Small molecule Mcl-1 inhibitors for the treatment of cancer

J Belmar, SW Fesik - Pharmacology & therapeutics, 2015 - Elsevier
J Belmar, SW Fesik
Pharmacology & therapeutics, 2015Elsevier
The Bcl-2 family of proteins serves as primary regulators of apoptosis. Myeloid cell leukemia
1 (Mcl-1), a pro-survival member of the Bcl-2 family of proteins, is overexpressed and the Mcl-
1 gene is amplified in many tumor types. Moreover, the overexpression of Mcl-1 is the cause
of resistance to several chemotherapeutic agents. Thus, Mcl-1 is a promising cancer target.
This review highlights the current progress on the discovery of small molecule Mcl-1
inhibitors.
Abstract
The Bcl-2 family of proteins serves as primary regulators of apoptosis. Myeloid cell leukemia 1 (Mcl-1), a pro-survival member of the Bcl-2 family of proteins, is overexpressed and the Mcl-1 gene is amplified in many tumor types. Moreover, the overexpression of Mcl-1 is the cause of resistance to several chemotherapeutic agents. Thus, Mcl-1 is a promising cancer target. This review highlights the current progress on the discovery of small molecule Mcl-1 inhibitors.
Elsevier