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 …
over 370 structures in total bound to different ligands and the receptors in various …
Structure determination of GPCRs: cryo-EM compared with X-ray crystallography
J García-Nafría, CG Tate - Biochemical Society Transactions, 2021 - portlandpress.com
G protein-coupled receptors (GPCRs) are the largest single family of cell surface receptors
encoded by the human genome and they play pivotal roles in co-ordinating cellular systems …
encoded by the human genome and they play pivotal roles in co-ordinating cellular systems …
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 …
Structural basis of odorant recognition by a human odorant receptor
CB Billesbølle, CA de March, WJC van der Velden… - Nature, 2023 - nature.com
Our sense of smell enables us to navigate a vast space of chemically diverse odour
molecules. This task is accomplished by the combinatorial activation of approximately 400 …
molecules. This task is accomplished by the combinatorial activation of approximately 400 …
Variable G protein determinants of GPCR coupling selectivity
G protein-coupled receptors (GPCRs) activate four families of heterotrimeric G proteins, and
individual receptors must select a subset of G proteins to produce appropriate cellular …
individual receptors must select a subset of G proteins to produce appropriate cellular …
Proton uptake mechanism in bacteriorhodopsin captured by serial synchrotron crystallography
Conformational dynamics are essential for proteins to function. We adapted time-resolved
serial crystallography developed at x-ray lasers to visualize protein motions using …
serial crystallography developed at x-ray lasers to visualize protein motions using …
Cryo-EM structures of GPCRs coupled to Gs, Gi and Go
J García-Nafría, CG Tate - Molecular and Cellular Endocrinology, 2019 - Elsevier
Advances in electron cryo-microscopy (cryo-EM) now permit the structure determination of G
protein-coupled receptors (GPCRs) coupled to heterotrimeric G proteins by single-particle …
protein-coupled receptors (GPCRs) coupled to heterotrimeric G proteins by single-particle …
Structural basis for allosteric ligand recognition in the human CC chemokine receptor 7
The CC chemokine receptor 7 (CCR7) balances immunity and tolerance by homeostatic
trafficking of immune cells. In cancer, CCR7-mediated trafficking leads to lymph node …
trafficking of immune cells. In cancer, CCR7-mediated trafficking leads to lymph node …
Cryo-electron microscopy: moving beyond X-ray crystal structures for drug receptors and drug development
J García-Nafría, CG Tate - Annual review of pharmacology and …, 2020 - annualreviews.org
Electron cryo-microscopy (cryo-EM) has revolutionized structure determination of membrane
proteins and holds great potential for structure-based drug discovery. Here we discuss the …
proteins and holds great potential for structure-based drug discovery. Here we discuss the …
An online resource for GPCR structure determination and analysis
G-protein-coupled receptors (GPCRs) transduce physiological and sensory stimuli into
appropriate cellular responses and mediate the actions of one-third of drugs. GPCR …
appropriate cellular responses and mediate the actions of one-third of drugs. GPCR …