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The development of small-molecule inhibitors targeting hexokinase 2
Shan, Wenying; Zhou, Yan; Tam, Kin Yip
2022
Source PublicationDrug Discovery Today
ISSN1359-6446
Volume27Issue:9Pages:2574-2585
Abstract

As one of the well-known hallmarks of cancer malignancy, most proliferating cancer cells exhibit enhanced rates of glycolysis. Hexokinase 2 (HK2) is the rate-limiting enzyme catalyzing the first step of glycolysis, and is often overexpressed in most cancer cells. Thus, targeting HK2 appears to be a promising anticancer therapy. However, selective inhibition of HK2 and the polar nature of the target site remain challenges to the development of small-molecule inhibitors, which could be addressed by targeting unique domains of HK2, such as its N-terminal domain. Here, we review different target–inhibitor binding modes and the associated pharmacological effects, which would be informative for rational molecular design. We also highlight further perspectives and strategies to develop novel HK2 inhibitors for cancer therapy.

KeywordCancer Metabolism Drug–target Binding Hexokinase 2 Selective Inhibition Structure-based Molecular Design
DOI10.1016/j.drudis.2022.05.017
URLView the original
Language英語English
Scopus ID2-s2.0-85131266181
Fulltext Access
FWCI0.9214138
Citation statistics
Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
AffiliationCancer Centre, Faculty of Health Sciences, University of Macau, Macao
First Author AffilicationCancer Centre
Recommended Citation
GB/T 7714
Shan, Wenying,Zhou, Yan,Tam, Kin Yip. The development of small-molecule inhibitors targeting hexokinase 2[J]. Drug Discovery Today,2022,27(9):2574-2585.
APA Shan, Wenying,Zhou, Yan,&Tam, Kin Yip.(2022).The development of small-molecule inhibitors targeting hexokinase 2.Drug Discovery Today,27(9),2574-2585.
MLA Shan, Wenying,et al."The development of small-molecule inhibitors targeting hexokinase 2".Drug Discovery Today 27.9(2022):2574-2585.
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