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https://hdl.handle.net/10356/82167
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DC Field | Value | Language |
---|---|---|
dc.contributor.author | Liu, Li-Juan | en |
dc.contributor.author | Leung, Ka-Ho | en |
dc.contributor.author | Lin, Sheng | en |
dc.contributor.author | Chan, Daniel Shiu-Hin | en |
dc.contributor.author | Susanti, Dewi | en |
dc.contributor.author | Rao, Weidong | en |
dc.contributor.author | Chan, Philip Wai Hong | en |
dc.contributor.author | Ma, Dik-Lung | en |
dc.contributor.author | Leung, Chung-Hang | en |
dc.date.accessioned | 2016-08-17T06:45:11Z | en |
dc.date.accessioned | 2019-12-06T14:47:54Z | - |
dc.date.available | 2016-08-17T06:45:11Z | en |
dc.date.available | 2019-12-06T14:47:54Z | - |
dc.date.issued | 2014 | en |
dc.identifier.citation | Liu, L.-J., Leung, K.-H., Lin, S., Chan, D. S.-H., Susanti, D., Rao, W., et al. (2014). Pharmacophore modeling for the identification of small-molecule inhibitors of TACE. Methods, 71, 92-97. | en |
dc.identifier.issn | 1046-2023 | en |
dc.identifier.uri | https://hdl.handle.net/10356/82167 | - |
dc.description.abstract | Tumor necrosis factor α-converting enzyme (TACE) plays a critical role in diverse physiological processes such as inflammation, hematopoiesis, and development. In this study, a pharmacophore model constructed from a training set of TACE inhibitors was used to screen an in-house database of organic compounds, from which compound 1 emerged as a top candidate. In a cell-free assay, compound 1 inhibited TACE enzymatic activity in a dose-dependent manner. Moreover, compound 1 inhibited the production of soluble TNF-α in human acute monocytic leukemia THP-1 cells without impacting nitric oxide production, and exhibited anti-proliferative activity against THP-1 cells. We envisage that compound 1 may be employed as a useful scaffold for the development of more potent TACE inhibitors. This study also validates the use of pharmacophore modeling to identify enzyme inhibitors. | en |
dc.description.sponsorship | ASTAR (Agency for Sci., Tech. and Research, S’pore) | en |
dc.language.iso | en | en |
dc.relation.ispartofseries | Methods | en |
dc.rights | © 2014 Elsevier Inc. | en |
dc.subject | Pharmacophore | en |
dc.subject | TACE | en |
dc.title | Pharmacophore modeling for the identification of small-molecule inhibitors of TACE | en |
dc.type | Journal Article | en |
dc.contributor.school | School of Physical and Mathematical Sciences | en |
dc.identifier.doi | 10.1016/j.ymeth.2014.09.005 | en |
item.fulltext | No Fulltext | - |
item.grantfulltext | none | - |
Appears in Collections: | SPMS Journal Articles |
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