Membrane receptor activation mechanisms and transmembrane peptide tools to elucidate them.

ABSTRACT: Single-pass membrane receptors contain extracellular domains that respond to external stimuli and transmit information to intracellular domains through a single transmembrane (TM) α-helix. Because membrane receptors have various roles in homeostasis, signaling malfunctions of these receptors can cause disease. Despite their importance, there is still much to be understood mechanistically about how single-pass receptors are activated. In general, single-pass receptors respond to extracellular stimuli via alterations in their oligomeric state. The details of this process are still the focus of intense study, and several lines of evidence indicate that the TM domain (TMD) of the receptor plays a central role. We discuss three major mechanistic hypotheses for receptor activation: ligand-induce

SUBMITTER: Westerfield JM 

PROVIDER: S-EPMC7029107 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature