apratoxin S8

Apratoxin S8 is a synthetic cyclodepsipeptide analog of the marine cyanobacterial natural product apratoxin A. Developed by Oceanyx Pharmaceuticals and originated at the University of Florida, apratoxin S8 acts as a potent inhibitor of the Sec61 translocon, specifically targeting the SEC61 translocon subunit alpha 1 (SEC61A1). By blocking cotranslational translocation in the endoplasmic reticulum, it prevents the biogenesis, glycosylation, and trafficking of secretory and membrane-bound proteins, including receptor tyrosine kinases (RTKs) and growth factors. This leads to downstream proteasomal degradation of these proteins, resulting in potent antiproliferative and antiangiogenic activity. Apratoxin S8 is being explored for the treatment of cancer and angiogenic disorders, and is also being investigated as an antibody-drug conjugate (ADC) payload.

Other names

Apratoxin S8