| pubmed-article:17502149 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17502149 | lifeskim:mentions | umls-concept:C0376358 | lld:lifeskim |
| pubmed-article:17502149 | lifeskim:mentions | umls-concept:C0144576 | lld:lifeskim |
| pubmed-article:17502149 | lifeskim:mentions | umls-concept:C0005508 | lld:lifeskim |
| pubmed-article:17502149 | lifeskim:mentions | umls-concept:C0599894 | lld:lifeskim |
| pubmed-article:17502149 | lifeskim:mentions | umls-concept:C1709059 | lld:lifeskim |
| pubmed-article:17502149 | pubmed:issue | 14 | lld:pubmed |
| pubmed-article:17502149 | pubmed:dateCreated | 2007-6-6 | lld:pubmed |
| pubmed-article:17502149 | pubmed:abstractText | Four novel water-soluble peptide-paclitaxel conjugates were designed and synthesized as prostate-specific antigen (PSA)-activated prodrugs for prostate cancer therapy. These prodrugs were composed of a peptide, HSSKLQ or SSKYQ, each of which is selectively cleavable by PSA; a self-immolative linker, either para-aminobenzyl alcohol (PABS) or ethylene diamine (EDA); and the parent drug, paclitaxel. Introduction of a PABA or EDA linker between the peptide and paclitaxel in prodrugs 2-5 resulted in products with an increased rate of hydrolysis by PSA. The stability of prodrugs 2 and 3, with the PABA linker, was poor in the serum-containing medium because of the weak carbonate bond between the PABA and paclitaxel; however, this disadvantage was overcome by introducing a carbamate bond using an EDA linker in prodrugs 4 and 5. Thus, the incorporation of an EDA linker increased both the stability and PSA-mediated activation of these prodrugs. The cytotoxicity of each prodrug, as compared to paclitaxel, was determined against a variety of cell lines, including the PSA-secreting CWR22Rv1 prostate cancer cell line. The EDA-derived prodrug of paclitaxel 5 was stable and capable of being efficiently converted to an active drug that killed cells specifically in the presence of PSA, suggesting that this prodrug and similarly designed PSA-cleavable prodrugs may have potential as prostate cancer-specific therapeutic agents. | lld:pubmed |
| pubmed-article:17502149 | pubmed:language | eng | lld:pubmed |
| pubmed-article:17502149 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17502149 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:17502149 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17502149 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17502149 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17502149 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17502149 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17502149 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17502149 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:17502149 | pubmed:issn | 0968-0896 | lld:pubmed |
| pubmed-article:17502149 | pubmed:author | pubmed-author:KhanSaeed RSR | lld:pubmed |
| pubmed-article:17502149 | pubmed:author | pubmed-author:DenmeadeSamue... | lld:pubmed |
| pubmed-article:17502149 | pubmed:author | pubmed-author:IsaacsJohn... | lld:pubmed |
| pubmed-article:17502149 | pubmed:author | pubmed-author:KumarSrinivas... | lld:pubmed |
| pubmed-article:17502149 | pubmed:author | pubmed-author:WilliamsSimon... | lld:pubmed |
| pubmed-article:17502149 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:17502149 | pubmed:day | 15 | lld:pubmed |
| pubmed-article:17502149 | pubmed:volume | 15 | lld:pubmed |
| pubmed-article:17502149 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17502149 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17502149 | pubmed:pagination | 4973-84 | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:meshHeading | pubmed-meshheading:17502149... | lld:pubmed |
| pubmed-article:17502149 | pubmed:year | 2007 | lld:pubmed |
| pubmed-article:17502149 | pubmed:articleTitle | Modulating paclitaxel bioavailability for targeting prostate cancer. | lld:pubmed |
| pubmed-article:17502149 | pubmed:affiliation | The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, The Johns Hopkins School of Medicine, 1650 Orleans Street, Baltimore, MD 21231, USA. | lld:pubmed |
| pubmed-article:17502149 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:17502149 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:17502149 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:17502149 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:17502149 | lld:pubmed |
