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Antagonists of IAP proteins: novel anti-tumor agents

Yichao Wan, Tingting Liu, Xuben Hou

  • 1Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44 West Wenhua Road, Jinan, PR China. haofangcn@sdu.edu.cn.

Current Medicinal Chemistry
|September 2, 2014
PubMed

Insights

Tumor cells resist cancer drugs by evading apoptosis. Inhibitor of apoptosis proteins (IAPs) promote cancer; targeting them with Smac-mimetic drugs can induce cancer cell death.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Evasion of apoptosis is a key mechanism of cancer drug resistance.
  • Inhibitor of apoptosis proteins (IAPs) are over-expressed in cancers like leukemia and lymphoma, promoting tumor growth.
  • IAPs inhibit caspases, crucial enzymes for programmed cell death.

Purpose of the Study:

  • To review the role of IAPs in apoptosis.
  • To discuss recent advances in developing IAP antagonists for cancer therapy.

Main Methods:

  • Review of scientific literature on IAPs and their antagonists.
  • Focus on structural biology studies of Smac-IAP interactions.
  • Analysis of therapeutic strategies targeting IAPs.

Main Results:

  • IAPs are critical regulators of apoptosis and are implicated in cancer development.
  • Second mitochondria-derived activator of caspases (Smac) antagonizes IAPs.
  • Smac utilizes an AVPI tetra-peptide motif to bind IAPs.

Conclusions:

  • Targeting IAPs represents a promising anti-cancer strategy.
  • Smac-mimetic agents designed to mimic the AVPI peptide can suppress IAPs.
  • This suppression leads to caspase activation and apoptosis induction in tumor cells.

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