GTPase-activating proteins or GTPase-accelerating proteins (GAPs) are a family of regulatory proteins whose members can bind to activated G proteins and stimulate their GTPase activity, with the result of terminating the signaling event. [1] .

Jun 1, 2007 · GEFs and GAPs are multidomain proteins that are regulated by extracellular signals and localized cues that control cellular events in time and space. Recent evidence suggests that these proteins may be potential therapeutic targets for developing drugs to treat various diseases, including cancer.

G protein-coupled receptors (GPCRs), also known as seven- (pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular res...

Explain the roles of GTPase-activating proteins (GAPs) in enhancing GTP hydrolysis and thereby turning off small G protein signaling. Describe how guanine nucleotide exchange factors (GEFs) promote the release of GDP and facilitate GTP binding, reactivating the small G proteins.

Eukaryotic cells sense and migrate toward chemoattractant gradients using G protein-coupled receptor (GPCR) signaling pathways. The fascinating feature of chemotaxis is that cells migrate through chemoattractant gradients with huge concentration ...

Heterotrimeric G proteins are major signaling hubs and essential components of the signal gating machinery in healthy eukaryotic cells. In the canonical scenario, activation of G proteins is triggered by agonist-bound GPCRs.

Nov 24, 2010 · Guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs) that control the GDP–GTP cycling of specific members of the Ras superfamily have been shown to contribute to...

Oct 22, 2022 · G protein-coupled receptors (GPCRs) are amongst the most pharmaceutically relevant and well-studied protein targets, yet unanswered questions in the field leave significant gaps in our understanding of their nuanced structure and function.

Apr 4, 2010 · We sought evidence from whole-cell GPCR signaling that could distinguish the contribution(s) of GAP and non-GAP functions of RGS proteins to the observations of accelerated kinetics, yet paradoxical lack of amplitude or sensitivity changes, attributed to RGS proteins.

G protein–coupled receptors (GPCRs) are integral membrane proteins that sense biologically salient cues and trigger appropriate responses through stimulus-dependent, allosteric interactions with intracellular transducer proteins (Hilger et al., 2018; Liu et al., 2024).Critical transducers of GPCR signaling are a family of heterotrimeric guanine nucleotide-binding proteins (G proteins).