Drug intelligence / Profile preview

gnrh-(1-5)

Development stage: Preclinical
Lead developer: The Uniformed Services University of the Health Sciences
Modality: Peptides
Administration: Intraperitoneal

Overview

GnRH-(1-5) is a bioactive pentapeptide metabolite (pGlu-His-Trp-Ser-Tyr) derived from the Gonadotropin-Releasing Hormone (GnRH) through cleavage by the metalloendopeptidase EP24.15 (Thimet oligopeptidase). While the parent GnRH molecule regulates reproductive function via the GnRH receptor, GnRH-(1-5) acts as a ligand for the orphan G protein-coupled receptor GPR101. Research indicates that GnRH-(1-5) promotes cell migration in endometrial cancer cell lines by transactivating the epidermal growth factor receptor (EGFR) and activating the ERK signaling pathway. It also increases the bioactivity of TGF-β, suggesting it plays a role in the local regulation of gynecologic tissues and potentially in the progression of hormone-responsive cancers.

Other names: LHRH-(1-5)pGlu-His-Trp-Ser-TyrGnRH1-(1-5)

Targets

XCR1 (X-C motif chemokine receptor 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)MAPK3 (Mitogen-activated protein kinase 1)GPR101 (G protein-coupled receptor 101)

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