Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution |
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| Authors: | Danho Waleed Swistok Joseph Cheung Adrian Wai-Hing Kurylko Grazyna Franco Lucia Chu Xin-Jie Chen Li Yagaloff Keith |
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| Affiliation: | Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. waleed.danho@roche.com |
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| Abstract: | A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Nal and Bta) were identified in this study. |
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