Biased allosteric modulators: new frontiers in GPCR drug discovery

LM Slosky, MG Caron, LS Barak - Trends in Pharmacological Sciences, 2021 - cell.com
G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors in the
genome and the most successful family of targets of FDA-approved drugs. New frontiers in …

Nanomaterials-based sensitive electrochemiluminescence biosensing

Y Chen, S Zhou, L Li, J Zhu - Nano Today, 2017 - Elsevier
Nanomaterials with wonderful optical, electrical and chemical properties are widely studied
in recent decades. In electrochemiluminescence (ECL) sensing area, nanomaterials have …

PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

WK Kroeze, MF Sassano, XP Huang, K Lansu… - Nature structural & …, 2015 - nature.com
G protein–coupled receptors (GPCRs) are essential mediators of cellular signaling and are
important targets of drug action. Of the approximately 350 nonolfactory human GPCRs, more …

NanoBRET A Novel BRET Platform for the Analysis of Protein–Protein Interactions

T Machleidt, CC Woodroofe, MK Schwinn… - ACS chemical …, 2015 - ACS Publications
Dynamic interactions between proteins comprise a key mechanism for temporal control of
cellular function and thus hold promise for development of novel drug therapies. It remains …

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 …

New insights into modes of GPCR activation

W Wang, Y Qiao, Z Li - Trends in pharmacological sciences, 2018 - cell.com
In classical G-protein-coupled receptor (GPCR) activation, GPCRs couple to a variety of
heterotrimeric G proteins on the membrane and then activate downstream signaling …

[HTML][HTML] Wnt/β-catenin signaling plays an ever-expanding role in stem cell self-renewal, tumorigenesis and cancer chemoresistance

MK Mohammed, C Shao, J Wang, Q Wei, X Wang… - Genes & diseases, 2016 - Elsevier
Wnt signaling transduces evolutionarily conserved pathways which play important roles in
initiating and regulating a diverse range of cellular activities, including cell proliferation …

High-Resolution Crystal Structure of an Engineered Human β2-Adrenergic G Protein–Coupled Receptor

V Cherezov, DM Rosenbaum, MA Hanson… - science, 2007 - science.org
Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors constitute
the largest family of eukaryotic signal transduction proteins that communicate across the …

Single-molecule analysis of fluorescently labeled G-protein–coupled receptors reveals complexes with distinct dynamics and organization

D Calebiro, F Rieken, J Wagner… - Proceedings of the …, 2013 - National Acad Sciences
G-protein–coupled receptors (GPCRs) constitute the largest family of receptors and major
pharmacological targets. Whereas many GPCRs have been shown to form di-/oligomers, the …

Materials for fluorescence resonance energy transfer analysis: beyond traditional donor–acceptor combinations

KE Sapsford, L Berti, IL Medintz - … Chemie International Edition, 2006 - Wiley Online Library
Fluorescence resonance energy transfer (FRET) is a nonradiative process whereby an
excited state donor D (usually a fluorophore) transfers energy to a proximal ground state …