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implications for interpreting EC50 shifts, partial agonism, and assay readouts—especially in systems with constitutive orthosterically, allosterically, or with mixed mechanisms—and why that matters for interpreting EC₅₀ shifts and constitutive

At some sites, such as at somatotrophs, GHSR1a has high constitutive activity. Typically, ghrelin-dependent and constitutive GHSR1a activation occurs via Gαq/11 pathways.

At equilibrium, these effects cancel. But kinetics unmasks them.

Further research will be needed to boost our understanding on the dynamics and biological relevance of

September 2022 "Class A (rhodopsin-like) G protein-coupled receptors (GPCRs) are constitutive phospholipid

We showed a diversity of ligand-free forms of CCR5 at the cell surface constituted of various oligomeric

dynamics (MD) simulation studies have shown PI(4,5)P2 interacting with the Glucagon receptor (GCGR), which constitutes

fatty acid receptor GPR84 is a G protein-coupled receptor primarily expressed in myeloid cells that constitute

Cholesterol-Induced Thermal Stability to the Serotonin 1A Receptor "G protein-coupled receptors (GPCRs) constitute

Constitutive G protein-coupled M33 signalling is required for these phenotypes, although the contribution M33 engages Gq/11 to constitutively activate phospholipase C β (PLCβ) and downstream cyclic AMP response-element

class of signaling proteins exemplified by the visual receptor rhodopsin and its apoprotein opsin, are constitutively

GPR3 is unique in its ability to constitutively activate the Gαs protein without a ligand, which elevates

Previous reports demonstrated that Fgr exhibits high constitutive activity, but can be further activated

involves a key region in the central core of the GABAB2 transmembrane domain, which also controls the constitutive

In brainstem slices, intracellular constitutively active ROCK2 (aROCK2) led to H1152-sensitive HMN hyper-excitability