| pubmed-article:17256834 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17256834 | lifeskim:mentions | umls-concept:C0376515 | lld:lifeskim |
| pubmed-article:17256834 | lifeskim:mentions | umls-concept:C1332397 | lld:lifeskim |
| pubmed-article:17256834 | lifeskim:mentions | umls-concept:C1522538 | lld:lifeskim |
| pubmed-article:17256834 | lifeskim:mentions | umls-concept:C2603343 | lld:lifeskim |
| pubmed-article:17256834 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:17256834 | lifeskim:mentions | umls-concept:C1554184 | lld:lifeskim |
| pubmed-article:17256834 | pubmed:issue | 4 | lld:pubmed |
| pubmed-article:17256834 | pubmed:dateCreated | 2007-2-15 | lld:pubmed |
| pubmed-article:17256834 | pubmed:abstractText | Overexpression of the antiapototic proteins Bcl-2 and Bcl-xL provides a common mechanism through which cancer cells gain a survival advantage and become resistant to conventional chemotherapy. Inhibition of these prosurvival proteins is an attractive strategy for cancer therapy. We recently described the discovery of a selective Bcl-xL antagonist that potentiates the antitumor activity of chemotherapy and radiation. Here we describe the use of structure-guided design to exploit a deep hydrophobic binding pocket on the surface of these proteins to develop the first dual, subnanomolar inhibitors of Bcl-xL and Bcl-2. This study culminated in the identification of 2, which exhibited EC50 values of 8 nM and 30 nM in Bcl-2 and Bcl-xL dependent cells, respectively. Compound 2 demonstrated single agent efficacy against human follicular lymphoma cell lines that overexpress Bcl-2, and efficacy in a murine xenograft model of lymphoma when given both as a single agent and in combination with etoposide. | lld:pubmed |
| pubmed-article:17256834 | pubmed:language | eng | lld:pubmed |
| pubmed-article:17256834 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17256834 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:17256834 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:17256834 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17256834 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17256834 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17256834 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:17256834 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:NgShi-ChungSC | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:PetrosAndrew... | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:FesikStephen... | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:DingHongH | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:RosenbergSaul... | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:KunzerAaronA | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:WendtMichael... | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:ZhangHaichaoH | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:WangXiluX | lld:pubmed |
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| pubmed-article:17256834 | pubmed:author | pubmed-author:MittenMichael... | lld:pubmed |
| pubmed-article:17256834 | pubmed:author | pubmed-author:MartineauDarl... | lld:pubmed |
| pubmed-article:17256834 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:17256834 | pubmed:day | 22 | lld:pubmed |
| pubmed-article:17256834 | pubmed:volume | 50 | lld:pubmed |
| pubmed-article:17256834 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17256834 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17256834 | pubmed:pagination | 641-62 | lld:pubmed |
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| pubmed-article:17256834 | pubmed:year | 2007 | lld:pubmed |
| pubmed-article:17256834 | pubmed:articleTitle | Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. | lld:pubmed |
| pubmed-article:17256834 | pubmed:affiliation | Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA. | lld:pubmed |
| pubmed-article:17256834 | pubmed:publicationType | Journal Article | lld:pubmed |
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