Targeting G protein-coupled receptor signalling by blocking G proteins

AP Campbell, AV Smrcka - Nature reviews Drug discovery, 2018 - nature.com
G protein-coupled receptors (GPCRs) are the largest class of drug targets, largely owing to
their druggability, diversity and physiological efficacy. Many drugs selectively target specific …

The expanding roles of Gβγ subunits in G protein–coupled receptor signaling and drug action

SM Khan, R Sleno, S Gora, P Zylbergold… - Pharmacological …, 2013 - ASPET
G βγ subunits from heterotrimeric G proteins perform a vast array of functions in cells with
respect to signaling, often independently as well as in concert with G α subunits. However …

A photoswitchable GPCR-based opsin for presynaptic inhibition

BA Copits, R Gowrishankar, PR O'Neill, JN Li… - Neuron, 2021 - cell.com
Optical manipulations of genetically defined cell types have generated significant insights
into the dynamics of neural circuits. While optogenetic activation has been relatively …

[HTML][HTML] Diversity of the Gβγ complexes defines spatial and temporal bias of GPCR signaling

I Masuho, NK Skamangas, BS Muntean… - Cell systems, 2021 - cell.com
The signal transduction by G-protein-coupled receptors (GPCRs) is mediated by
heterotrimeric G proteins composed from one of the 16 Gα subunits and the inseparable Gβγ …

G-protein βγ subunits as multi-functional scaffolds and transducers in G-protein-coupled receptor signaling

AV Smrcka, I Fisher - Cellular and Molecular Life Sciences, 2019 - Springer
G-protein βγ subunits are key participants in G-protein signaling. These subunits facilitate
interactions between receptors and G proteins that are critical for the G protein activation …

[HTML][HTML] Optogenetic approaches for dissecting neuromodulation and GPCR signaling in neural circuits

SM Spangler, MR Bruchas - Current opinion in pharmacology, 2017 - Elsevier
Highlights•Optogenetic tools provide precise spatial and temporal control of GPCR
signaling.•Light-sensitive proteins can be engineered for GPCR-specific applications.• …

Subtype-dependent regulation of Gβγ signalling

M Tennakoon, K Senarath, D Kankanamge… - Cellular signalling, 2021 - Elsevier
G protein-coupled receptors (GPCRs) transmit information to the cell interior by transducing
external signals to heterotrimeric G protein subunits, Gα and Gβγ subunits, localized on the …

Gβγ subunits—Different spaces, different faces

SM Khan, JY Sung, TE Hebert - Pharmacological research, 2016 - Elsevier
Gβγ subunits play key roles in modulation of canonical effectors in G protein-coupled
receptor (GPCR)-dependent signalling at the cell surface. However, a number of recent …

Golgi-resident Gαo promotes protrusive membrane dynamics

GP Solis, O Bilousov, A Koval, AM Lüchtenborg, C Lin… - Cell, 2017 - cell.com
To form protrusions like neurites, cells must coordinate their induction and growth. The first
requires cytoskeletal rearrangements at the plasma membrane (PM), the second requires …

Optically triggering spatiotemporally confined GPCR activity in a cell and programming neurite initiation and extension

WKA Karunarathne, L Giri… - Proceedings of the …, 2013 - National Acad Sciences
G-protein–coupled receptor (GPCR) activity gradients evoke important cell behavior but
there is a dearth of methods to induce such asymmetric signaling in a cell. Here we …