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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 |
2010-2-3
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pubmed:abstractText |
We report a strategy based on bioisosterism to improve the physicochemical properties of existing hydrophilic, urea-based GCPII inhibitors. Comprehensive structure-activity relationship studies of the P1' site of ZJ-43- and DCIBzL-based compounds identified several glutamate-free inhibitors with K(i) values below 20nM. Among them, compound 32d (K(i)=11nM) exhibited selective uptake in GCPII-expressing tumors by SPECT-CT imaging in mice. A novel conformational change of amino acids in the S1' pharmacophore pocket was observed in the X-ray crystal structure of GCPII complexed with 32d.
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pubmed:grant |
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pubmed:commentsCorrections |
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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:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
392-7
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pubmed:dateRevised |
2011-7-19
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pubmed:meshHeading |
pubmed-meshheading:19897367-Animals,
pubmed-meshheading:19897367-Binding Sites,
pubmed-meshheading:19897367-Crystallography, X-Ray,
pubmed-meshheading:19897367-Glutamate Carboxypeptidase II,
pubmed-meshheading:19897367-Lysine,
pubmed-meshheading:19897367-Mice,
pubmed-meshheading:19897367-Radiopharmaceuticals,
pubmed-meshheading:19897367-Structure-Activity Relationship,
pubmed-meshheading:19897367-Tomography, Emission-Computed, Single-Photon,
pubmed-meshheading:19897367-Urea
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pubmed:year |
2010
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pubmed:articleTitle |
Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies.
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pubmed:affiliation |
Department of Radiology, Johns Hopkins Medical Institutions, Baltimore, MD 21231, 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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