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Structural insights into G protein-coupled receptor signaling [PDF]

Structural Dynamics
G protein-coupled receptors (GPCRs) are the largest single family of transmembrane proteins encoded in the human genome, and they are among the most successful classes of therapeutic drug targets of all time.
Andrew Kruse
doaj   +2 more sources

The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)

Biomolecules, 2021
G protein-coupled receptors (GPCRs), which regulate a vast number of eukaryotic processes, are desensitized by various mechanisms but, most importantly, by the GPCR kinases (GRKs).
M. Claire Cato, Yu-Chen Yen, Charnelle J. Francis, Kaely E. Elkins, Afzaal Shareef, Rachel Sterne-Marr, John J. G. Tesmer   +6 more
doaj   +1 more source

DEER Analysis of GPCR Conformational Heterogeneity

Biomolecules, 2021
G protein-coupled receptors (GPCRs) represent a large class of transmembrane helical proteins which are involved in numerous physiological signaling pathways and therefore represent crucial pharmacological targets.
Matthias Elgeti, Wayne L. Hubbell
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G Protein-Coupled Receptor Kinases Take Central Stage

Cells, 2022
The relevance of the family of G protein-coupled receptor kinases (GRKs) is based on its key participation in the regulation and intracellular dynamics of the largest family of membrane receptors, namely G protein-coupled receptors (GPCRs) [...]
Federico Mayor, Cristina Murga
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Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology.

J Cell Sci
Pearce A, Redfern-Nichols T, Wills E, Rosa M, Manulak I, Sisk C, Huang X, Atakpa-Adaji P, Prole DL, Ladds G.   +9 more
europepmc   +2 more sources

Allosteric modulation of G protein-coupled receptor signaling

Frontiers in Endocrinology, 2023
G protein-coupled receptors (GPCRs), the largest family of transmembrane proteins, regulate a wide array of physiological processes in response to extracellular signals. Although these receptors have proven to be the most successful class of drug targets,
Siyuan Shen, Chang Zhao, Chao Wu, Suyue Sun, Ziyan Li, Wei Yan, Zhenhua Shao   +6 more
doaj   +1 more source

Creation of photocyclic vertebrate rhodopsin by single amino acid substitution

eLife, 2022
Opsins are universal photoreceptive proteins in animals and can be classified into three types based on their photoreaction properties. Upon light irradiation, vertebrate rhodopsin forms a metastable active state, which cannot revert back to the original
Kazumi Sakai, Yoshinori Shichida, Yasushi Imamoto, Takahiro Yamashita   +3 more
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C-terminal threonines and serines play distinct roles in the desensitization of rhodopsin, a G protein-coupled receptor

eLife, 2015
Rod photoreceptors generate measurable responses to single-photon activation of individual molecules of the G protein-coupled receptor (GPCR), rhodopsin.
Anthony W Azevedo, Thuy Doan, Hormoz Moaven, Iza Sokal, Faiza Baameur, Sergey A Vishnivetskiy, Kristoff T Homan, John JG Tesmer, Vsevolod V Gurevich, Jeannie Chen, Fred Rieke   +10 more
doaj   +1 more source

A G-Protein Coupled Receptor and Macular Degeneration

Cells, 2020
Age-related macular degeneration (AMD) is a leading cause of irreversible blindness in the world. The risk of AMD increases with age and is most common among the white population. Here, we discuss the convergence of factors related to race, pigmentation,
Anna G. Figueroa, Brian S. McKay
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Regulation Role of Non-Rhodopsin G Protein-coupled Receptor Kinases on Tumor

Zhongliu Fangzhi Yanjiu, 2019
G protein-coupled receptor kinases (GRKs) are involved in a wide range of cellular physiology and pathological activities by specifically phosphorylating activated G-protein coupled receptors (GPCRs) to terminate GPCR signaling and phosphorylating non ...
LI Ruirui, JIANG Xiaoshan
doaj   +1 more source