Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin recep
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Novel binding motif of ACTH analogues at the melanocortin receptorsDesign, synthesis and biological evaluation of ligands selective for the melanocortin-3 receptorInteractions of human melanocortin 4 receptor with nonpeptide and peptide agonistsStructure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptorFurther structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 560 YEARS OF POMC: Regulation of feeding and energy homeostasis by α-MSHBoth MC1 and MC3 Receptors Provide Protection From Cerebral Ischemia-Reperfusion-Induced Neutrophil Recruitment.Molecular determinants of human melanocortin-4 receptor responsible for antagonist SHU9119 selective activityActivation of central melanocortin receptors by MT-II increases cavernosal pressure in rabbits by the neuronal release of NOMagel2 is required for leptin-mediated depolarization of POMC neurons in the hypothalamic arcuate nucleus in miceMelanocortin receptor 4 deficiency affects body weight regulation, grooming behavior, and substrate preference in the ratDevelopment of a high throughput screen for allosteric modulators of melanocortin-4 receptor signaling using a real time cAMP assay.Solution structures of cyclic melanocortin agonists and antagonists by NMR.New melanocortin 1 receptor binding motif based on the C-terminal sequence of alpha-melanocyte-stimulating hormone.Cell signaling and trafficking of human melanocortin receptors in real time using two-photon fluorescence and confocal laser microscopy: differentiation of agonists and antagonists.Conformational study on cyclic melanocortin ligands and new insight into their binding mode at the MC4 receptor.Integrated control of appetite and fat metabolism by the leptin-proopiomelanocortin pathway.Effect of serotonergic anorectics on food intake and induction of Fos in brain of mice with disruption of melanocortin 3 and/or 4 receptorsDesign and synthesis of trivalent ligands targeting opioid, cholecystokinin, and melanocortin receptors for the treatment of pain.Multinodal regulation of the arcuate/paraventricular nucleus circuit by leptin.Solid-phase peptide head-to-side chain cyclodimerization: discovery of C(2)-symmetric cyclic lactam hybrid α-melanocyte-stimulating hormone (MSH)/agouti-signaling protein (ASIP) analogues with potent activities at the human melanocortin receptorsOrganic chemistry and biology: chemical biology through the eyes of collaboration.Synthesis and evaluation of bivalent ligands for binding to the human melanocortin-4 receptor.Structure-activity studies of new melanocortin peptides containing an aromatic amino acid at the N-terminal position.Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.Interactions of the melanocortin-4 receptor with the peptide agonist NDP-MSH.Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R AntagonistIdentification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).The role of the central melanocortin system in the regulation of food intake and energy homeostasis: lessons from mouse models.Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptorsDesign, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptorEmerging antiobesity drugs.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.Gamma-MSH, sodium metabolism, and salt-sensitive hypertension.Design of cyclic and other templates for potent and selective peptide alpha-MSH analogues.Effects of macrocycle size and rigidity on melanocortin receptor-1 and -5 selectivity in cyclic lactam alpha-melanocyte-stimulating hormone analogs.The melanocortin-4 receptor: physiology, pharmacology, and pathophysiology.Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.Melanotropins as drugs for the treatment of obesity and other feeding disorders: potential and problems.Approaches to the rational design of selective melanocortin receptor antagonists.
P2860
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P2860
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin recep
description
1995 nî lūn-bûn
@nan
1995年の論文
@ja
1995年学术文章
@wuu
1995年学术文章
@zh-cn
1995年学术文章
@zh-hans
1995年学术文章
@zh-my
1995年学术文章
@zh-sg
1995年學術文章
@yue
1995年學術文章
@zh
1995年學術文章
@zh-hant
name
Cyclic lactam alpha-melanotrop ...... at specific melanocortin recep
@en
type
label
Cyclic lactam alpha-melanotrop ...... at specific melanocortin recep
@en
prefLabel
Cyclic lactam alpha-melanotrop ...... at specific melanocortin recep
@en
P2093
P356
P1476
Cyclic lactam alpha-melanotrop ...... at specific melanocortin recep
@en
P2093
Castrucci AL
Kesterson RA
al-Obeidi FA
P304
P356
10.1021/JM00018A005
P407
P577
1995-09-01T00:00:00Z