Glycosyltransferase inhibitors: A promising strategy to pave a path from laboratory to therapy

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13 Citations (Scopus)


Abnormal glycosylation is a common feature in disease that typically results from misregulation in expression and/or activity of glycosyltransferases (GTs) and glycosidases. Interfering with these enzymes, by developing a prospect of targeted inhibitors, has opened newer avenues to meet the challenge of abnormal glycosylation. Progress in GT inhibitors has been relatively slower in comparison to glycosidases. In case of GTs, their polyspecific nature, structural homology, overlapping specificities, multi-substrate catalytic mechanism and relatively less available 3D-structural data stance a big challenge to explore the whole potential of GT target inhibitors in comparison to glycosidases for therapeutic purposes. In this review, we focus on GT specific inhibitors, which are organised as conventional donor analogues (viz. donor, acceptor and transition state mimetic), glycomimetic, alternative inhibitor chemotype and metabolic chain terminator. Conventional donor analogues are however limited by the poor membrane permeability and chemical instability. Thus, in the last two decades, alternative inhibitor chemotypes caught attention as a promising lead, which are not structurally derived from GT substrates and possess drug like properties offering an alternate non-substrate like inhibitor based strategy for drug development. Although successful cellular GT-targeted molecules are yet to be achieved, recent designing of metabolic inhibitors i.e., dead end substrates are emerging as an impetus to explore the potential of GT families as therapeutic targets.

Original languageEnglish
Title of host publicationCarbohydrate Chemistry: Chemical and Biological Approaches
EditorsThisbe K. Lindhorst, Yves Queneau, Amelia Pilar Rauter
PublisherRSC - Royal Society of Chemistry
Number of pages24
ISBN (Electronic)978-1-78801-064-1 (PDF), 978-1-78801-409-0 (ePub)
ISBN (Print)978-1-78801-003-0
Publication statusPublished - 2018

Publication series

NameCarbohydrate Chemistry
PublisherRoyal Society of Chemistry
ISSN (Print)2041-353X
ISSN (Electronic)1465-1963


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