagonist naltrindole) maintained the inactive conformation

Kenakin walks through cases where two equipotent ligands produce radically different clinical outcomes

The structures reveal distinctive ligand engaging model and activation conformations of GPR110.

Ligand-based pharmacophore modeling was performed since no 3D structure of human β3 -AR is yet available

From biased ligands to computational targeting, this is where the pipelines of the 2030s begin.

Their capabilities span cAMP, β-arrestin recruitment, receptor internalization, calcium flux, ligand

macrophages, but not erythroblasts and ECs, suggesting that macrophage ACKR1 engages its non-cognate ligand

Alterations in mouse visceral adipose tissue mRNA expression of islet G-protein-coupled receptor ligands conformational ensemble of CX3C chemokine receptor 1 (CX3CR1) and its interactions with antagonist and agonist ligands

Furthermore, we found that castration-resistant cells produced AVP, the endogenous ligand for arginine

assays were performed using PBMCs isolated from these individuals in response to the synthetic GPR15 ligand

AYPGKF peptide ligand activation of PAR4 induces EGF receptor (EGFR) Tyr-phosphorylation, effectively

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein

GPCR Activation and Signaling Homodimerization of CB2 cannabinoid receptor triggered by a bivalent ligand

GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates

However, opioids that prevent recruiting β-arrestin 2 do not address the problem since ligands that only Biased Opioid Ligands. Molecules. 2020 Sep 16;25(18):4257. doi: 10.3390/molecules25184257.

appropriate glucose homeostasis through their secretion of insulin, and islet function can be modified by ligands

within the transmembrane domain limits the identification and development of nonpeptide small molecule ligands

Value at a glance: From screens to hits —how to identify novel GPCR ligands with structure-based workflows

pharmacology series where Terry Kenakin breaks down receptor pharmacology, functional selectivity, and ligand

Adhesion GPCRs Optimized genetic code expansion technology for time-dependent induction of adhesion GPCR-ligand Reviews, GPCRs, and more NMR applications to GPCR recognition by peptide ligands.

Transporter affinity and solubility limits routinely sabotage otherwise strong ligands Effective PK

GPCR Binders, Drugs, and more Ligands selectively tune the local and global motions of neurotensin receptor Development and challenges in the discovery of 5-HT1A and 5-HT7 receptor ligands.

This article provides an extensive review on the current status of ligand development targeting LPA receptors

In rodents, intrathecal injection of its ligand, 7α,25-dihydroxycholesterol (7α,25-OHC), causes time-dependent

of progress in structural biology and pharmacology, predicting how  a GPCR will respond to a given ligand

These GPCRs and their probable ligands were predicted.

receptors (GPCRs) are cell surface receptors that mediate the function of a great variety of extracellular ligands