Structural insights into ligand recognition and selectivity for classes A, B, and C GPCRs
The G protein-coupled receptor (GPCR) superfamily constitutes the largest collection of cell
surface signaling proteins with approximately 800 members in the human genome. GPCRs …
surface signaling proteins with approximately 800 members in the human genome. GPCRs …
Discovery of GPCR ligands by molecular docking screening: novel opportunities provided by crystal structures
D Rodríguez, A Ranganathan… - Current Topics in …, 2015 - ingentaconnect.com
G protein-coupled receptors (GPCRs) constitute the largest group of human membrane
proteins and have received significant attention in drug discovery for their important roles in …
proteins and have received significant attention in drug discovery for their important roles in …
A molecular pharmacologist's guide to G protein–coupled receptor crystallography
CL Piscitelli, J Kean, C de Graaf, X Deupi - Molecular pharmacology, 2015 - ASPET
G protein–coupled receptor (GPCR) structural biology has progressed dramatically in the
last decade. There are now over 120 GPCR crystal structures deposited in the Protein Data …
last decade. There are now over 120 GPCR crystal structures deposited in the Protein Data …
From G protein-coupled receptor structure resolution to rational drug design
A Jazayeri, JM Dias, FH Marshall - Journal of Biological Chemistry, 2015 - ASBMB
A number of recent technical solutions have led to significant advances in G protein-coupled
receptor (GPCR) structural biology. Apart from a detailed mechanistic view of receptor …
receptor (GPCR) structural biology. Apart from a detailed mechanistic view of receptor …
Chemical diversity in the G protein-coupled receptor superfamily
G protein-coupled receptors (GPCRs) are the largest family of cell signaling transmembrane
proteins that can be modulated by a plethora of chemical compounds. Systematic …
proteins that can be modulated by a plethora of chemical compounds. Systematic …
Class A GPCRs: Structure, function, modeling and structure-based ligand design
G protein-coupled receptors (GPCRs), especially the class A, are the most heavily
investigated drug targets in the pharmaceutical industry. Tremendous efforts have been …
investigated drug targets in the pharmaceutical industry. Tremendous efforts have been …
The GPCR Network: a large-scale collaboration to determine human GPCR structure and function
G protein-coupled receptors (GPCRs) are targeted by∼ 30–40% of marketed drugs, and
their key roles in normal physiology and in disease demonstrate that an understanding of …
their key roles in normal physiology and in disease demonstrate that an understanding of …
Integrating structural and mutagenesis data to elucidate GPCR ligand binding
Highlights•A wealth of GPCR ligand binding site data is available from structures and
mutants.•Integrating structural and mutant data is a tool to design mutagenesis …
mutants.•Integrating structural and mutant data is a tool to design mutagenesis …
Progress in GPCR structure determination
X Qu, D Wang, B Wu - GPCRs, 2020 - Elsevier
G protein-coupled receptors (GPCRs) are widely distributed in the human body and trigger
cellular responses to a variety of extracellular stimuli. The diverse functions of GPCRs make …
cellular responses to a variety of extracellular stimuli. The diverse functions of GPCRs make …
Structural basis for G protein-coupled receptor activation
G protein-coupled receptors (GPCRs) are critical regulators of human physiology and make
up the largest single class of therapeutic drug targets. Although GPCRs regulate highly …
up the largest single class of therapeutic drug targets. Although GPCRs regulate highly …