Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
23
pubmed:dateCreated
2009-2-20
pubmed:abstractText
A series of tricyclic, conformationally constrained Smac mimetics have been designed, synthesized, and evaluated. The most potent compound 6 (WS-5) binds to XIAP, cIAP-1, and cIAP-2 with K(i) of 18, 1.1, and 4.2 nM, respectively. Compound 6 antagonizes XIAP in a functional assay, induces cIAP-1 degradation, inhibits cell growth with an IC(50) of 68 nM in the MDA-MB-231 cancer cell line, and effectively induces cancer cells to undergo apoptosis.
pubmed:grant
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-10688869, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-10929711, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-10929712, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-11140637, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-11140638, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-11242052, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-11445667, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-12042762, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-12120092, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-12620238, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-14960576, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-15293984, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-15317454, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-15325294, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-15337122, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-15353805, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-15612682, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-17168540, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-17181177, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-17892425, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-17996648, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-17999504, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-18022362, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-18022363, http://linkedlifedata.com/resource/pubmed/commentcorrection/19012392-9990849
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
11
pubmed:volume
51
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
7352-5
pubmed:dateRevised
2011-11-1
pubmed:meshHeading
pubmed-meshheading:19012392-Antineoplastic Agents, pubmed-meshheading:19012392-Apoptosis, pubmed-meshheading:19012392-Binding Sites, pubmed-meshheading:19012392-Biomimetic Materials, pubmed-meshheading:19012392-Caspases, pubmed-meshheading:19012392-Cell Line, Tumor, pubmed-meshheading:19012392-Cell Proliferation, pubmed-meshheading:19012392-Crystallography, X-Ray, pubmed-meshheading:19012392-Cyclization, pubmed-meshheading:19012392-Dose-Response Relationship, Drug, pubmed-meshheading:19012392-Drug Design, pubmed-meshheading:19012392-Drug Evaluation, Preclinical, pubmed-meshheading:19012392-Drug Screening Assays, Antitumor, pubmed-meshheading:19012392-Enzyme Inhibitors, pubmed-meshheading:19012392-Humans, pubmed-meshheading:19012392-Inhibitor of Apoptosis Proteins, pubmed-meshheading:19012392-Mitochondria, pubmed-meshheading:19012392-Models, Molecular, pubmed-meshheading:19012392-Molecular Conformation, pubmed-meshheading:19012392-Molecular Weight, pubmed-meshheading:19012392-Stereoisomerism, pubmed-meshheading:19012392-Structure-Activity Relationship
pubmed:year
2008
pubmed:articleTitle
Design, synthesis, and evaluation of tricyclic, conformationally constrained small-molecule mimetics of second mitochondria-derived activator of caspases.
pubmed:affiliation
State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, China.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural