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Small molecule approaches to regulation of gene transcription

Croatian Society of Natural Sciences
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  • Biology
  • Ecology
  • Geography
  • Medicine


pesut-sopta.vp Small molecule approaches to regulation of gene transcription Regulation of gene expression is fundamental to the processes of cel-lular differentiation and organismal development. The human ge- nome project has identified approximately 30,000 protein coding genes in the genome and the regulation of expression of these genes in time and space leads to the complex structure of the human form. How are these genes expressed at the appropriate time and in the appropriate place is a fundamentally important area of study which has yet to be fully defined. Regulation of gene transcription is a primary means of regulating gene expression. Transcription factors, both activators and repressors, are the molecular arbiters regulating gene expression in or- ganisms as diverse as bacteria, yeast and mammals. Aberrant gene tran- scription plays a role in the onset of many diseases including cancer, neurodegenerative disease and others. In eukaryotes at least, transcrip- tional regulation involves a complex assembly of activators, repressors, coactivators/corepressors, general transcription factors and RNA poly- merases to elicit proper expression of protein coding, tRNA and rRNA genes. In this review we focus on the regulation of protein coding genes by RNA polymerase II and small molecule approaches to regulating this complex process. Transcriptional activators are a diverse set of molecules that activate gene expression in response to environmental and developmental cues. Activators generally bind to sequence elements upstream of protein coding genes and thus confer specificity of gene expression. Transcrip- tional activators are modular in nature containing discrete DNA bind- ing domains and discrete activation domains (1). A wide variety of DNA binding domains have been defined both functionally and struc- turally and include domains such as the Zn-finger domain, the he- lix-turn-helix domain among others (2). Activation domains are less rigidly defined on the basis of structure a

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