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McGeary, Ross P., Vella, Peter, Mak, Jeffrey Y. W., Guddat, Luke W. and Schenk, Gerhard (2009) Inhibition of purple acid phosphatase with a-alkoxynaphthylmethylphosphonic acids. Bioorganic and Medicinal Chemistry Letters , 19. pp. 163-166. ISSN 0960-894X
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Abstract
Purple acid phosphatases (PAPs) are binuclear hydrolases that catalyse the hydrolysis of a range of phosphorylated
substrates. Human PAP is a major histochemical marker for the diagnosis of osteoporosis. In
patients suffering from this disorder, PAP activity contributes to increased bone resorption and, therefore,
human PAP is a key target for the development of anti-osteoporotic drugs. This manuscript describes the
design and synthesis of derivatives of 1-naphthylmethylphosphonic acids as inhibitors of PAP. The Ki values
of these compounds are as low as 4 lM, the lowest reported to date for a PAP inhibitor.
| Item Type: | Article |
|---|---|
| Keywords: | Purple acid phosphatase; PAP; Phosphonate; |
| Academic Unit: | Faculty of Science and Engineering > Chemistry |
| Item ID: | 3719 |
| Depositing User: | Gary Schenk |
| Date Deposited: | 31 May 2012 14:30 |
| Journal or Publication Title: | Bioorganic and Medicinal Chemistry Letters |
| Publisher: | Elsevier |
| Refereed: | Yes |
| Related URLs: | |
| URI: | https://mu.eprints-hosting.org/id/eprint/3719 |
| Use Licence: | This item is available under a Creative Commons Attribution Non Commercial Share Alike Licence (CC BY-NC-SA). Details of this licence are available here |
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