| Residential College | false |
| Status | 已發表Published |
| Recent developments of human monocarboxylate transporter (hMCT) inhibitors as anticancer agents | |
Wu Pahau1; Zhou Yan1; Guo Yizhen1; Shaolin Zhang2; TAM KIN YIP1 
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| 2021-03 | |
| Source Publication | Drug Discovery Today
 |
| ISSN | 1359-6446 |
| Volume | 26Issue:3Pages:836-844 |
| Abstract | Cancer cells metabolize glucose via anaerobic glycolysis, with lactate formed in the cytosol as the end-product. To avoid intercellular acidification, excessive lactate and proton are excreted by monocarboxylate transporters (MCTs), which are often overexpressed in different malignant cancers. Targeting the MCT-mediated lactate/proton efflux makes MCTs a potentially interesting anticancer target. Although X-ray co-crystal structures of human MCTs with inhibitors are not yet available, homology models have been established, which helped to rationalize the binding modes and the design of new MCT inhibitors. In this review, we discuss the structures and functions of MCTs as well as recently reported small-molecule MCTs inhibitors. We assess the current development of MCT inhibitors and highlight possible directions for future development. |
| Keyword | Antineoplastic Agents Drug Design Drug Development Glucose/metabolism Glycolysis Humans Monocarboxylic Acid Transporters |
| DOI | 10.1016/j.drudis.2021.01.003 |
| URL | View the original |
| Indexed By | SCIE |
| Language | 英語English |
| Fulltext Access | |
| Citation statistics | |
| Document Type | Journal article |
| Collection | DEPARTMENT OF PHARMACEUTICAL SCIENCES |
| Corresponding Author | TAM KIN YIP |
| Affiliation | 1.Faculty of Health Sciences 2.Chongqing University |
| Recommended Citation GB/T 7714 | Wu Pahau,Zhou Yan,Guo Yizhen,et al. Recent developments of human monocarboxylate transporter (hMCT) inhibitors as anticancer agents[J]. Drug Discovery Today, 2021, 26(3), 836-844. |
| APA | Wu Pahau., Zhou Yan., Guo Yizhen., Shaolin Zhang., & TAM KIN YIP (2021). Recent developments of human monocarboxylate transporter (hMCT) inhibitors as anticancer agents. Drug Discovery Today, 26(3), 836-844. |
| MLA | Wu Pahau,et al."Recent developments of human monocarboxylate transporter (hMCT) inhibitors as anticancer agents".Drug Discovery Today 26.3(2021):836-844. |
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| File Name/Size | Publications | Version | Access | License | ||
| 1-s2.0-S135964462100（1506KB） | 期刊论文 | 作者接受稿 | 开放获取 | CC BY-NC-SA | View Download | |
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