G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

Biased signalling: from simple switches to allosteric microprocessors

JS Smith, RJ Lefkowitz, S Rajagopal - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of receptors in the human
genome and some of the most common drug targets. It is now well established that GPCRs …

Analysis of aptamer discovery and technology

MR Dunn, RM Jimenez, JC Chaput - Nature Reviews Chemistry, 2017 - nature.com
Aptamers are nucleic acid molecules that mimic antibodies by folding into complex 3D
shapes that bind to specific targets. Although some aptamers exist naturally as the ligand …

Nanodiscs in membrane biochemistry and biophysics

IG Denisov, SG Sligar - Chemical reviews, 2017 - ACS Publications
Membrane proteins play a most important part in metabolism, signaling, cell motility,
transport, development, and many other biochemical and biophysical processes which …

Structural insights into G-protein-coupled receptor allostery

DM Thal, A Glukhova, PM Sexton, A Christopoulos - Nature, 2018 - nature.com
G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external
environmental cues into biochemical signals across the membrane. GPCRs are intrinsically …

Highly efficient expression of circular RNA aptamers in cells using autocatalytic transcripts

JL Litke, SR Jaffrey - Nature biotechnology, 2019 - nature.com
RNA aptamers and RNA aptamer-based devices can be genetically encoded and
expressed in cells to probe and manipulate cellular function. However, their usefulness in …

Bispecific aptamer induced artificial protein-pairing: a strategy for selective inhibition of receptor function

L Wang, H Liang, J Sun, Y Liu, J Li, J Li… - Journal of the …, 2019 - ACS Publications
Cell surface receptors play a critical role in modulating intracellular signal transduction,
making them important drug targets. However, it remains challenging to develop a selective …

Aptamers: Uptake mechanisms and intracellular applications

S Yoon, JJ Rossi - Advanced drug delivery reviews, 2018 - Elsevier
The structural flexibility and small size of aptamers enable precise recognition of cellular
elements for imaging and therapeutic applications. The process by which aptamers are …

GPCR-mediated β-arrestin activation deconvoluted with single-molecule precision

WB Asher, DS Terry, GGA Gregorio, AW Kahsai… - Cell, 2022 - cell.com
Summary β-arrestins bind G protein-coupled receptors to terminate G protein signaling and
to facilitate other downstream signaling pathways. Using single-molecule fluorescence …

Activated protein C, protease activated receptor 1, and neuroprotection

JH Griffin, BV Zlokovic… - Blood, The Journal of the …, 2018 - ashpublications.org
Protein C is a plasma serine protease zymogen whose active form, activated protein C
(APC), exerts potent anticoagulant activity. In addition to its antithrombotic role as a plasma …