| pubmed-article:10945629 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C0013216 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C0242275 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C0019932 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C0599894 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C0851285 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C1511636 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:10945629 | lifeskim:mentions | umls-concept:C1521840 | lld:lifeskim |
| pubmed-article:10945629 | pubmed:issue | 15 | lld:pubmed |
| pubmed-article:10945629 | pubmed:dateCreated | 2000-8-31 | lld:pubmed |
| pubmed-article:10945629 | pubmed:abstractText | Targeting chemotherapy selectively to cancers can reduce the toxic side effects. AN-152, a conjugate of doxorubicin and [D-Lys6]-luteinizing hormone-releasing hormone (LH-RH), is more potent against LH-RH receptor-bearing cancers and produces less peripheral toxicity than doxorubicin. Many cancers, e.g., 50% of breast cancers, but few normal tissues express these receptors, providing a selective target for this cytotoxic conjugate. In this study, the effectiveness of AN-152 was heightened by receptor up-regulation. The cytotoxic effect of AN-152 can be regulated by the number of active LH-RH receptors on cancer cells. LH-RH receptor-positive (MCF-7) and -negative (UCI-107) cancer cells were treated with epidermal growth factor (EGF) or the somatostatin analogue, RC-160. EGF and RC-160 have been shown previously to regulate LH-RH receptors through phosphorylation. The effect of receptor regulation, by hormone exposure, on the cytotoxicity of AN-152 and doxorubicin and on the cellular uptake of AN-152, [D-Lys6]LH-RH, or doxorubicin was assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and by two-photon laser scanning microscopy. The results demonstrated that the cellular entry of the conjugate was: (a) specific for cancers with LH-RH receptors; (b) up-regulated by EGF; (c) down-regulated by RC-160; and (d) the cytotoxicity of the AN-152 paralleled the efficiency of entry. This study illustrates the potential use of receptor regulation for increasing the efficacy of chemotherapeutic approaches that are directed to cell surface receptors. | lld:pubmed |
| pubmed-article:10945629 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:language | eng | lld:pubmed |
| pubmed-article:10945629 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:10945629 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:10945629 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:10945629 | pubmed:issn | 0008-5472 | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:SchallyA VAV | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:NagyAA | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:BergerE AEA | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:LiebowCC | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:WangXX | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:PrasadP NPN | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:KrebsL JLJ | lld:pubmed |
| pubmed-article:10945629 | pubmed:author | pubmed-author:PudavarH EHE | lld:pubmed |
| pubmed-article:10945629 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:10945629 | pubmed:day | 1 | lld:pubmed |
| pubmed-article:10945629 | pubmed:volume | 60 | lld:pubmed |
| pubmed-article:10945629 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:10945629 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:10945629 | pubmed:pagination | 4194-9 | lld:pubmed |
| pubmed-article:10945629 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
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| pubmed-article:10945629 | pubmed:meshHeading | pubmed-meshheading:10945629... | lld:pubmed |
| pubmed-article:10945629 | pubmed:meshHeading | pubmed-meshheading:10945629... | lld:pubmed |
| pubmed-article:10945629 | pubmed:meshHeading | pubmed-meshheading:10945629... | lld:pubmed |
| pubmed-article:10945629 | pubmed:meshHeading | pubmed-meshheading:10945629... | lld:pubmed |
| pubmed-article:10945629 | pubmed:meshHeading | pubmed-meshheading:10945629... | lld:pubmed |
| pubmed-article:10945629 | pubmed:meshHeading | pubmed-meshheading:10945629... | lld:pubmed |
| pubmed-article:10945629 | pubmed:year | 2000 | lld:pubmed |
| pubmed-article:10945629 | pubmed:articleTitle | Regulation of targeted chemotherapy with cytotoxic lutenizing hormone-releasing hormone analogue by epidermal growth factor. | lld:pubmed |
| pubmed-article:10945629 | pubmed:affiliation | Department of Chemistry, Institute for Lasers, Photonics, and Biophotonics, State University of New York, Buffalo 14260, USA. | lld:pubmed |
| pubmed-article:10945629 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:10945629 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:10945629 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:10945629 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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