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1.
The Parallel Structure-Activity Relationship Screening of Three Compounds Identifies the Common Agonist Pharmacophore of Pyrrolidine Bis-Cyclic Guanidine Melanocortin-3 Receptor (MC3R) Small-Molecule Ligands.
Int J Mol Sci
; 24(12)2023 Jun 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-37373293
2.
Structureâ»Activity Relationships of the Tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 at the Mouse Melanocortin Receptors: Modification at the (pI)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands.
Molecules
; 24(8)2019 Apr 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-31013889
3.
A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.
Bioorg Med Chem Lett
; 25(22): 5306-8, 2015 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26433448
4.
Incorporation of Three Extracyclic Arginine Residues into a Melanocortin Macrocyclic Agonist (c[Pro-His-DPhe-Arg-Trp-Dap-Lys(Arg-Arg-Arg-Ac)-DPro]) Decreases Food Intake When Administered Intrathecally or Subcutaneously Compared to a Macrocyclic Ligand Lacking Extracyclic Arginine Residues (c[Pro-His-DPhe-Arg-Trp-Dap-Ala-DPro)].
ACS Pharmacol Transl Sci
; 7(4): 1114-1125, 2024 Apr 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-38633589
5.
Neuroplasticity of sensory and sympathetic nerve fibers in a mouse model of a painful arthritic joint.
Arthritis Rheum
; 64(7): 2223-32, 2012 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-22246649
6.
Discovery of a Pan-Melanocortin Receptor Antagonist [Ac-DPhe(pI)-Arg-Nal(2')-Orn-NH2] at the MC1R, MC3R, MC4R, and MC5R that Mediates an Increased Feeding Response in Mice and a 40-Fold Selective MC1R Antagonist [Ac-DPhe(pI)-DArg-Nal(2')-Arg-NH2].
J Med Chem
; 66(12): 8103-8117, 2023 06 22.
Artículo
en Inglés
| MEDLINE | ID: mdl-37307241
7.
Incorporation of Indoylated Phenylalanine Yields a Sub-Micromolar Selective Melanocortin-4 Receptor Antagonist Tetrapeptide.
ACS Omega
; 7(31): 27656-27663, 2022 Aug 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-35967074
8.
Pathological sprouting of adult nociceptors in chronic prostate cancer-induced bone pain.
J Neurosci
; 30(44): 14649-56, 2010 Nov 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-21048122
9.
Multiresidue Tetrapeptide Substitutions Yield a 140-fold Selective Melanocortin-3 over Melanocortin-4 Receptor Agonist.
ACS Med Chem Lett
; 12(1): 115-120, 2021 Jan 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-33488972
10.
Discovery of Molecular Interactions of the Human Melanocortin-4 Receptor (hMC4R) Asp189 (D189) Amino Acid with the Endogenous G-Protein-Coupled Receptor (GPCR) Antagonist Agouti-Related Protein (AGRP) Provides Insights to AGRP's Inverse Agonist Pharmacology at the hMC4R.
ACS Chem Neurosci
; 12(3): 542-556, 2021 02 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-33470098
11.
Development of hMC1R Selective Small Agonists for Sunless Tanning and Prevention of Genotoxicity of UV in Melanocytes.
J Invest Dermatol
; 141(7): 1819-1829, 2021 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-33609553
12.
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.
J Med Chem
; 64(19): 14860-14875, 2021 10 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-34592820
13.
Administration of a tropomyosin receptor kinase inhibitor attenuates sarcoma-induced nerve sprouting, neuroma formation and bone cancer pain.
Mol Pain
; 6: 87, 2010 Dec 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-21138586
14.
Peptoid NPhe4 in AGRP-Based c[Pro1-Arg2-Phe3-Phe4-Xxx5-Ala6-Phe7-DPro8] Scaffolds Maintain Mouse MC4R Antagonist Potency.
ACS Med Chem Lett
; 11(10): 1942-1948, 2020 Oct 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-33062177
15.
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
ACS Med Chem Lett
; 11(3): 272-277, 2020 Mar 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-32184956
16.
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.
J Med Chem
; 63(5): 2194-2208, 2020 03 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-31845801
17.
Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over ß-Arrestin 2 Recruitment) Within the Melanocortin Receptors.
J Med Chem
; 62(1): 144-158, 2019 01 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-29669202
18.
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.
J Med Chem
; 62(5): 2738-2749, 2019 03 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-30741545
19.
A fracture pain model in the rat: adaptation of a closed femur fracture model to study skeletal pain.
Anesthesiology
; 108(3): 473-83, 2008 Mar.
Artículo
en Inglés
| MEDLINE | ID: mdl-18292685
20.
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.
J Med Chem
; 61(17): 7729-7740, 2018 09 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-30035543