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Compound P
- Development stage
- Preclinical
- Lead developer
- Central South University
- Modality
- Small Molecules
01
Overview
Compound P is a natural small-molecule inhibitor that directly binds to the FERM, RhoGEF and pleckstrin domain-containing protein 1 (FARP1) with a dissociation constant (Kd) of 19.4 μM. FARP1 is a Rho-GEF family signal transduction protein that is progressively upregulated from primary to metastatic melanoma and acts as a key driver of melanoma metastasis. By directly binding to FARP1, Compound P inhibits FARP1-mediated activation of the small GTPase Rac1 (specifically downregulating Rac1-GTP levels), thereby uncoupling the FARP1-Rac1 signaling axis. This pharmacological blockade impairs melanoma cell migration and invasion in vitro and profoundly suppresses both lymph node and pulmonary metastasis in human melanoma xenograft models in vivo, without causing significant systemic toxicity.
- Other names
- Compound P
02
Targets
FARP1 (FERM, RhoGEF and pleckstrin domain-containing protein 1)
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