title: Small molecule Mcl-1 inhibitors for the treatment of cancer.
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.
authors.affiliation: Department of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, TN 37232-0146, United States.
authors.forename: Johannes
authors.initials: J
authors.lastname: Belmar
authors.affiliation: Department of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, TN 37232-0146, United States. Electronic address: stephen.fesik@vanderbilt.edu.
authors.forename: Stephen W
authors.initials: SW
authors.lastname: Fesik
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D064549:Myeloid Cell Leukemia Sequence 1 Protein / Q000037:antagonists & inhibitors*; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; C579095:MCL1 protein, human; D064549:Myeloid Cell Leukemia Sequence 1 Protein
keywords: BH3-mimetic; Inhibitors; Mcl-1; Myeloid cell leukemia-1; Small molecule