Test for inhibitors of heparanase, useful for treatment of e.g. cancer and inflammatory disease, using immobilized, labeled heparanase substrate

摘要

Testing agents (I) for inhibition of the catalytic activity of heparanase (II) comprising: (a) allowing a binding partner (III) for a heparanase substrate (IV), immobilized on a solid support, to interact with labeled (IV), to form an immobilized, labeled substrate (X); (b) treating (X) with (II) in presence of test compound; and (c) testing for presence/absence of the label in the separated solution, is new. Independent claims are also included for the following: (1) similar method in which (IV) is bound, by bridging, to molecules immobilized on the support; (2) testing potential of agents to inhibit binding between FGF (fibroblast growth factor) and (IV), by incubating immobilized FGF with test compound and labeled (IV), then detecting absence or presence of the label in the seprated solution; (3) kits for performing the new processes; and (4) inhibitors of the catalytic activity of (II) identified by the new methods.