Recent discovery and development of protein tyrosine phosphatase inhibitors

Blaskovich, Mark A. and Kim, Hwa-Ok (2002) Recent discovery and development of protein tyrosine phosphatase inhibitors. Expert Opinion on Therapeutic Patents, 12 6: 871-905. doi:10.1517/13543776.12.6.871


Author Blaskovich, Mark A.
Kim, Hwa-Ok
Title Recent discovery and development of protein tyrosine phosphatase inhibitors
Journal name Expert Opinion on Therapeutic Patents   Check publisher's open access policy
ISSN 1354-3776
1744-7674
Publication date 2002-06
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1517/13543776.12.6.871
Volume 12
Issue 6
Start page 871
End page 905
Total pages 35
Place of publication London, U. K.
Publisher Informa Healthcare
Language eng
Subject 030401 Biologically Active Molecules
1115 Pharmacology and Pharmaceutical Sciences
Formatted abstract
The protein tyrosine phosphatases (PTPases or PTPs) play an important role in controlling the status of tyrosine phosphorylation and the regulation of cellular function. The ability to selectively inhibit PTPs holds enormous therapeutic potential for the treatment of diseases such as diabetes, cancer and osteoporosis. However, an understanding of the role of many PTPs has yet to be unravelled, with only PTP1B convincingly validated as a therapeutic target. Furthermore, the intricate network of different PTPs extensively involved in signalling events requires high selectivity for the desired PTP target, in order to minimise potential side effects. Most research programmes into PTP inhibitors are still at an early stage and have yet to convert initial leads into compounds with more drug-like properties. Inhibitors have been identified by modification of peptide substrates, from natural product screening and by rational design. This article will give an overview of PTPs, followed by a more detailed description of the development of PTP inhibitors. Patents on PTP inhibitors published between January 1998 and Feb 2002 will be discussed in the context of the available literature.
2002 © Ashley Publications Ltd
Keyword Cancer
CD45
Hyperglycaemia
Insulin resistance
LAR
Obesity
Protein tyrosine phosphatase
Protein tyrosine phosphatase inhibitor
PTP1B
TCPTP
Type II diabetes
VHR
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collection: Institute for Molecular Bioscience - Publications
 
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Created: Thu, 05 Feb 2009, 12:17:39 EST by Gina Velli on behalf of Institute for Molecular Bioscience