Current Topics in Medicinal Chemistry

Author(s): Hector Viadiu

DOI: 10.2174/156802608786141160

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Molecular Architecture of Tumor Suppressor p53

Page: [1327 - 1334] Pages: 8

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Abstract

p53 is a transcription factor central to cellular DNA metabolism that controls cellular responses to DNA damage. p53 activity, finely regulated, integrates the information from several pathways to preserve the cells genetic information. Great attention has been given to the structural determination of p53 domains and its cancerous mutants because 50% of cancer cases present mutations in p53 that hinder its activity resulting in uncontrolled cell reproduction. We enumerate the multiple studies carried to elucidate the structure of p53 domains and we highlight their main findings. The ultimate goal of the reviewed structural efforts is to understand p53 function at atomic level with the aim to overcome cancer by reversing p53 mutant activity to its normal function.

Keywords: p53, transcription factor, transactivation domain, DNA-binding domain, tetramerization domain, regulatory domain, X-ray crystallography, NMR