Drug intelligence / Profile preview

SR-18292

Development stage
Preclinical
Lead developer
Scripps Research
Modality
Small Molecules
Administration
Intraperitoneal, Intragastric
01

Overview

SR-18292 is a small molecule modulator of Peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α), a master regulator of mitochondrial biogenesis and oxidative metabolism. In the majority of preclinical research, SR-18292 is characterized as a PGC-1α inhibitor that functions by increasing the acetylation of the protein, thereby suppressing its transcriptional activity. This inhibition has been explored as a therapeutic strategy for non-alcoholic fatty liver disease (NAFLD), various cancers (including melanoma, renal cell carcinoma, and oral cancer), and fibrotic conditions of the lung and kidney. Conversely, recent research in the context of sickle cell disease has described SR-18292 as an inducer of PGC-1α that promotes fetal hemoglobin expression, suggesting a potential therapeutic role in hemoglobinopathies. It was developed through a collaboration involving the Dana-Farber Cancer Institute and Scripps Research.

02

Targets

KAT2A (Lysine acetyltransferase 2A)PPARGC1A (Peroxisome proliferator–activated receptor gamma coactivator 1-alpha)

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