Kifunensine is an immunoactive compound originally produced by Kitasatosporia kifunense. Kifunensine displays competitive inhibition against immunosuppressive factor in tumor-bearing mice. Kifunensine has also been shown to be a potent inhibitor of the purified glycoprotein processing enzyme, mannosidase I (MAN1), specifically MAN1A1, MAN1A2, MAN1B1 and MAN1C1. Enzymes of this class are important factors for the biosynthesis of various types of N-linked oligosaccharide structures. Inhibition of these structures by kifunensine can interfere with cell-to-cell adhesion, targeting of lysosomal hydrolases to lysosomes, and clearance of asialoglycoproteins from the serum. Kifunensine inhibits human endoplasmic reticulum α-1,2-mannosidase I as well as members of the Golgi subfamily of the class I mannosidases (Golgi α-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM, respectively.
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