A novel series of non-nucleoside inhibitors of inosine 5′-monophosphate dehydrogenase with immunosuppressive activity§ § Abbreviations: β, coefficient of interaction; DTH, delayed-type hypersensitivity; FBS, foetal bovine serum; IMP, inosine 5′-monophosphate; IMPDH, IMP dehydrogenase; K ′ i , apparent inhibition constant for compound I; K ii , inhibition constant for effect on intercept of Lineweaver–Burk plots; K ′ x , apparent inhibition constant for compound X; MFT, mycophenolate mofetil; MTT, 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide; MPA, mycophenolic acid; TCA, trichloroacteic acid (10% w/v); v, velocity; v 0, uninhibited velocity; and XMP, xanthosine monophosphate.
Titel:
A novel series of non-nucleoside inhibitors of inosine 5′-monophosphate dehydrogenase with immunosuppressive activity§ § Abbreviations: β, coefficient of interaction; DTH, delayed-type hypersensitivity; FBS, foetal bovine serum; IMP, inosine 5′-monophosphate; IMPDH, IMP dehydrogenase; K ′ i , apparent inhibition constant for compound I; K ii , inhibition constant for effect on intercept of Lineweaver–Burk plots; K ′ x , apparent inhibition constant for compound X; MFT, mycophenolate mofetil; MTT, 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide; MPA, mycophenolic acid; TCA, trichloroacteic acid (10% w/v); v, velocity; v 0, uninhibited velocity; and XMP, xanthosine monophosphate.
Auteur:
Franklin, Trevor J Morris, William P Jacobs, Vivien N Culbert, Eric J Heys, Christine A Ward, Walter H.J Cook, Peter N Jung, Frédéric Plé, Patrick