Literature DB >> 10876051

The agouti-related protein decapeptide (Yc[CRFFNAFC]Y) possesses agonist activity at the murine melanocortin-1 receptor.

C Haskell-Luevano1, E K Monck, Y P Wan, A M Schentrup.   

Abstract

Agouti-related protein (AGRP) is a naturally occurring antagonist of the brain melanocortin receptors (MC3R and MC4R) and is physiologically implicated as participating in feeding behavior and energy homeostasis. The human AGRP decapeptide Yc[CRFFNAFC]Y has been previously reported as binding to the human MC3 and MC4 receptors and antagonizing the MC4 receptor. We have synthesized this decapeptide and pharmacologically characterized it at the murine melanocortin receptors and found it to possess MC4R antagonist activity (pA(2) = 6.8) and, unexpectedly, MC1R agonist activity (EC(50) = 2.89 microM). This study characterizes the first AGRP-based peptide agonist at the melanocortin receptors.

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Year:  2000        PMID： 10876051     DOI： 10.1016/s0196-9781(00)00194-7

Source DB:  PubMed          Journal:  Peptides        ISSN： 0196-9781            Impact factor:   3.750


  8 in total

1.  Arg-Phe-Phe d-Amino Acid Stereochemistry Scan in the Macrocyclic Agouti-Related Protein Antagonist Scaffold c[Pro-Arg-Phe-Phe-Xxx-Ala-Phe-DPro] Results in Unanticipated Melanocortin-1 Receptor Agonist Profiles.

Authors:  Mark D Ericson; Zoe M Koerperich; Katie T Freeman; Katlyn A Fleming; Carrie Haskell-Luevano
Journal:  ACS Chem Neurosci       Date:  2018-07-20       Impact factor: 4.418

2.  Structure-Activity Relationship Studies of a Macrocyclic AGRP-Mimetic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Yield Potent and Selective Melanocortin-4 Receptor Antagonists and Melanocortin-5 Receptor Inverse Agonists That Increase Food Intake in Mice.

Authors:  Katlyn A Fleming; Mark D Ericson; Katie T Freeman; Danielle N Adank; Mary M Lunzer; Stacey L Wilber; Carrie Haskell-Luevano
Journal:  ACS Chem Neurosci       Date:  2018-02-13       Impact factor: 4.418

3.  1,2,3-Triazole Rings as a Disulfide Bond Mimetic in Chimeric AGRP-Melanocortin Peptides: Design, Synthesis, and Functional Characterization.

Authors:  Srinivasa R Tala; Anamika Singh; Cody J Lensing; Sathya M Schnell; Katie T Freeman; James R Rocca; Carrie Haskell-Luevano
Journal:  ACS Chem Neurosci       Date:  2018-01-18       Impact factor: 4.418

4.  Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.

Authors:  Mark D Ericson; Andrzej Wilczynski; Nicholas B Sorensen; Zhimin Xiang; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2015-04-21       Impact factor: 7.446

5.  Implication of the melanocortin-3 receptor in the regulation of food intake.

Authors:  Boman G Irani; Zhimin Xiang; Hossein N Yarandi; Jerry R Holder; Marcus C Moore; Rayna M Bauzo; Bettina Proneth; Amanda M Shaw; William J Millard; James B Chambers; Stephen C Benoit; Deborah J Clegg; Carrie Haskell-Luevano
Journal:  Eur J Pharmacol       Date:  2011-01-01       Impact factor: 4.432

6.  Loop-swapped chimeras of the agouti-related protein and the agouti signaling protein identify contacts required for melanocortin 1 receptor selectivity and antagonism.

Authors:  Mira P Patel; Camila S Cribb Fabersunne; Ying-Kui Yang; Christopher B Kaelin; Gregory S Barsh; Glenn L Millhauser
Journal:  J Mol Biol       Date:  2010-09-08       Impact factor: 5.469

7.  Synergistic Multiresidue Substitutions of a Macrocyclic c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Agouti-Related Protein (AGRP) Scaffold Yield Potent and >600-Fold MC4R versus MC3R Selective Melanocortin Receptor Antagonists.

Authors:  Katlyn A Fleming; Katie T Freeman; Mark D Ericson; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2018-08-16       Impact factor: 7.446

8.  Macrocyclic Modalities Combining Peptide Epitopes and Natural Product Fragments.

Authors:  Stéphanie M Guéret; Sasikala Thavam; Rodrigo J Carbajo; Marco Potowski; Niklas Larsson; Göran Dahl; Anita Dellsén; Tom N Grossmann; Alleyn T Plowright; Eric Valeur; Malin Lemurell; Herbert Waldmann
Journal:  J Am Chem Soc       Date:  2020-03-02       Impact factor: 15.419
  8 in total

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