Advances in the development of SUMO specific protease (SENP) inhibitors

作者: Ashutosh Kumar , Kam Y.J. Zhang

DOI: 10.1016/J.CSBJ.2015.03.001

关键词:

摘要: Sumoylation is a reversible post-translational modification that involves the covalent attachment of small ubiquitin-like modifier (SUMO) proteins to their substrate proteins. Prior conjugation, SUMO need be proteolytically processed from its precursor form mature or active form. specific proteases (SENPs) are cysteine cleave pro inactive at C-terminus using hydrolase activity expose two glycine residues. SENPs also catalyze de-conjugation isopeptidase activity, which crucial for recycling important maintaining balance between sumoylated and unsumoylated required normal cellular physiology. Several studies reported overexpression in disease conditions highlighted role development various diseases, especially cancer. In this review, we will address current biological understanding SENP isoforms pathogenesis different cancers other diseases. We then discuss advances protein-based, peptidyl molecule inhibitors isoforms. Finally, summarize successful examples computational screening allowed identification with therapeutic potential.

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