Literature DB >> 26599352

Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.

Alfonso Carotenuto1, Francesco Merlino1, Minying Cai2, Diego Brancaccio1, Ali Munaim Yousif1, Ettore Novellino1, Victor J Hruby2, Paolo Grieco1,3.   

Abstract

The melanocortin receptors 3 and 4 control energy homeostasis, food-intake behavior, and correlated pathophysiological conditions. The melanocortin-4 receptor (MC4R) has been broadly investigated. In contrast, the knowledge related to physiological roles of the melanocortin-3 receptor (MC3R) is lacking because of the limited number of known MC3R selective ligands. Here, we report the design, synthesis, biological activity, conformational analysis, and docking with receptors of two potent and selective agonists at the human MC3 receptor.

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Year:  2015        PMID： 26599352      PMCID： PMC5070805          DOI： 10.1021/acs.jmedchem.5b01285

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  25 in total

1.  Analogs of MTII, lactam derivatives of alpha-melanotropin, modified at the N-terminus, and their selectivity at human melanocortin receptors 3, 4, and 5.

Authors:  M A Bednarek; T Macneil; R N Kalyani; R Tang; L H Van der Ploeg; D H Weinberg
Journal:  Biochem Biophys Res Commun       Date:  1999-07-22       Impact factor: 3.575

2.  Conformational study on cyclic melanocortin ligands and new insight into their binding mode at the MC4 receptor.

Authors:  Paolo Grieco; Diego Brancaccio; Ettore Novellino; Victor J Hruby; Alfonso Carotenuto
Journal:  Eur J Med Chem       Date:  2011-05-23       Impact factor: 6.514

Review 3.  Automated docking of flexible ligands: applications of AutoDock.

Authors:  D S Goodsell; G M Morris; A J Olson
Journal:  J Mol Recognit       Date:  1996 Jan-Feb       Impact factor: 2.137

4.  Torsion angle dynamics for NMR structure calculation with the new program DYANA.

Authors:  P Güntert; C Mumenthaler; K Wüthrich
Journal:  J Mol Biol       Date:  1997-10-17       Impact factor: 5.469

5.  Role of melanocortinergic neurons in feeding and the agouti obesity syndrome.

Authors:  W Fan; B A Boston; R A Kesterson; V J Hruby; R D Cone
Journal:  Nature       Date:  1997-01-09       Impact factor: 49.962

6.  Structures of the agouti signaling protein.

Authors:  Joseph C McNulty; Pilgrim J Jackson; Darren A Thompson; Biaoxin Chai; Ira Gantz; Gregory S Barsh; Philip E Dawson; Glenn L Millhauser
Journal:  J Mol Biol       Date:  2005-01-25       Impact factor: 5.469

Review 7.  Pro-opiomelanocortin processing in the hypothalamus: impact on melanocortin signalling and obesity.

Authors:  L E Pritchard; A V Turnbull; A White
Journal:  J Endocrinol       Date:  2002-03       Impact factor: 4.286

8.  The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist.

Authors:  Veli-Pekka Jaakola; Mark T Griffith; Michael A Hanson; Vadim Cherezov; Ellen Y T Chien; J Robert Lane; Adriaan P Ijzerman; Raymond C Stevens
Journal:  Science       Date:  2008-10-02       Impact factor: 47.728

Review 9.  Molecular signatures of G-protein-coupled receptors.

Authors:  A J Venkatakrishnan; Xavier Deupi; Guillaume Lebon; Christopher G Tate; Gebhard F Schertler; M Madan Babu
Journal:  Nature       Date:  2013-02-14       Impact factor: 49.962

10.  Modulation of blood pressure by central melanocortinergic pathways.

Authors:  Jerry R Greenfield; Jeffrey W Miller; Julia M Keogh; Elana Henning; Julie H Satterwhite; Gregory S Cameron; Beatrice Astruc; John P Mayer; Soren Brage; Teik Choon See; David J Lomas; Stephen O'Rahilly; I Sadaf Farooqi
Journal:  N Engl J Med       Date:  2008-12-17       Impact factor: 91.245
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  9 in total

1.  A Macrocyclic Agouti-Related Protein/[Nle4,DPhe7]α-Melanocyte Stimulating Hormone Chimeric Scaffold Produces Subnanomolar Melanocortin Receptor Ligands.

Authors:  Mark D Ericson; Katie T Freeman; Sathya M Schnell; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2017-01-17       Impact factor: 7.446

2.  Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.

Authors:  Katlyn A Fleming; Katie T Freeman; Mike D Powers; Radleigh G Santos; Ginamarie Debevec; Marc A Giulianotti; Richard A Houghten; Skye R Doering; Clemencia Pinilla; Carrie Haskell-Luevano
Journal:  J Med Chem       Date:  2019-02-28       Impact factor: 7.446

Review 3.  Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.

Authors:  Mark D Ericson; Cody J Lensing; Katlyn A Fleming; Katherine N Schlasner; Skye R Doering; Carrie Haskell-Luevano
Journal:  Biochim Biophys Acta Mol Basis Dis       Date:  2017-03-29       Impact factor: 5.187

4.  Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.

Authors:  Francesco Merlino; Yang Zhou; Minying Cai; Alfonso Carotenuto; Ali M Yousif; Diego Brancaccio; Salvatore Di Maro; Silvia Zappavigna; Antonio Limatola; Ettore Novellino; Paolo Grieco; Victor J Hruby
Journal:  J Med Chem       Date:  2018-04-25       Impact factor: 7.446

5.  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

6.  Multiresidue Tetrapeptide Substitutions Yield a 140-fold Selective Melanocortin-3 over Melanocortin-4 Receptor Agonist.

Authors:  Mark D Ericson; Romessa Shaikh; Courtney M Larson; Katie T Freeman; Carrie Haskell-Luevano
Journal:  ACS Med Chem Lett       Date:  2020-12-17       Impact factor: 4.345

7.  Demonstration of a Common DPhe7 to DNal(2')7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides.

Authors:  Luis E Gimenez; Terry A Noblin; Savannah Y Williams; Satarupa Mullick Bagchi; Ren-Lei Ji; Ya-Xiong Tao; Claus B Jeppesen; Kilian W Conde-Frieboes; Tomi K Sawyer; Paolo Grieco; Roger D Cone
Journal:  J Med Chem       Date:  2022-04-11       Impact factor: 7.446

8.  Enhanced Cationic Charge is a Key Factor in Promoting Staphylocidal Activity of α-Melanocyte Stimulating Hormone via Selective Lipid Affinity.

Authors:  Jyotsna Singh; Seema Joshi; Sana Mumtaz; Nancy Maurya; Ilora Ghosh; Shivangi Khanna; Vivek T Natarajan; Kasturi Mukhopadhyay
Journal:  Sci Rep       Date:  2016-08-16       Impact factor: 4.379

9.  DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst2,5 Receptors.

Authors:  Alessandro Pratesi; Mauro Ginanneschi; Marco Lumini; Anna M Papini; Ettore Novellino; Diego Brancaccio; Alfonso Carotenuto
Journal:  Front Chem       Date:  2017-02-23       Impact factor: 5.221
  9 in total

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