Imaging of Sialidase Activity and Its Clinical Application.

Sialidase releases sialic acid residues from the ends of sugar chains. The sialidases are involved in many physiological processes including cell differentiation and proliferation and immune function as well as pathophysiological conditions such as various human cancers and infections. Therefore visualization of sialidase activities with high sensitivity could provide valuable insights into these isozyme's activity. We developed novel fluorescent sialidase substrates, 2-benzothiazol-2-yl-phenol derivatives-based N-acetylneuraminic acid (Neu5Ac) (BTP-Neu5Ac) substrates, for highly sensitive and specific visualization of sialidase activity in living mammalian tissues and virus-infected cells. We found that BTP-Neu5Ac can visualize sialidase activities sensitively and selectively in rat tissues including brain slices. BTP-Neu5Ac can also clearly detect cancer cells implanted orthotopically in mouse colons and human colon cancers. In this review, I describe imaging of sialidase activity with BTP-Neu5Ac in animal tissues, detection of colon cancer, memory formation, detection of virus-infected cells, and application to drug-resistant influenza virus detection and separation.