Small molecule Mcl-1 inhibitors for the treatment of cancer

Pharmacol Ther. 2015 Jan;145:76-84. doi: 10.1016/j.pharmthera.2014.08.003. Epub 2014 Aug 27.


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.

Keywords: BH3-mimetic; Inhibitors; Mcl-1; Myeloid cell leukemia-1; Small molecule.

Publication types

  • Review

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Humans
  • Myeloid Cell Leukemia Sequence 1 Protein / antagonists & inhibitors*
  • Neoplasms / drug therapy
  • Neoplasms / metabolism


  • Antineoplastic Agents
  • MCL1 protein, human
  • Myeloid Cell Leukemia Sequence 1 Protein