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Impact of GPCR structures on drug discovery
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 …
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
Wnt signaling executes an indispensable performance in osteoblast differentiation, bone
development, homeostasis, and remodeling. Wnt signals trigger the intracellular Wnt …
development, homeostasis, and remodeling. Wnt signals trigger the intracellular Wnt …
Common activation mechanism of class A GPCRs
Class A G-protein-coupled receptors (GPCRs) influence virtually every aspect of human
physiology. Understanding receptor activation mechanism is critical for discovering novel …
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?
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 …
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
Abstract Our previous International Union of Basic and Clinical Pharmacology report on the
nomenclature and classification of adenosine receptors (2011) contained a number of …
nomenclature and classification of adenosine receptors (2011) contained a number of …
Advances in therapeutic peptides targeting G protein-coupled receptors
Dysregulation of peptide-activated pathways causes a range of diseases, fostering the
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
discovery and clinical development of peptide drugs. Many endogenous peptides activate G …
GPCRomics: an approach to discover GPCR drug targets
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 …
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 …
including G protein-coupled receptors, ion channels, transporters and membrane-bound …
KLIFS: an overhaul after the first 5 years of supporting kinase research
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 …
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 …
and activation of GPCRs is involved in enormous metabolic pathways, including nutrient …