Please use this identifier to cite or link to this item:
http://hdl.handle.net/10397/65844
DC Field | Value | Language |
---|---|---|
dc.contributor | Department of Applied Biology and Chemical Technology | en_US |
dc.creator | Qiu, ZC | en_US |
dc.creator | Dong, XL | en_US |
dc.creator | Dai, Y | en_US |
dc.creator | Xiao, GK | en_US |
dc.creator | Wang, XL | en_US |
dc.creator | Wong, KC | en_US |
dc.creator | Wong, MS | en_US |
dc.creator | Yao, X | en_US |
dc.date.accessioned | 2017-05-22T02:09:20Z | - |
dc.date.available | 2017-05-22T02:09:20Z | - |
dc.identifier.issn | 1661-6596 | en_US |
dc.identifier.uri | http://hdl.handle.net/10397/65844 | - |
dc.language.iso | en | en_US |
dc.publisher | Molecular Diversity Preservation International (MDPI) | en_US |
dc.rights | © 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/). | en_US |
dc.rights | The following publication Qiu, Z.-C.; Dong, X.-L.; Dai, Y.; Xiao, G.-K.; Wang, X.-L.; Wong, K.-C.; Wong, M.-S.; Yao, X.-S. Discovery of a New Class of Cathepsin K Inhibitors in Rhizoma Drynariae as Potential Candidates for the Treatment of Osteoporosis. Int. J. Mol. Sci. 2016, 17, 2116 is available at https://dx.doi.org/10.3390/ijms17122116 | en_US |
dc.subject | Bone resorption | en_US |
dc.subject | Cathepsin K | en_US |
dc.subject | In silico target fishing | en_US |
dc.subject | Kushennol F | en_US |
dc.subject | Osteoclasts | en_US |
dc.subject | Osteoporosis | en_US |
dc.subject | RAW264.7 cells | en_US |
dc.subject | Rhizoma Drynariae | en_US |
dc.subject | Sophoraflavanone G | en_US |
dc.title | Discovery of a new class of Cathepsin K inhibitors in Rhizoma Drynariae as potential candidates for the treatment of osteoporosis | en_US |
dc.type | Journal/Magazine Article | en_US |
dc.identifier.spage | 1 | en_US |
dc.identifier.epage | 18 | en_US |
dc.identifier.volume | 17 | en_US |
dc.identifier.issue | 12 | en_US |
dc.identifier.doi | 10.3390/ijms17122116 | en_US |
dcterms.abstract | Rhizoma Drynariae (RD), as one of the most common clinically used folk medicines, has been reported to exert potent anti-osteoporotic activity. The bioactive ingredients and mechanisms that account for its bone protective effects are under active investigation. Here we adopt a novel in silico target fishing method to reveal the target profile of RD. Cathepsin K (Ctsk) is one of the cysteine proteases that is over-expressed in osteoclasts and accounts for the increase in bone resorption in metabolic bone disorders such as postmenopausal osteoporosis. It has been the focus of target based drug discovery in recent years. We have identified two components in RD, Kushennol F and Sophoraflavanone G, that can potentially interact with Ctsk. Biological studies were performed to verify the effects of these compounds on Ctsk and its related bone resorption process, which include the use of in vitro fluorescence-based Ctsk enzyme assay, bone resorption pit formation assay, as well as Receptor Activator of Nuclear factor κB (NF-κB) ligand (RANKL)-induced osteoclastogenesis using murine RAW264.7 cells. Finally, the binding mode and stability of these two compounds that interact with Ctsk were determined by molecular docking and dynamics methods. The results showed that the in silico target fishing method could successfully identify two components from RD that show inhibitory effects on the bone resorption process related to protease Ctsk. | en_US |
dcterms.accessRights | open access | en_US |
dcterms.bibliographicCitation | International journal of molecular sciences, Dec. 2016, v. 17, no. 12, 2116 | en_US |
dcterms.isPartOf | International journal of molecular sciences | en_US |
dcterms.issued | 2016-12 | - |
dc.identifier.isi | WOS:000392280500160 | - |
dc.identifier.scopus | 2-s2.0-85007061947 | - |
dc.identifier.ros | 2016002245 | - |
dc.identifier.eissn | 1422-0067 | en_US |
dc.identifier.artn | 2116 | en_US |
dc.identifier.rosgroupid | 2016002198 | - |
dc.description.ros | 2016-2017 > Academic research: refereed > Publication in refereed journal | en_US |
dc.description.validate | 201804_a bcma | en_US |
dc.description.oa | Version of Record | en_US |
dc.identifier.FolderNumber | OA_IR/PIRA, a1375 | - |
dc.identifier.SubFormID | 44730 | - |
dc.description.fundingSource | Others | en_US |
dc.description.fundingText | National Natural Science Foundation of China (81220108028);Shenzhen Basic Research Program (JCYJ20140819153305697, JCYJ20140819153305696);National Major Scientific and Program of Introducing Talents of Discipline to Universities (B13038) | en_US |
dc.description.pubStatus | Published | en_US |
dc.description.oaCategory | CC | en_US |
Appears in Collections: | Journal/Magazine Article |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
Qiu_New_Cathepsin_K.pdf | 6.3 MB | Adobe PDF | View/Open |
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