Biased allosteric modulators: new frontiers in GPCR drug discovery
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 …
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 …
in recent decades. In electrochemiluminescence (ECL) sensing area, nanomaterials have …
PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome
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 …
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 …
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 …
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 …
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
Wnt signaling transduces evolutionarily conserved pathways which play important roles in
initiating and regulating a diverse range of cellular activities, including cell proliferation …
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
Heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors constitute
the largest family of eukaryotic signal transduction proteins that communicate across the …
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 …
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 …
excited state donor D (usually a fluorophore) transfers energy to a proximal ground state …