TLK60404

TLK60404 is a small molecule inhibitor of Glutathione S-transferase P1-1 (GSTP1-1), an enzyme that is frequently overexpressed in a wide range of human cancers. Developed by Telik, Inc., TLK60404 was designed to address the role of GSTP1-1 in chemotherapy resistance and the regulation of cell survival pathways. In many cancer cells, GSTP1-1 binds to and sequesters c-Jun N-terminal kinase (JNK), thereby preventing the induction of apoptosis. By inhibiting GSTP1-1, TLK60404 facilitates the release and subsequent activation of JNK, which triggers the apoptotic cascade. This mechanism of action is intended to both directly induce cancer cell death and sensitize tumors to other chemotherapeutic agents. While it showed promise in preclinical models for solid tumors and hematological malignancies, its development was largely superseded by other compounds in Telik's pipeline, such as ezatiostat.

Other names

GSTP1-1 inhibitorGSTP-1-1 inhibitorGSTP 1-1 inhibitor