Impact of GPCR structures on drug discovery

M Congreve, C de Graaf, NA Swain, CG Tate - Cell, 2020 - cell.com
Structures of 70 unique G protein-coupled receptors (GPCRs) have been determined, with
over 370 structures in total bound to different ligands and the receptors in various …

[HTML][HTML] Wnt signaling: Essential roles in osteoblast differentiation, bone metabolism and therapeutic implications for bone and skeletal disorders

R Vlashi, X Zhang, M Wu, G Chen - Genes & diseases, 2023 - Elsevier
Wnt signaling executes an indispensable performance in osteoblast differentiation, bone
development, homeostasis, and remodeling. Wnt signals trigger the intracellular Wnt …

Common activation mechanism of class A GPCRs

Q Zhou, D Yang, M Wu, Y Guo, W Guo, L Zhong, X Cai… - Elife, 2019 - elifesciences.org
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …

Structure-based virtual screening for ligands of G protein–coupled receptors: what can molecular docking do for you?

F Ballante, AJ Kooistra, S Kampen, C de Graaf… - Pharmacological …, 2021 - Elsevier
G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …

International union of basic and clinical pharmacology. CXII: adenosine receptors: a further update

AP IJzerman, KA Jacobson, CE Müller… - Pharmacological …, 2022 - Elsevier
Abstract Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …

Advances in therapeutic peptides targeting G protein-coupled receptors

AP Davenport, CCG Scully, C de Graaf… - Nature Reviews Drug …, 2020 - nature.com
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …

GPCRomics: an approach to discover GPCR drug targets

PA Insel, K Sriram, MW Gorr, SZ Wiley… - Trends in …, 2019 - cell.com
G protein-coupled receptors (GPCRs) are targets for∼ 35% of approved drugs but only∼
15% of the∼ 800 human GPCRs are currently such targets. GPCRomics, the use of …

Ligand binding at the protein–lipid interface: strategic considerations for drug design

J Payandeh, M Volgraf - Nature Reviews Drug Discovery, 2021 - nature.com
Many drug targets are embedded within the phospholipid bilayer of cellular membranes,
including G protein-coupled receptors, ion channels, transporters and membrane-bound …

KLIFS: an overhaul after the first 5 years of supporting kinase research

GK Kanev, C de Graaf, BA Westerman… - Nucleic acids …, 2021 - academic.oup.com
Kinases are a prime target of drug development efforts with> 60 drug approvals in the past
two decades. Due to the research into this protein family, a wealth of data has been …

GPCRs involved in metabolic diseases: pharmacotherapeutic development updates

C **, H Chen, L **e, Y Zhou, L Liu, J Wu - Acta Pharmacologica Sinica, 2024 - nature.com
G protein-coupled receptors (GPCRs) are expressed in a variety of cell types and tissues,
and activation of GPCRs is involved in enormous metabolic pathways, including nutrient …