Using specificity to strategically target proteases.

Bioorganic & Medicinal Chemistry
Mark D Lim, Charles S Craik

Abstract

Proteases are a family of naturally occurring enzymes in the body whose dysregulation has been implicated in numerous diseases and cancers. Their ability to selectively and catalytically turnover substrate adds both signal amplification and functionality as parameters for the detection of disease. This review will focus on the development of activity-based methodologies to characterize proteases, and in particular, the use of positional scanning, synthetic combinatorial libraries (PS-SCL's), and substrate activity screening (SAS) assays. The use of these approaches to better understand a protease's natural substrate will be discussed as well as the technologies that emerged.

References

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Citations

Feb 20, 2014·Proceedings of the National Academy of Sciences of the United States of America·Paulina KasperkiewiczMarcin Drag
Jan 17, 2012·Proteomics·Bart H J van den Berg, Andreas Tholey
Feb 1, 2011·Chemistry & Biology·Christopher M BrownCharles S Craik
Jan 29, 2013·Chemistry & Biology·Bainan WuMaurizio Pellecchia
Sep 20, 2012·Memórias do Instituto Oswaldo Cruz·Karina Mastropasqua RebelloHenrique Leonel Lenzi
Dec 25, 2010·Integrative Biology : Quantitative Biosciences From Nano to Macro·Miles A MillerDouglas A Lauffenburger
Nov 21, 2009·Journal of the American Chemical Society·Navin VaradarajanBrent L Iverson

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