Development of novel frog‐skin peptide scaffolds with selectivity towards melanocortin receptor subtypes
Sign Up to like & getrecommendations! Published in 2020 at "Peptide Science"
DOI: 10.1002/pep2.24209
Abstract: Melanocortin receptors are pharmaceutically important receptors that are involved in complex physiological functions. They have been associated with various diseases including obesity, erectile dysfunction, acne, and skin cancer. It has been challenging to transform nonselective… read more here.
Keywords: skin; towards melanocortin; frog skin; selectivity towards ... See more keywords
Melanocortin 5 receptor signaling pathway in health and disease
Sign Up to like & getrecommendations! Published in 2020 at "Cellular and Molecular Life Sciences"
DOI: 10.1007/s00018-020-03511-0
Abstract: Melanocortin hormone system plays a key role in maintaining the homeostasis of our body via their neuro-immune-endocrine activities and regulates a diverse array of physiological functions, including melanogenesis, inflammation, immunomodulation, adrenocortical steroidogenesis, hemodynamics, natriuresis, energy… read more here.
Keywords: disease; mc5r; melanocortin receptor; health ... See more keywords
Characterization of ligand binding to melanocortin 4 receptors using fluorescent peptides with improved kinetic properties
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Pharmacology"
DOI: 10.1016/j.ejphar.2017.01.040
Abstract: Abstract Melanocortin 4 (MC4) receptors are important drug targets as they regulate energy homeostasis, eating behaviour and sexual functions. The ligand binding process to these G protein‐coupled receptors is subject to considerable complexity. Different steps… read more here.
Keywords: ligand binding; mc4 receptors; melanocortin mc4; kinetic properties ... See more keywords
Melanocortin receptor agonists suppress experimental autoimmune uveitis.
Sign Up to like & getrecommendations! Published in 2022 at "Experimental eye research"
DOI: 10.1016/j.exer.2022.108986
Abstract: The melanocortin system plays an essential role in the regulation of immune activity. The anti-inflammatory microenvironment of the eye is dependent on the expression of the melanocortin-neuropeptide alpha-melanocyte stimulating hormone (α-MSH). In addition, the melanocortin… read more here.
Keywords: msh; melanocortin; eau mice; uveitis ... See more keywords
Regulation of melanocortin-1 receptor pharmacology by melanocortin receptor accessory protein 2 in orange-spotted grouper (Epinephelus coioides).
Sign Up to like & getrecommendations! Published in 2019 at "General and comparative endocrinology"
DOI: 10.1016/j.ygcen.2019.113291
Abstract: Melanocortin-1 receptor (MC1R) has important roles in regulating pigmentation and inflammation. Melanocortin receptor accessory protein 2 (MRAP2) modulates trafficking, ligand binding, and signaling of mammalian melanocortin receptors. However, the effect of MRAP2 on fish MC1R… read more here.
Keywords: protein; melanocortin receptor; pharmacology; receptor accessory ... See more keywords
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.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01295
Abstract: Melanocortin peptides containing a 3-(2-naphthyl)-d-alanine residue in position 7 (DNal(2')7), reported as melanocortin-3 receptor (MC3R) subtype-specific agonists in two separate publications, were found to lack significant MC3R agonist activity. The cell lines used at the… read more here.
Keywords: mischaracterization pharmacological; melanocortin peptides; systematic mischaracterization; pharmacological properties ... See more keywords
Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00238
Abstract: Understanding the functional relevance of G protein-coupled receptor (GPCR) homodimerization has been limited by the insufficient tools to assess asymmetric signaling occurring within dimers comprised of the same receptor type. We present unmatched bivalent ligands… read more here.
Keywords: arrestin recruitment; allosteric signaling; unmatched bivalent; receptor ... See more keywords
1,2,3-Triazole Rings as a Disulfide Bond Mimetic in Chimeric AGRP-Melanocortin Peptides: Design, Synthesis, and Functional Characterization.
Sign Up to like & getrecommendations! Published in 2018 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.7b00422
Abstract: The melanocortin system is involved in the regulation of complex physiological functions, including energy and weight homeostasis, feeding behavior, inflammation, sexual function, pigmentation, and exocrine gland function. The five melanocortin receptors that belong to the… read more here.
Keywords: disulfide bond; melanocortin receptors; agrp melanocortin; chimeric agrp ... See more keywords
Discovery of Melanocortin Ligands via a Double Simultaneous Substitution Strategy Based on the Ac-His-dPhe-Arg-Trp-NH2 Template.
Sign Up to like & getrecommendations! Published in 2018 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.8b00181
Abstract: The melanocortin system regulates an array of diverse physiological functions including pigmentation, feeding behavior, energy homeostasis, cardiovascular regulation, sexual function, and steroidogenesis. Endogenous melanocortin agonist ligands all possess the minimal messaging tetrapeptide sequence His-Phe-Arg-Trp. Based… read more here.
Keywords: melanocortin; double simultaneous; substitution strategy; simultaneous substitution ... See more keywords
Incorporation of Indoylated Phenylalanine Yields a Sub-Micromolar Selective Melanocortin-4 Receptor Antagonist Tetrapeptide
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c03307
Abstract: The melanocortin family is involved in many physiological functions, including pigmentation, steroidogenesis, and appetite. The centrally expressed melanocortin-3 and melanocortin-4 receptors (MC3R and MC4R) possess overlapping but distinct roles in energy homeostasis. Herein, the third… read more here.
Keywords: melanocortin; incorporation indoylated; yields sub; phenylalanine yields ... See more keywords
Identification of a novel specific small-molecule melanocortin-2-receptor antagonist
Sign Up to like & getrecommendations! Published in 2022 at "Endocrine Connections"
DOI: 10.1530/ec-22-0338
Abstract: The overproduction of adrenocorticotropic hormone (ACTH), in conditions such as Cushing’s disease and congenital adrenal hyperplasia (CAH), leads to significant morbidity. Current treatment with glucocorticoids does not adequately suppress plasma ACTH, resulting in excess adrenal… read more here.
Keywords: small molecule; acth; identification; melanocortin ... See more keywords