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AssigneesUniversity of South Florida, H. Lee Moffitt Cancer Center and Research, H. Lee Moffitt Cancer Center and Research Institute, Inc.
InventorsJie Wu, Nicholas J. Lawrence, Said M. Sebti, Harshani R. Lawrence
Estimating the term…
Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erk1/2 activation pathway. Additionally, a number of analogs of NSC-117199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and are found to be potent and/or selective inhibitors of Shp1 and/or Shp2 protein tyrosine phosphatases.
A method of inhibiting a protein tyrosine phosphatase in a cell comprising the step of contacting the cell with an effective amount of a compound having the formula (I):
A method of inhibiting a protein tyrosine phosphatase in a cell comprising the step of contacting the cell with an effective amount of a compound having the formula (II):
A method of inhibiting a protein tyrosine phosphatase comprising the step of contacting the cell with an effective amount of a compound having the formula (III):
A method of treating a disease in a subject characterized by elevated protein tyrosine phosphatase activity comprising the step of administering to the subject in need thereof an effective amount of a compound having the formula (IV):
A method of inhibiting a protein tyrosine phosphatase comprising the step of contacting the cell with an effective amount of a compound having the formula (V):
A method of treating a disease in a subject characterized by elevated Shp2 protein tyrosine phosphatase comprising the step of administering to the patient an NSC-87877 (8-hydroxy-7-(6-sulfonaphthalen-2-yl)diazenyl-quinoline-5-sulfonic acid).
A method of inhibiting a protein tyrosine phosphatase comprising the step of contacting the cell with an effective amount of a compound having the formula (VI):
Dependencies are inferred from the claim text.