[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

Holder et al., 2002 - Google Patents

Structure− activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors: part 2 modifications at the Phe …

Holder et al., 2002

Document ID
5452630784870161972
Author
Holder J
Bauzo R
Xiang Z
Haskell-Luevano C
Publication year
Publication venue
Journal of medicinal chemistry

External Links

Snippet

The melanocortin pathway is an important participant in skin pigmentation, steroidogenesis, obesity, energy homeostasis and exocrine gland function. The centrally located melanocortin-3 and melanocortin-4 receptors (MC3R, MC4R) are involved in the metabolic …
Continue reading at pubs.acs.org (other versions)

Classifications

    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
    • G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/502—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing non-proliferative effects
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4702—Regulators; Modulating activity
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • C07K14/68—Melanocyte-stimulating hormone [MSH]
    • C07K14/685—Melanocyte-stimulating hormone [MSH] alpha-Melanotropin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by the preceding groups
    • G01N33/48—Investigating or analysing materials by specific methods not covered by the preceding groups biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/50—Cyclic peptides containing at least one abnormal peptide link
    • C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
    • C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid

Similar Documents

Publication Publication Date Title
Holder et al. Structure− activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors: part 2 modifications at the Phe position
Haskell-Luevano et al. Structure activity studies of the melanocortin-4 receptor by in vitro mutagenesis: identification of agouti-related protein (AGRP), melanocortin agonist and synthetic peptide antagonist interaction determinants
Holder et al. Structure− Activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors. 1. Modifications at the his position
Haskell-Luevano et al. Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors
Holder et al. Structure− activity relationships of the melanocortin tetrapeptide Ac-His-d-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position
Haskell-Luevano et al. Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R
Grieco et al. D-amino acid scan of γ-melanocyte-stimulating hormone: Importance of Trp8 on human MC3 receptor selectivity
Wilczynski et al. Identification of putative agouti-related protein (87− 132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands
Testa et al. 1, 4-disubstituted-[1, 2, 3] triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity
US11332499B2 (en) Cyclic peptides and methods of use thereof
Ericson et al. 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
Cai et al. Novel 3D pharmacophore of α-MSH/γ-MSH hybrids leads to selective human MC1R and MC3R analogues
Holder et al. Structure–activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 at the mouse melanocortin receptors: Part 3: modifications at the Arg position
Tala et al. 1, 2, 3-Triazole rings as a disulfide bond mimetic in chimeric AGRP-melanocortin peptides: design, synthesis, and functional characterization
US20210179666A1 (en) Cyclic peptides and methods of use thereof
Zhou et al. Design of MC1R selective γ-MSH analogues with canonical amino acids leads to potency and pigmentation
Xiang et al. Peptide and small molecules rescue the functional activity and agonist potency of dysfunctional human melanocortin-4 receptor polymorphisms
Holder et al. Characterization of aliphatic, cyclic, and aromatic N-terminally “capped” His-D-Phe-Arg-Trp-NH2 tetrapeptides at the melanocortin receptors
Ericson et al. Structure–Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at the Melanocortin-5 Receptor
Fleming et al. 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
Koikov et al. Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH2
Doering et al. 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
Ericson et al. A macrocyclic agouti-related protein/[Nle4, DPhe7] α-melanocyte stimulating hormone chimeric scaffold produces subnanomolar melanocortin receptor ligands
Todorovic et al. N-terminal fatty acylated His-DPhe-Arg-Trp-NH2 tetrapeptides: Influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes
Fleming et al. 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