GPR101 Activators

GPR101 is an orphan G protein-coupled receptor (GPCR), meaning its endogenous ligand and physiological role are not well-defined. This receptor is predominantly expressed in the pituitary gland and the hypothalamus, regions of the brain that are critical for hormonal regulation and homeostasis. GPR101 has garnered significant interest due to its genetic association with X-linked acrogigantism (X-LAG), a condition characterized by excessive growth due to the overproduction of growth hormone.

The GPR101 gene is located on the X chromosome, and duplications in this gene are strongly linked to the development of X-LAG, suggesting that GPR101 overexpression leads to abnormal growth hormone secretion. This has led to the hypothesis that GPR101 may be involved in the signaling pathways that regulate pituitary function and growth hormone release.Despite its association with pathological growth, the normal physiological function of GPR101 remains elusive. It is speculated to be involved in neuroendocrine signaling given its expression profile. The receptor's activity and regulation could be influenced by various factors including hormones, intracellular messengers, and pharmacological agents, which may modulate its expression or activity.