pubmed-article:20728365 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0025202 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0020205 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0022646 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0002302 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0003765 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0024337 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0030956 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0184511 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0332294 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0392756 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0243144 | lld:lifeskim |
pubmed-article:20728365 | lifeskim:mentions | umls-concept:C0559956 | lld:lifeskim |
pubmed-article:20728365 | pubmed:issue | 18 | lld:pubmed |
pubmed-article:20728365 | pubmed:dateCreated | 2010-9-6 | lld:pubmed |
pubmed-article:20728365 | pubmed:abstractText | The purpose of this study was to reduce the non-specific renal uptake of Arg-Gly-Asp (RGD)-conjugated alpha-melanocyte stimulating hormone (alpha-MSH) hybrid peptide through structural modification or L-lysine co-injection. The RGD motif {cyclic(Arg-Gly-Asp-DTyr-Asp)} was coupled to [Cys(3,4,10), D-Phe7, Arg11] alpha-MSH3-13 {(Arg11)CCMSH} through the Arg linker (substituting the Lys linker) to generate a novel RGD-Arg-(Arg11)CCMSH hybrid peptide. The melanoma targeting and pharmacokinetic properties of 99mTc-RGD-Arg-(Arg11)CCMSH were determined in B16/F1 melanoma-bearing C57 mice. The effect of L-lysine co-injection on the renal uptake was determined through the co-injection of L-lysine with 99mTc-RGD-Arg-(Arg11)CCMSH or 99mTc-RGD-Lys-(Arg11)CCMSH. Replacement of the Lys linker with an Arg linker exhibited a profound effect in reducing the non-specific renal uptake of 99mTc-RGD-Arg-(Arg11)CCMSH, as well as increasing the tumor uptake of 99mTc-RGD-Arg-(Arg11)CCMSH compared to 99mTc-RGD-Lys-(Arg11)CCMSH. 99mTc-RGD-Arg-(Arg11)CCMSH exhibited high tumor uptake (21.41+/-3.74% ID/g at 2 h post-injection) and prolonged tumor retention (6.81+/-3.71% ID/g at 24 h post-injection) in B16/F1 melanoma-bearing mice. The renal uptake values of 99mTc-RGD-Arg-(Arg11)CCMSH were 40.14-64.08% of those of 99mTc-RGD-Lys-(Arg11)CCMSH (p<0.05) at 0.5, 2, 4 and 24 h post-injection. Co-injection of L-lysine was effective in decreasing the renal uptakes of 99mTc-RGD-Arg-(Arg11)CCMSH by 27.7% and 99mTc-RGD-Lys-(Arg11)CCMSH by 52.1% at 2 h post-injection. Substitution of the Lys linker with an Arg linker dramatically improved the melanoma uptake and reduced the renal uptake of 99mTc-RGD-Arg-(Arg11)CCMSH, warranting the further evaluation of 188Re-labeled RGD-Arg-(Arg11)CCMSH as a novel MC1 receptor-targeting therapeutic peptide for melanoma treatment in the future. | lld:pubmed |
pubmed-article:20728365 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:language | eng | lld:pubmed |
pubmed-article:20728365 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:20728365 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:20728365 | pubmed:month | Sep | lld:pubmed |
pubmed-article:20728365 | pubmed:issn | 1464-3391 | lld:pubmed |
pubmed-article:20728365 | pubmed:author | pubmed-author:BerwickMarian... | lld:pubmed |
pubmed-article:20728365 | pubmed:author | pubmed-author:MiaoYubinY | lld:pubmed |
pubmed-article:20728365 | pubmed:author | pubmed-author:GuoHaixunH | lld:pubmed |
pubmed-article:20728365 | pubmed:author | pubmed-author:YangJianquanJ | lld:pubmed |
pubmed-article:20728365 | pubmed:author | pubmed-author:PadillaR... | lld:pubmed |
pubmed-article:20728365 | pubmed:copyrightInfo | Copyright (c) 2010 Elsevier Ltd. All rights reserved. | lld:pubmed |
pubmed-article:20728365 | pubmed:issnType | Electronic | lld:pubmed |
pubmed-article:20728365 | pubmed:day | 15 | lld:pubmed |
pubmed-article:20728365 | pubmed:volume | 18 | lld:pubmed |
pubmed-article:20728365 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:20728365 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:20728365 | pubmed:pagination | 6695-700 | lld:pubmed |
pubmed-article:20728365 | pubmed:dateRevised | 2011-9-26 | lld:pubmed |
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pubmed-article:20728365 | pubmed:year | 2010 | lld:pubmed |
pubmed-article:20728365 | pubmed:articleTitle | Replacement of the Lys linker with an Arg linker resulting in improved melanoma uptake and reduced renal uptake of Tc-99m-labeled Arg-Gly-Asp-conjugated alpha-melanocyte stimulating hormone hybrid peptide. | lld:pubmed |
pubmed-article:20728365 | pubmed:affiliation | College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA. | lld:pubmed |
pubmed-article:20728365 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:20728365 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
pubmed-article:20728365 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:20728365 | lld:chembl |