IAP proteins as targets for drug development in oncology

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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

Laurence Dubrez1, Jean Berthelet, Valérie Glorian

  • 1Institut National de la Santé et de la Recherche Médicale (Inserm), Dijon, France ; Université de Bourgogne, Dijon, France.

Oncotargets and Therapy
|October 5, 2013
PubMed

Insights

Inhibitors of apoptosis proteins (IAPs) are key regulators of cell processes implicated in cancer. Targeting IAPs shows promise for new anticancer therapies, with several drug candidates in clinical trials.

Area of Science:

  • Molecular Biology
  • Oncology
  • Biochemistry

Background:

  • Inhibitors of apoptosis proteins (IAPs) regulate critical cellular functions, including cell death, proliferation, and migration.
  • IAP overexpression is observed in various human tumors, correlating with tumor progression and poor treatment response.
  • IAPs can be rapidly induced by chemotherapy/radiotherapy via IRES-dependent translation, potentially causing therapeutic resistance.

Purpose of the Study:

  • To review the multifaceted role of IAPs in tumor development and progression.
  • To discuss the development of IAP-targeting molecules as a therapeutic strategy against cancer.
  • To highlight the current status of IAP antagonists in clinical trials.

Main Methods:

  • Literature review of studies on IAPs in cancer.
  • Analysis of IAP expression patterns in human tumor samples.
  • Examination of mechanisms underlying IAP-mediated chemoresistance.
  • Overview of preclinical and clinical development of IAP antagonists.

Main Results:

  • IAPs play a significant role in promoting tumor growth, survival, and metastasis.
  • IAP overexpression is a validated biomarker for poor prognosis in several cancers.
  • IAP antagonists have demonstrated potential in preclinical models and are advancing in clinical trials.

Conclusions:

  • IAPs represent a promising therapeutic target for novel anticancer strategies.
  • Targeting IAPs may overcome resistance mechanisms and improve treatment outcomes.
  • The ongoing clinical evaluation of IAP antagonists is crucial for their future application in oncology.
Keywords:
Smac mimeticsantitumor therapyapoptosis

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