Toward Targeting Antiapoptotic MCL-1 for Cancer Therapy
AuthorKelly, GL; Strasser, A
EditorJacks, T; Sawyers, CL
Source TitleAnnual Review of Cancer Biology
AffiliationMedical Biology (W.E.H.I.)
CitationsKelly, G. L. & Strasser, A. (2020). Toward Targeting Antiapoptotic MCL-1 for Cancer Therapy. Jacks, T (Ed.). Sawyers, CL (Ed.). ANNUAL REVIEW OF CANCER BIOLOGY, VOL 4, 4, pp.299-313. ANNUAL REVIEWS.
Access StatusOpen Access
Apoptosis is critical for embryonic development, tissue homeostasis, and the removal of infected or otherwise dangerous cells. It is controlled by three subgroups of the BCL-2 protein family—the BH3-only proteins that initiate cell death; the effectors of cell killing, BAX and BAK; and the antiapoptotic guardians, including MCL-1 and BCL-2. Defects in apoptosis can promote tumorigenesis and render malignant cells refractory to anticancer therapeutics. Activation of cell death by inhibiting antiapoptotic BCL-2 family members has emerged as an attractive strategy for cancer therapy, with the BCL-2 inhibitor venetoclax leading the way. Large-scale cancer genome analyses have revealed frequent amplification of the locus encoding antiapoptotic MCL-1 in human cancers, and functional studies have shown that MCL-1 is essential for the sustained survival and expansion of many types of tumor cells. Structural analysis and medicinal chemistry have led to the development of three distinct small-molecule inhibitors of MCL-1 that are currently undergoing clinical testing.
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