NOV-980

NOV-980 is a novel phosphopeptide inhibitor of farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate (MVA) pathway. FPPS is responsible for the biosynthesis of isoprenoids like farnesyl pyrophosphate and geranylgeranyl pyrophosphate, which are essential for the post-translational prenylation of small guanosine triphosphatases (GTPases) such as Ras, Rho, and Rab. By inhibiting FPPS, NOV-980 disrupts the prenylation process, thereby modulating cellular signaling and survival pathways. This mechanism is particularly relevant in the treatment of bone-related diseases, where FPPS is a validated target for bisphosphonates, and in various cancers, including colorectal cancer (CRC), where the mevalonate pathway is often upregulated. NOV-980 was developed through a multidisciplinary approach involving computational modeling, biochemical assays, and biophysical techniques, demonstrating significant antiproliferative effects in CRC cell models.