Covalent Inhibition of the Lymphoid Tyrosine Phosphatase

Journal article


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Publication Details

Author list: Ahmed VF, Bottini N, Barrios AM
Publisher: Wiley: 12 months
Publication year: 2014
Volume number: 9
Issue number: 2
Start page: 296
End page: 299
Number of pages: 4
ISSN: 1860-7179
Languages: English-Great Britain (EN-GB)


Covalent inhibitors of lymphoid tyrosine phosphatase (LYP) were identified from a screen of the NIH Molecular Libraries Small Molecules Repository (MLSMR). Both of the two lead compounds identified have phosphotyrosine-mimetic benzoic acid moieties as well as electrophilic acrylonitrile groups. Inhibition kinetics of both compounds are consistent with covalent modification of the enzyme, with nanomolar KI and reciprocal millisecond k(inact) values, representing the best efficiency ratios (k(inact)/K-I) among currently reported covalent LYP inhibitors. Covalent inhibitors can provide longer efficacy and better selectivity than more conventional noncovalent inhibitors, and these lead compounds are an important step toward the development of protein tyrosine phosphatase (PTP)-targeted covalent therapeutic compounds.


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