| pubmed-article:20927342 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0035647 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0115305 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0005839 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0333348 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0023688 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0599894 | lld:lifeskim |
| pubmed-article:20927342 | lifeskim:mentions | umls-concept:C0185125 | lld:lifeskim |
| pubmed-article:20927342 | pubmed:issue | 9 | lld:pubmed |
| pubmed-article:20927342 | pubmed:dateCreated | 2010-10-7 | lld:pubmed |
| pubmed-article:20927342 | pubmed:abstractText | Active targeting of a drug carrier to a specific target site is crucial to provide a safe and efficient delivery of therapeutics and imaging contrast agents. E-selectin expression is induced on the endothelial cell surface of vessels in response to inflammatory stimuli but is absent in the normal vessels. Thus, E-selectin is an attractive molecular target, and high affinity ligands for E-selectin could be powerful tools for the delivery of therapeutics and/or imaging agents to inflamed vessels. In this study, we identified a thiophosphate modified aptamer (thioaptamer, TA) against E-selectin (ESTA-1) by employing a two-step selection strategy: a recombinant protein-based TA binding selection from a combinatorial library followed by a cell-based TA binding selection using E-selectin expressing human microvascular endothelial cells. ESTA-1 selectively bound to E-selectin with nanomolar binding affinity (K(D)?= 47 nM) while exhibiting minimal cross reactivity to P- and L-selectin. Furthermore, ESTA-1 binding to E-selectin on the endothelial cells markedly antagonized the adhesion (over 75% inhibition) of sLe(x) positive HL-60 cells at nanomolar concentration. ESTA-1 also bound specifically to the inflamed tumor-associated vasculature of human carcinomas derived from breast, ovarian, and skin but not to normal organs, and this binding was highly associated with the E-selectin expression level. Similarly, intravenously injected ESTA-1 demonstrated distinct binding to the tumor vasculature in a breast cancer xenograft model. Together, our data substantiates the discovery of a thioaptamer (ESTA-1) that binds to E-selectin with high affinity and specificity, thereby highlighting the potential application of ESTA-1 for E-selectin targeted delivery. | lld:pubmed |
| pubmed-article:20927342 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20927342 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:20927342 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20927342 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20927342 | pubmed:issn | 1932-6203 | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:XuZ CZC | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:ZelTT | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:AustinEEJr | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:SoodAnil KAK | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:GorensteinDav... | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:FerrariMauroM | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:SomasunderamA... | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:MannAman PAP | lld:pubmed |
| pubmed-article:20927342 | pubmed:author | pubmed-author:Nieves-Alicea... | lld:pubmed |
| pubmed-article:20927342 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20927342 | pubmed:volume | 5 | lld:pubmed |
| pubmed-article:20927342 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20927342 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20927342 | pubmed:meshHeading | pubmed-meshheading:20927342... | lld:pubmed |
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| pubmed-article:20927342 | pubmed:meshHeading | pubmed-meshheading:20927342... | lld:pubmed |
| pubmed-article:20927342 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20927342 | pubmed:articleTitle | Identification of thioaptamer ligand against E-selectin: potential application for inflamed vasculature targeting. | lld:pubmed |
| pubmed-article:20927342 | pubmed:affiliation | Department of Nanomedicine and Biomedical Engineering, University of Texas Health Science Center, Houston, Texas, United States of America. | lld:pubmed |
| pubmed-article:20927342 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:20927342 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:20927342 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:20927342 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
