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Inhibitor of Apoptosis Protein (IAP) Antagonists in Anticancer Agent Discovery: Current Status and Perspectives

Hui Cong1,2, Lijuan Xu1,2, Yougen Wu3,4

  • 1School of Pharmacy , Ningxia Medical University , 1160 Shengli Street , Yinchuan 750004 , China.

Journal of Medicinal Chemistry
|January 25, 2019
PubMed

Insights

Cancer cells resist apoptosis, a key cell death process. SMAC-mimetic inhibitors of apoptosis proteins (IAPs) show promise in restoring apoptosis for cancer treatment by disrupting IAP function.

Area of Science:

  • Molecular Biology
  • Cellular Biology
  • Cancer Research

Background:

  • Apoptosis, or programmed cell death, is crucial for eliminating damaged cells.
  • Cancer cells often evade apoptosis, contributing to treatment resistance.
  • Inhibitor of Apoptosis Proteins (IAPs) are key regulators that promote cancer cell survival.

Purpose of the Study:

  • To review the functions of IAPs.
  • To explore the structural interactions between IAPs and SMAC.
  • To discuss the development and clinical evaluation of SMAC-mimetic IAP antagonists.

Main Methods:

  • Literature review focusing on research from the past 15 years.
  • Analysis of structural interactions between IAPs and SMAC.
  • Evaluation of clinical data for SMAC-mimetic antagonists.

Main Results:

  • IAPs are critical for cancer cell survival by inhibiting apoptosis.
  • SMAC-mimetics disrupt IAP function, restoring apoptotic sensitivity.
  • Four generations of SMAC-mimetics have been developed, with several in clinical trials.

Conclusions:

  • Targeting IAPs with SMAC-mimetics is a viable strategy to overcome cancer resistance to apoptosis.
  • Further research and clinical evaluation are ongoing for these promising cancer therapeutics.
  • Understanding IAP-SMAC interactions is key to designing effective apoptosis-inducing cancer treatments.

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