| pubmed-article:18088090 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0002302 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0022914 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0250457 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0038477 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0599894 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:18088090 | lifeskim:mentions | umls-concept:C0439596 | lld:lifeskim |
| pubmed-article:18088090 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:18088090 | pubmed:dateCreated | 2008-1-17 | lld:pubmed |
| pubmed-article:18088090 | pubmed:abstractText | A variety of dicarboxylic acid linkers introduced between the alpha-amino group of Pro(6) and the -amino group of Lys(10) of the cyclic lactam alpha-melanocyte-stimulating hormone (alpha-MSH)-derived Pro(6)-D-Phe(7)/D-Nal(2')(7)-Arg(8)-Trp(9)-Lys(10)-NH2 pentapeptide template lead to nanomolar range and selective hMC3R agonists and antagonists. Replacement of the Pro(6) residue and the dicarboxylic acid linker with 2,3-pyrazine-dicarboxylic acid furnished a highly selective nanomolar range hMC3R partial agonist (analogue 12, c[CO-2,3-pyrazine-CO-D-Phe-Arg-Trp-Lys]-NH2, EC50 = 27 nM, 70% max cAMP) and an hMC3R antagonist (analogue 13, c[CO-2,3-pyrazine-CO-D-Nal(2')-Arg-Trp-Lys]-NH2, IC50 = 23 nM). Modeling experiments suggest that 2,3-pyrazinedicarboxylic acid stabilizes a beta-turn-like structure with the D-Phe/D-Nal(2') residues, which explains the high potency of the corresponding peptides. Placement of a Nle residue in position 6 produced a hMC3R/hMC5R antagonist (analogue 15, c[CO-(CH 2)2-CO-Nle-D-Nal(2')-Arg-Trp-Lys]-NH2, IC50 = 12 and 17 nM, respectively), similarly to the previously described cyclic gamma-melanocyte-stimulating hormone (gamma-MSH)-derived hMC3R/hMC5R antagonists. These newly developed melanotropins will serve as critical biochemical tools for elucidating the full spectrum of functions performed by the physiologically important melanocortin-3 receptor. | lld:pubmed |
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| pubmed-article:18088090 | pubmed:language | eng | lld:pubmed |
| pubmed-article:18088090 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18088090 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:18088090 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:18088090 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:18088090 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:18088090 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:18088090 | pubmed:author | pubmed-author:HrubyVictor... | lld:pubmed |
| pubmed-article:18088090 | pubmed:author | pubmed-author:TrivediDevD | lld:pubmed |
| pubmed-article:18088090 | pubmed:author | pubmed-author:CaiMinyingM | lld:pubmed |
