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 …

Emerging diversity in lipid–protein interactions

V Corradi, BI Sejdiu, H Mesa-Galloso… - Chemical …, 2019 - ACS Publications
Membrane lipids interact with proteins in a variety of ways, ranging from providing a stable
membrane environment for proteins to being embedded in to detailed roles in complicated …

GPCR dynamics: structures in motion

NR Latorraca, AJ Venkatakrishnan, RO Dror - Chemical reviews, 2017 - ACS Publications
The function of G protein-coupled receptors (GPCRs) which represent the largest class of
both human membrane proteins and drug targets depends critically on their ability to …

Regulation, signaling, and physiological functions of G-proteins

V Syrovatkina, KO Alegre, R Dey, XY Huang - Journal of molecular biology, 2016 - Elsevier
Heterotrimeric guanine-nucleotide-binding regulatory proteins (G-proteins) mainly relay the
information from G-protein-coupled receptors (GPCRs) on the plasma membrane to the …

Structural insights into µ-opioid receptor activation

W Huang, A Manglik, AJ Venkatakrishnan… - Nature, 2015 - nature.com
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective
analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X …

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

Y Kang, XE Zhou, X Gao, Y He, W Liu, A Ishchenko… - Nature, 2015 - nature.com
G-protein-coupled receptors (GPCRs) signal primarily through G proteins or arrestins.
Arrestin binding to GPCRs blocks G protein interaction and redirects signalling to numerous …

High-resolution crystal structure of the human CB1 cannabinoid receptor

Z Shao, J Yin, K Chapman, M Grzemska, L Clark… - Nature, 2016 - nature.com
The human cannabinoid G-protein-coupled receptors (GPCRs) CB1 and CB2 mediate the
functional responses to the endocannabinoids anandamide and 2-arachidonyl glycerol (2 …

Microbial and animal rhodopsins: structures, functions, and molecular mechanisms

OP Ernst, DT Lodowski, M Elstner, P Hegemann… - Chemical …, 2014 - ACS Publications
Organisms of all domains of life use photoreceptor proteins to sense and respond to light.
The light-sensitivity of photoreceptor proteins arises from bound chromophores such as …

Molecular signatures of G-protein-coupled receptors

AJ Venkatakrishnan, X Deupi, G Lebon, CG Tate… - Nature, 2013 - nature.com
G-protein-coupled receptors (GPCRs) are physiologically important membrane proteins that
sense signalling molecules such as hormones and neurotransmitters, and are the targets of …

GPCR drug discovery: integrating solution NMR data with crystal and cryo-EM structures

I Shimada, T Ueda, Y Kofuku, MT Eddy… - Nature Reviews Drug …, 2019 - nature.com
The 826 G protein-coupled receptors (GPCRs) in the human proteome regulate key
physiological processes and thus have long been attractive drug targets. With the crystal …