Publications [#330232] of Michael J. Therien

Papers Published

  1. Lau, CK; Bayly, CI; Gauthier, JY; Li, CS; Therien, M; Asante-Appiah, E; Cromlish, W; Boie, Y; Forghani, F; Desmarais, S; Wang, Q; Skorey, K; Waddleton, D; Payette, P; Ramachandran, C; Kennedy, BP; Scapin, G, "Structure based design of a series of potent and selective non peptidic PTP-1B inhibitors.", Bioorganic & medicinal chemistry lettersFebruary,, 2004, 14(4), 1043-1048 [doi].
    (last updated on 2026/01/18)

    Abstract:
    A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase.