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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-9
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pubmed:abstractText |
Prostate-specific membrane antigen (PSMA) is a membrane-bound cell surface peptidase which is over-expressed in prostate cancer cells. The enzymatic activities of PSMA are understood but the role of the enzyme in prostate cancer remains conjectural. We previously confirmed the existence of a hydrophobic binding site remote from the enzyme's catalytic center. To explore the specificity and accommodation of this binding site, we prepared a series of six glutamate-containing phosphoramidate derivatives of various hydroxysteroids (1a-1f). The inhibitory potencies of the individual compounds of the series were comparable to a simple phenylalkyl analog (8), and in all cases IC50 values were sub-micromolar. Molecular docking was used to develop a binding model for these inhibitors and to understand their relative inhibitory potencies against PSMA.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-10221263,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-10537328,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-10987952,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-11210180,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-11306418,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-11642607,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-11991853,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-12210476,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-12384542,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-12482445,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-15336276,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-16154750,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-16467855,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-16809768,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-16815035,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-17869524,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-6831420,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-8570628,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-8950359,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18023582-9816319
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
281-4
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
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pubmed:year |
2008
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pubmed:articleTitle |
Phosphoramidate derivatives of hydroxysteroids as inhibitors of prostate-specific membrane antigen.
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pubmed:affiliation |
Department of Chemistry, Washington State University, Pullman, WA 99164-4630, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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