19354253

Source:http://linkedlifedata.com/resource/pubmed/id/19354253

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Predicate	Object
rdf:type	pubmed:Citation
lifeskim:mentions	umls-concept:C0002482, umls-concept:C0021246, umls-concept:C0038323, umls-concept:C0041221, umls-concept:C0205314, umls-concept:C0599894, umls-concept:C0679622, umls-concept:C1521991
pubmed:issue	9
pubmed:dateCreated	2009-5-7
pubmed:abstractText	Trypanosoma cruzi (TC) causes Chagas disease, which in its chronic stage remains incurable. We have shown recently that specific inhibition of TC sterol 14alpha-demethylase (TCCYP51) with imidazole derivatives is effective in killing both extracellular and intracellular human stages of TC. An alternative set of TCCYP51 inhibitors has been identified using optical high throughput screening followed by web-database search for similar structures. The best TCCYP51 inhibitor from this search was found to have structural similarity to a class of cyclooxygenase-2-selective inhibitors, the indomethacin-amides. A number of indomethacin-amides were found to bind to TCCYP51, inhibit its activity in vitro, and produce strong antiparasitic effects in the cultured TC cells. Analysis of TC sterol composition indicated that the mode of action of the compounds is by inhibition of sterol biosynthesis in the parasite.
pubmed:grant	http://linkedlifedata.com/resource/pubmed/grant/AI007281, http://linkedlifedata.com/resource/pubmed/grant/AI080580, http://linkedlifedata.com/resource/pubmed/grant/CA89450, http://linkedlifedata.com/resource/pubmed/grant/ES00267, http://linkedlifedata.com/resource/pubmed/grant/GM067871, http://linkedlifedata.com/resource/pubmed/grant/HL007737, http://linkedlifedata.com/resource/pubmed/grant/R01 GM067871-06
pubmed:commentsCorrections	http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-10639181, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-10956194, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-12118272, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-12885242, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-14209972, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-14709628, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-15311940, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-15581355, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-15616285, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-15832445, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-16020724, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-16150644, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-16321980, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-16495535, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-16963187, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-17053932, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-17585868, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-17709461, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-18022567, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-18367671, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-18473504, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-3333533, http://linkedlifedata.com/resource/pubmed/commentcorrection/19354253-9835521
pubmed:language	eng
pubmed:journal	http://linkedlifedata.com/resource/pubmed/journal/9716531
pubmed:citationSubset	IM
pubmed:chemical	http://linkedlifedata.com/resource/pubmed/chemical/Amides, http://linkedlifedata.com/resource/pubmed/chemical/Antiparasitic Agents, http://linkedlifedata.com/resource/pubmed/chemical/CYP51A1 protein, human, http://linkedlifedata.com/resource/pubmed/chemical/Cytochrome P-450 Enzyme System, http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors, http://linkedlifedata.com/resource/pubmed/chemical/Indomethacin, http://linkedlifedata.com/resource/pubmed/chemical/Ligands, http://linkedlifedata.com/resource/pubmed/chemical/Sterol 14-Demethylase, http://linkedlifedata.com/resource/pubmed/chemical/Sterols
pubmed:status	MEDLINE
pubmed:month	May
pubmed:issn	1520-4804
pubmed:author	pubmed-author:CaprioliRichard MRM, pubmed-author:HargroveTatiana YTY, pubmed-author:KleshchenkoYuliya YYY, pubmed-author:KonkleMary EME, pubmed-author:LepeshevaGalina IGI, pubmed-author:MarnettLawrence JLJ, pubmed-author:NesW DavidWD, pubmed-author:RidenourWhitneyW, pubmed-author:UddinMd JashimMJ, pubmed-author:VillaltaFernandoF, pubmed-author:WatermanMichael RMR, pubmed-author:von KriesJens PJP
pubmed:issnType	Electronic
pubmed:day	14
pubmed:volume	52
pubmed:owner	NLM
pubmed:authorsComplete	Y
pubmed:pagination	2846-53
pubmed:dateRevised	2010-12-3
pubmed:meshHeading	pubmed-meshheading:19354253-Amides, pubmed-meshheading:19354253-Animals, pubmed-meshheading:19354253-Antiparasitic Agents, pubmed-meshheading:19354253-Cytochrome P-450 Enzyme System, pubmed-meshheading:19354253-Drug Evaluation, Preclinical, pubmed-meshheading:19354253-Enzyme Inhibitors, pubmed-meshheading:19354253-Extracellular Space, pubmed-meshheading:19354253-Indomethacin, pubmed-meshheading:19354253-Intracellular Space, pubmed-meshheading:19354253-Ligands, pubmed-meshheading:19354253-Sterol 14-Demethylase, pubmed-meshheading:19354253-Sterols, pubmed-meshheading:19354253-Trypanosoma cruzi
pubmed:year	2009
pubmed:articleTitle	Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase.
pubmed:affiliation	Department of Chemistry, School of Medicine, Vanderbilt University, Nashville, Tennessee 37232, USA.
pubmed:publicationType	Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural