Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 한소엽 | - |
dc.date.accessioned | 2018-05-30T08:13:48Z | - |
dc.date.available | 2018-05-30T08:13:48Z | - |
dc.date.issued | 2006 | - |
dc.identifier.issn | 1747-0277 | - |
dc.identifier.other | OAK-3464 | - |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/243388 | - |
dc.description.abstract | The effects of the linker arm rigidity and size on melanocortin receptor selectivity were explored in a series of compounds using cyclic lactam α-melanocyte-stimulating hormone template. A variety of dicarboxylic acid linkers introduced between the α-amino group of His 6 and the ε-amino group of Lys 10 lead to high-affinity, selective human melanocortin receptor-1 and -5 (hMC1R and hMC5R) antagonists. The incorporation of hydrophilic functions into the linker arm was found to be unfavorable for both binding potency and receptor selectivity. Analogs 8 and 9 containing highly conformationally constrained hydrophobic linkers (m- and p-phthalic acids) were found to be selective nanomolar range hMC1R antagonists (IC 50 = 7 and 4 nm, respectively), whereas the employment of a small conformationally constrained linker (maleic acid) resulted in a high-affinity (IC 50 = 19 nm) and selective hMC5R antagonist (analog 12). These newly developed melanotropins will serve as critical biochemical tools for elucidating the full spectrum of functions performed by the physiologically important melanocortin-1 and -5 receptors. © 2006 The Authors. | - |
dc.language | English | - |
dc.title | Effects of macrocycle size and rigidity on melanocortin receptor-1 and -5 selectivity in cyclic lactam α-melanocyte-stimulating hormone analogs | - |
dc.type | Article | - |
dc.relation.issue | 5 | - |
dc.relation.volume | 67 | - |
dc.relation.index | SCI | - |
dc.relation.index | SCIE | - |
dc.relation.index | SCOPUS | - |
dc.relation.startpage | 329 | - |
dc.relation.lastpage | 335 | - |
dc.relation.journaltitle | Chemical Biology and Drug Design | - |
dc.identifier.doi | 10.1111/j.1747-0285.2006.00383.x | - |
dc.identifier.wosid | WOS:000239311000003 | - |
dc.identifier.scopusid | 2-s2.0-33745232379 | - |
dc.author.google | Mayorov A.V. | - |
dc.author.google | Han S.-Y. | - |
dc.author.google | Cai M. | - |
dc.author.google | Hammer M.R. | - |
dc.author.google | Trivedi D. | - |
dc.author.google | Hruby V.J. | - |
dc.contributor.scopusid | 한소엽(7405944194) | - |
dc.date.modifydate | 20200928112844 | - |