Authors: Chasapis, Christos T.; Spyroulias, Georgios A.

Source: Current Pharmaceutical Design, Volume 15, Number 31, November 2009 , pp. 3716-3731(16)

Publisher: Bentham Science Publishers

Abstract:

The RING (Really Interesting New Gene) family is the largest type of E3 ubiquitin ligases. RING finger domains bind two zinc ions in a unique “cross-brace” arrangement through a defined motif of cysteine and histidine residues. This arrangement endows the RING domain with a globular conformation, characterized by a central α-helix and variable-length loops separated by several small β-strands. RING E3 ubiquitin ligases, play an essential role in the regulation of many biologic processes and defects in some of them are involved in cancer development. Furthermore, some RING E3 ligases are frequently overexpressed in human cancers. Today, RING ligases represent potentially molecular targets for disease intervention and could act as prognostic biomarkers. Targeting specific RING E3 ligases could lead to the development of a novel class of anticancer drugs. However RING fingers exhibit remarkable variations in their sequence and their topology characteristics. Structure determination of new RING finger domain is in the core of the design of new pharmaceuticals and what is presented in this article is a thorough review of achievements on the NMR or Xray structure determinations. Protein preparation protocols along with analysis of the structural features of known RING finger are also presented.

Keywords: Ubiquitin; E3 ubiquitin ligase; RING finger; zinc-coordination; anticancer drugs

Document Type: Research article

DOI: http://dx.doi.org/10.2174/138161209789271825

Affiliations: 1: Department of Pharmacy, University of Patras, Panepistimioupoli - Rion, GR-26504, Patras, Greece.

Publication date: 2009-11-01

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  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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