Identifying Potent, Selective Protein Tyrosine Phosphatase Inhibitors from a Library of Au(I) Complexes

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Publication Details

Author list: Karver MR, Krishnamurthy D, Kulkarni RA, Bottini N, Barrios AM
Publisher: American Chemical Society
Publication year: 2009
Volume number: 52
Issue number: 21
Start page: 6912
End page: 6918
Number of pages: 7
ISSN: 0022-2623
Languages: English-Great Britain (EN-GB)


Therapeutic inhibition of protein tyrosine phosphatase activity is a compelling yet challenging approach to the treatment of human disease. Toward this end, a library of 40 gold complexes with the general formula R(3)P-Au-Cl was screened to identify novel inhibitors of PTP activity. The most promising inhibitor obtained for the lymphoid tyrosine phosphatase LYP, (2-pyridine)(Ph(2))P-Au-Cl, is one of the most potent and selective LYP inhibitors identified to date with an IC(50) of 1.5 +/- 0.3 mu M, 10-fold selectivity for LYP over PTP-PEST, HePTP, and CD45 in vitro, and activity in cellular studies as well.


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Last updated on 2019-23-08 at 11:15