TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome

RHJ Olsen, JF DiBerto, JG English, AM Glaudin… - Nature chemical …, 2020 - nature.com
G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete
understanding of how they signal through 16 non-visual G-protein signal transducers …

Protein functional landscapes, dynamics, allostery: a tortuous path towards a universal theoretical framework

PI Zhuravlev, GA Papoian - Quarterly reviews of biophysics, 2010 - cambridge.org
Energy landscape theories have provided a common ground for understanding the protein
folding problem, which once seemed to be overwhelmingly complicated. At the same time …

Targeting G protein-coupled receptor signaling at the G protein level with a selective nanobody inhibitor

S Gulati, H Jin, I Masuho, T Orban, Y Cai… - Nature …, 2018 - nature.com
G protein-coupled receptors (GPCRs) activate heterotrimeric G proteins by mediating a GDP
to GTP exchange in the Gα subunit. This leads to dissociation of the heterotrimer into Gα …

Molecular targeting of Gα and Gβγ subunits: a potential approach for cancer therapeutics

AV Smrcka - Trends in pharmacological sciences, 2013 - cell.com
G-Protein-coupled receptors (GPCRs) signal through G protein α and βγ subunit families to
regulate a wide range of physiological and pathophysiological processes. As such, GPCRs …

Heterotrimeric G proteins as therapeutic targets in drug discovery

J Li, Y Ge, JX Huang, K Strømgaard… - Journal of medicinal …, 2019 - ACS Publications
Heterotrimeric G proteins are molecular switches in GPCR signaling pathways and regulate
a plethora of physiological and pathological processes. GPCRs are efficient drug targets …

[PDF][PDF] Update 1 of: computational modeling approaches to structure–function analysis of G protein-coupled receptors

F Fanelli, PG De Benedetti - Chemical Reviews-Columbus, 2011 - researchgate.net
Any aspect of cell activity is regulated by extracellular signals that are recognized, decoded,
and transduced inside the cell via different classes of plasma membrane receptors. 1À3 G …

Mapping the conformational landscape of the stimulatory heterotrimeric G protein

SK Huang, LP Picard, RSM Rahmatullah… - Nature Structural & …, 2023 - nature.com
Heterotrimeric G proteins serve as membrane-associated signaling hubs, in concert with
their cognate G-protein-coupled receptors. Fluorine nuclear magnetic resonance …

NMR studies of protein–ligand interactions

M Goldflam, T Tarragó, M Gairí, E Giralt - Protein NMR techniques, 2012 - Springer
Nuclear magnetic resonance (NMR) has evolved into a powerful tool for characterizing
protein–ligand interactions in solution under near physiological conditions. It is now …

Direct-reversible binding of small molecules to G protein βγ subunits

A Seneviratne, M Burroughs, E Giralt… - Biochimica et Biophysica …, 2011 - Elsevier
Heterotrimeric guanine nucleotide-binding proteins (G proteins) composed of three subunits
α, β, γ mediate activation of multiple intracellular signaling cascades initiated by G protein …

Differential large-amplitude breathing motions in the interface of FKBP12–drug complexes

CJ Yang, M Takeda, T Terauchi, JG Jee… - Biochemistry, 2015 - ACS Publications
The tight complexes FKBP12 forms with immunosuppressive drugs, such as FK506 and
rapamycin, are frequently used as models for developing approaches to structure-based …