Receptor Selective Synthetic Retinoids as Potential Cancer Chemotherapy Agents

Author: Crowe D.L.

Source: Current Cancer Drug Targets, Volume 2, Number 1, March 2002 , pp. 77-86(10)

Publisher: Bentham Science Publishers

Abstract:

For many years, the vitamin A metabolite retinoic acid (RA) has been known to have profound effects on development, cellular proliferation and differentiation, and tumor growth and invasion. The wide-ranging effects of RA on cellular proliferation and migration have made it a useful chemotherapeutic agent in the treatment of many types of cancer. In the last fifteen years, with the discovery of nuclear receptors for RA, the molecular basis for the effects of this molecule has become apparent. Retinoic acid receptors (RAR) are members of a superfamily of ligand dependent transcription factors that interact with an increasingly large array of coactivators and repressors to regulate target gene expression through binding to cognate recognition sequences in the promoters of these genes. Alterations in RAR expression and function have been demonstrated in many types of cancer. The translocation of RAR with PML or PLZF genes in acute promyelocytic leukemia is a paradigm of the role of RARs in cancer biology. In addition, the development of receptor selective synthetic retinoids has greatly expanded our knowledge of RAR function in tumor cells and provided additional treatment options for cancer patients. This review will examine the development of receptor selective retinoids, their uses to date, and future potential.

Keywords: Synthetic Retinoids; Cancer Chemotherapy Agents; A metabolite retinoic acid (RA)

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1568009023333935

Publication date: 2002-03-01

• Current Cancer Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular drug targets involved in cancer, e.g. disease specific proteins, receptors, enzymes, genes.
  Each issue of the journal contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics on drug targets involved in cancer.
  As the discovery, identification, characterization and validation of novel human drug targets for anti-cancer drug discovery continues to grow; this journal has become essential reading for all pharmaceutical scientists involved in drug discovery and development.

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