Literature DB >> 12639550

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.

Waleed Danho1, Joseph Swistok, Adrian Wai-Hing Cheung, Grazyna Kurylko, Lucia Franco, Xin-Jie Chu, Li Chen, Keith Yagaloff.   

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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Year:  2003        PMID： 12639550     DOI： 10.1016/s0960-894x(02)01052-1

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.

Authors:  Bettina Proneth; Irina D Pogozheva; Federico P Portillo; Henry I Mosberg; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2008-09-25       Impact factor: 7.446

2.  Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melanocortin-4 receptor (mMC4R).

Authors:  Anamika Singh; Marvin Dirain; Rachel Witek; James R Rocca; Arthur S Edison; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2013-03-25       Impact factor: 7.446

3.  Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.

Authors:  Skye R Doering; Aleksandar Todorovic; Carrie Haskell-Luevano
Journal:  ACS Med Chem Lett       Date:  2014-12-29       Impact factor: 4.345

4.  Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa1-Arg-(pI)DPhe-Xaa4-NH2.

Authors:  Skye R Doering; Katie T Freeman; Sathya M Schnell; Erica M Haslach; Marvin Dirain; Ginamarie Debevec; Phaedra Geer; Radleigh G Santos; Marc A Giulianotti; Clemencia Pinilla; Jon R Appel; Robert C Speth; Richard A Houghten; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2017-05-15       Impact factor: 7.446
  4 in total

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