GPCR signaling regulation: the role of GRKs and arrestins

VV Gurevich, EV Gurevich - Frontiers in pharmacology, 2019 - frontiersin.org
Every animal species expresses hundreds of different G protein-coupled receptors (GPCRs)
that respond to a wide variety of external stimuli. GPCRs-driven signaling pathways are …

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 …

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 …

Structure of the nanobody-stabilized active state of the kappa opioid receptor

T Che, S Majumdar, SA Zaidi, P Ondachi, JD McCorvy… - Cell, 2018 - cell.com
The κ-opioid receptor (KOP) mediates the actions of opioids with hallucinogenic, dysphoric,
and analgesic activities. The design of KOP analgesics devoid of hallucinatory and …

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 …

The molecular basis of G protein–coupled receptor activation

WI Weis, BK Kobilka - Annual review of biochemistry, 2018 - annualreviews.org
G protein–coupled receptors (GPCRs) mediate the majority of cellular responses to external
stimuli. Upon activation by a ligand, the receptor binds to a partner heterotrimeric G protein …

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 …

Update on melatonin receptors: IUPHAR Review 20

R Jockers, P Delagrange… - British journal of …, 2016 - Wiley Online Library
Melatonin receptors are seven transmembrane‐spanning proteins belonging to the GPCR
superfamily. In mammals, two melatonin receptor subtypes exist‐MT1 and MT2‐encoded by …

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 …

Activation and allosteric modulation of a muscarinic acetylcholine receptor

AC Kruse, AM Ring, A Manglik, J Hu, K Hu, K Eitel… - Nature, 2013 - nature.com
Despite recent advances in crystallography and the availability of G-protein-coupled
receptor (GPCR) structures, little is known about the mechanism of their activation process …