What is it about?
The largest class of glycosidase inhibitor is iminosugars that can act as bases to deprotonate catalytic acid residues in the enzyme active site. However, many non-basic compounds can inhibit this family of enzymes and these are covered in our review. We cover inhibitors that either have no basic functional groups (like the basic nitrogen of iminosugars) that ionize readily at physiologic pH or compounds that are charge-neutral zwitterions.
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Why is it important?
Iminosugars include both natural alkaloids and designer synthetic molecules but can have undesirable side effects. Thus, researchers have identified a variety of different types of molecules that can inhibit glycosidases and have anticancer, antidiabetic and antiviral properties. Inhibitors such as epoxides and sulfonium ions were actually developed synthetically before they were discovered as components of natural products that display potent glycosidase inhibitory activities.
Perspectives
This is a follow-up review to one I published in the same journal in 2003 also titled "Back to (non-)Basics". This play on words highlights the fact the first glycosidase inhibitors discovered in the 1940's were neutral, non-basic, sugar lactones. In the latter half of the 20th century, research on glycosidase inhibitors shifted heavily toward basic iminosugars. However, this century much attention has been paid to neutral compounds like cyclophellitol and charge-balanced zwitterions like salacinol, both natural products.
Todd Houston
Griffith University
Read the Original
This page is a summary of: Back to (non-)Basics: An Update on Neutral and Charge-Balanced Glycosidase Inhibitors, Mini-Reviews in Medicinal Chemistry, April 2018, Bentham Science Publishers,
DOI: 10.2174/1389557517666171002161325.
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