| pubmed-article:18630890 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:18630890 | lifeskim:mentions | umls-concept:C0442027 | lld:lifeskim |
| pubmed-article:18630890 | lifeskim:mentions | umls-concept:C0005508 | lld:lifeskim |
| pubmed-article:18630890 | lifeskim:mentions | umls-concept:C1515655 | lld:lifeskim |
| pubmed-article:18630890 | lifeskim:mentions | umls-concept:C1879762 | lld:lifeskim |
| pubmed-article:18630890 | pubmed:issue | 15 | lld:pubmed |
| pubmed-article:18630890 | pubmed:dateCreated | 2008-8-8 | lld:pubmed |
| pubmed-article:18630890 | pubmed:abstractText | Aurora kinase inhibitors have attracted a great deal of interest as a new class of antimitotic agents. We report a novel class of Aurora inhibitors based on a pentacyclic scaffold. A prototype pentacyclic inhibitor 32 (AKI-001) derived from two early lead structures improves upon the best properties of each parent and compares favorably to a previously reported Aurora inhibitor, 39 (VX-680). The inhibitor exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near stasis (92% TGI) in an HCT116 mouse xenograft model. | lld:pubmed |
| pubmed-article:18630890 | pubmed:language | eng | lld:pubmed |
| pubmed-article:18630890 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:18630890 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18630890 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:18630890 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:18630890 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:MeeSS | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:WalkerLeslieL | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:MoffatJohnJ | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:RanYingqingY | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:UltschMarkM | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:CochranAndrea... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:KrellHans-Wil... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:LiangJunJ | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:ZhuBing-YanBY | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:WiesmannChris... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:PhillipsGailG | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:RügerPetraP | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:RüthMatthiasM | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:SafinaBrianB | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:BlackwoodEliz... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:RawsonThomas... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:BurdickDanD | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:CorsonLauraL | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:DotsonJennaJ | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:DrummondJason... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:FieldsCarterC | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:GeorgesGuy... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:GollerBernhar... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:HalladayJason... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:HunsakerThoma... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:KleinheinzTra... | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:LimbergAnjaA | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:McNuttAngelaA | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:ZhangBirongB | lld:pubmed |
| pubmed-article:18630890 | pubmed:author | pubmed-author:ZhouAiheA | lld:pubmed |
| pubmed-article:18630890 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:18630890 | pubmed:day | 14 | lld:pubmed |
| pubmed-article:18630890 | pubmed:volume | 51 | lld:pubmed |
| pubmed-article:18630890 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:18630890 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:18630890 | pubmed:pagination | 4465-75 | lld:pubmed |
| pubmed-article:18630890 | pubmed:dateRevised | 2011-7-11 | lld:pubmed |
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| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:meshHeading | pubmed-meshheading:18630890... | lld:pubmed |
| pubmed-article:18630890 | pubmed:year | 2008 | lld:pubmed |
| pubmed-article:18630890 | pubmed:articleTitle | A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability. | lld:pubmed |
| pubmed-article:18630890 | pubmed:affiliation | Departments of Small Molecule Drug DiscoVery, Cell Cycle and Global Regulators, Translational Oncology, and Protein Engineering, Genentech, Inc, 1 DNA Way, South San Francisco, California 94080, USA. | lld:pubmed |
| pubmed-article:18630890 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:18630890 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:18630890 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:18630890 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:18630890 | lld:pubmed |
