Structure-activity relationship of cyclic peptide Penta-c[Asp-His6-DPhe7-Arg8-Trp 9-Lys]-NH2 at the human melanocortin-1 and -4 receptors: His6 substitution

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 7, 2003, Pages 1307-1311

  Cheung, Adrian Wai Hing ^a   Danho, Waleed ^a   Swistok, Joseph ^a   Qi, Lida ^a   Kurylko, Grazyna ^a   Rowan, Karen ^a   Yeon, Mitch ^a   Franco, Lucia ^a   Chu, Xin Jie ^a   Chen, Li ^a   Yagaloff, Keith ^a  

^a HOFFMANN LA ROCHE INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOPEPTIDE; HISTIDINE; MELANOCORTIN 1 RECEPTOR AGONIST; MELANOCORTIN 4 RECEPTOR AGONIST; UNCLASSIFIED DRUG;

ARTICLE; DRUG ACTIVITY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; STRUCTURE ACTIVITY RELATION;

EID: 0037424716     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00114-8     Document Type: Article

References (14)

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12. A portion of this work was previously presented: Danho, W.; Swistok, J.; Cheung, A.; Chu, X.-J.; Wang, Y.; Chen, L.; Bartkovitz, D.; Gore, V.; Qi, L.; Fry, D.; Greeley, D.; Sun, H.; Guenot, J.; Franco, L.; Kurylko, G.; Rumennik, L.; Yagaloff, K. In Proceedings of the 2nd International/17th American Peptide Symposium; Lebl, M., Houghten, R., Eds.; Kluwer Academic: The Netherlands, 2001; p 701.
13. After our discovery that histidine surrogates such as 5-BrAtc could give rise to excellent hMC4R selectivity, Hruby et al. independently proposed that 'the position 6 of the synthetic melanocortin ligands is important for enhancing potency and selectivity at MC3 and MC4 melanocortin receptors'. Hruby, V. J.; Grieco, P.; Balse, P.; Han, G.; Weinberg, D.; McNeil, T. Abstract of Papers, 217th National Meeting of the American Chemical Society, Anaheim, CA; American Chemical Society: Washington, DC, 1999; Abstract MEDI-231. See also ref 13.
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