The evolving world of protein-G-quadruplex recognition: A medicinal chemist's perspective

  • Sissi C
  • Gatto B
  • Palumbo M
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Abstract

The physiological and pharmacological role of nucleic acids structures folded into the non canonical G-quadruplex conformation have recently emerged. Their activities are targeted at vital cellular processes including telomere maintenance, regulation of transcription and processing of the pre-messenger or telomeric RNA. In addition, severe conditions like cancer, fragile X syndrome, Bloom syndrome, Werner syndrome and Fanconi anemia J are related to genomic defects that involve G-quadruplex forming sequences. In this connection G-quadruplex recognition and processing by nucleic acid directed proteins and enzymes represents a key event to activate or deactivate physiological or pathological pathways. In this review we examine protein-G-quadruplex recognition in physiologically significant conditions and discuss how to possibly exploit the interactions' selectivity for targeted therapeutic intervention. © 2011 Elsevier Masson SAS. All rights reserved.

Author-supplied keywords

  • Drug binding
  • G-quadruplex
  • Nucleic acids
  • Proteins

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