Sialyltransferase inhibition and recent advances

L Wang, Y Liu, L Wu, XL Sun - … et Biophysica Acta (BBA)-Proteins and …, 2016 - Elsevier
Sialic acids, existing as terminal sugars of glycoconjugates, play important roles in various
physiological and pathological processes, such as cell–cell adhesion, immune defense …

Advancement of sialyltransferase inhibitors: therapeutic challenges and opportunities

R Szabo, D Skropeta - Medicinal Research Reviews, 2017 - Wiley Online Library
Hypersialylation of tumor cell surface proteins along with a marked upregulation of
sialyltransferase (ST) activity is a well‐established hallmark of cancer. Due to the critical role …

An efficient approach to the discovery of potent inhibitors against glycosyltransferases

K Hosoguchi, T Maeda, J Furukawa… - Journal of medicinal …, 2010 - ACS Publications
We describe a standardized approach for searching potent and selective inhibitors of
glycosyltransferases by high throughput quantitative MALDI-TOFMS-based screening of …

Highly substituted cyclopentane–CMP conjugates as potent sialyltransferase inhibitors

W Li, Y Niu, DC Xiong, X Cao… - Journal of Medicinal …, 2015 - ACS Publications
Sialylconjugates on cell surfaces are involved in many biological events such as cellular
recognition, signal transduction, and immune response. It has been reported that aberrant …

Bisubstrate analogues as glycosyltransferase inhibitors

M Izumi, H Yuasa, H Hashimoto - Current topics in medicinal …, 2009 - ingentaconnect.com
Oligosaccharides in glycoconjugates such as glycoproteins and glycolipids play important
roles in a variety of biological functions. Since glycosyltransferases are responsible for the …

Transition state-based ST6Gal I inhibitors: Mimicking the phosphodiester linkage with a triazole or carbamate through an enthalpy-entropy compensation

AP Montgomery, D Skropeta, H Yu - Scientific Reports, 2017 - nature.com
Abstract Human β-galactoside α-2, 6-sialyltransferase I (ST6Gal I) catalyses the synthesis of
sialylated glycoconjugates. Overexpression of ST6Gal I is observed in many cancers, where …

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

PA Videira, F Marcelo, RK Grewal - 2017 - books.rsc.org
Abnormal glycosylation is a common feature in disease that typically results from
misregulation in expression and/or activity of glycosyltransferases (GTs) and glycosidases …

Computational characterisation of the interactions between human ST6Gal I and transition‐state analogue inhibitors: insights for inhibitor design

A Montgomery, R Szabo, D Skropeta… - Journal of Molecular …, 2016 - Wiley Online Library
Human β‐galactoside α‐2, 6‐sialyltransferase I (hST6Gal I) catalyses the synthesis of
sialylated glycoconjugates involved in cell–cell interactions. Overexpression of hST6Gal I is …

Synthesis of glycosyltransferase inhibitors

T Kajimoto, M Node - Synthesis, 2009 - thieme-connect.com
Glycosyltransferases and glycosidases work together to construct the oligosaccharide
moieties of biologically active glycoconjugates. Although many excellent glycosidase …

Synthesis of bisubstrate and donor analogues of sialyltransferase and their inhibitory activities

M Izumi, K Wada, H Yuasa… - The Journal of organic …, 2005 - ACS Publications
Sialyltransferases (STs) are involved in the biosynthesis of glycoconjugates with important
biological activities. Most STs utilize cytidine-5 '-monophospho-N-acetylneuraminic acid …