Molecular mechanism and physiological functions of clathrin-mediated endocytosis

HT McMahon, E Boucrot - Nature reviews Molecular cell biology, 2011 - nature.com
Clathrin-mediated endocytosis is the endocytic portal into cells through which cargo is
packaged into vesicles with the aid of a clathrin coat. It is fundamental to neurotransmission …

Biased receptor signaling in drug discovery

T Kenakin - Pharmacological reviews, 2019 - ASPET
A great deal of experimental evidence suggests that ligands can stabilize different receptor
active states that go on to interact with cellular signaling proteins to form a range of different …

Lack of beta-arrestin signaling in the absence of active G proteins

M Grundmann, N Merten, D Malfacini, A Inoue… - Nature …, 2018 - nature.com
G protein-independent, arrestin-dependent signaling is a paradigm that broadens the
signaling scope of G protein-coupled receptors (GPCRs) beyond G proteins for numerous …

Distinct conformations of GPCR–β-arrestin complexes mediate desensitization, signaling, and endocytosis

TJ Cahill III, ARB Thomsen… - Proceedings of the …, 2017 - National Acad Sciences
β-Arrestins (βarrs) interact with G protein-coupled receptors (GPCRs) to desensitize G
protein signaling, to initiate signaling on their own, and to mediate receptor endocytosis …

Subcellular organization of GPCR signaling

K Eichel, M von Zastrow - Trends in Pharmacological Sciences, 2018 - cell.com
G protein-coupled receptors (GPCRs) comprise a large and diverse class of signal-
transducing receptors that undergo dynamic and isoform-specific membrane trafficking …

Structure and function of serotonin G protein-coupled receptors

JD McCorvy, BL Roth - Pharmacology & therapeutics, 2015 - Elsevier
Serotonin receptors are prevalent throughout the nervous system and the periphery, and
remain one of the most lucrative and promising drug discovery targets for disorders ranging …

Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET

Y Namkung, C Le Gouill, V Lukashova… - Nature …, 2016 - nature.com
Endocytosis and intracellular trafficking of receptors are pivotal to maintain physiological
functions and drug action; however, robust quantitative approaches are lacking to study …

β-Arrestin-mediated receptor trafficking and signal transduction

SK Shenoy, RJ Lefkowitz - Trends in pharmacological sciences, 2011 - cell.com
β-Arrestins function as endocytic adaptors and mediate trafficking of a variety of cell-surface
receptors, including seven-transmembrane receptors (7TMRs). In the case of 7TMRs, β …

Teaching old receptors new tricks: biasing seven-transmembrane receptors

S Rajagopal, K Rajagopal, RJ Lefkowitz - Nature reviews Drug …, 2010 - nature.com
Abstract Seven-transmembrane receptors (7TMRs; also known as G protein-coupled
receptors) are the largest class of receptors in the human genome and are common targets …

G protein–coupled receptor signaling through β-arrestin–dependent mechanisms

PY Jean-Charles, S Kaur… - Journal of cardiovascular …, 2017 - journals.lww.com
β-arrestin1 (or arrestin2) and β-arrestin2 (or arrestin3) are ubiquitously expressed cytosolic
adaptor proteins that were originally discovered for their inhibitory role in G protein–coupled …