rdf:type |
|
lifeskim:mentions |
umls-concept:C0005516,
umls-concept:C0006142,
umls-concept:C0025914,
umls-concept:C0026809,
umls-concept:C0035647,
umls-concept:C0086418,
umls-concept:C0243077,
umls-concept:C0259190,
umls-concept:C0591833,
umls-concept:C1261253,
umls-concept:C1328819,
umls-concept:C1334043,
umls-concept:C1417602
|
pubmed:issue |
2
|
pubmed:dateCreated |
2009-1-26
|
pubmed:abstractText |
The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine N-acetyltransferase 1 and mouse arylamine N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner. (1)H NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Arylamine N-Acetyltransferase,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/N-acetyltransferase 1,
http://linkedlifedata.com/resource/pubmed/chemical/Nat2 enzyme, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Rhodanine,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazolidinediones,
http://linkedlifedata.com/resource/pubmed/chemical/Tumor Markers, Biological,
http://linkedlifedata.com/resource/pubmed/chemical/thiazolidine-2,4-dione
|
pubmed:status |
MEDLINE
|
pubmed:month |
Jan
|
pubmed:issn |
1464-3391
|
pubmed:author |
|
pubmed:issnType |
Electronic
|
pubmed:day |
15
|
pubmed:volume |
17
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
905-18
|
pubmed:meshHeading |
pubmed-meshheading:19059786-Animals,
pubmed-meshheading:19059786-Arylamine N-Acetyltransferase,
pubmed-meshheading:19059786-Binding Sites,
pubmed-meshheading:19059786-Breast Neoplasms,
pubmed-meshheading:19059786-Enzyme Inhibitors,
pubmed-meshheading:19059786-Female,
pubmed-meshheading:19059786-Humans,
pubmed-meshheading:19059786-Isoenzymes,
pubmed-meshheading:19059786-Mice,
pubmed-meshheading:19059786-Rhodanine,
pubmed-meshheading:19059786-Thiazolidinediones,
pubmed-meshheading:19059786-Tumor Markers, Biological
|
pubmed:year |
2009
|
pubmed:articleTitle |
Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2.
|
pubmed:affiliation |
Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|