Novel modulators of melanocortin receptors
AssigneeArizona Board of Regents on Behalf of the University of Arizona
InventorsVictor J. Hruby, Minying Cai
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Abstract
Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2′)7-Arg8-Trp9-(NMe)Zaa10]-R2. R1 can be an acetyl, a glycosylated amino acid, —CO—(CH2)nCH3, or —CO—(CH2)nCF3 with n ranging from 1 to 6. R2 can be an —CONH2, —COON, or —CH2OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.
Claims9
A melanocortin 5 receptor (MC5R) peptide ligand according to Formula 1:
- R1-Nle4-c[Xaa5-Yaa6-(NMe)D-Nal(2′)7-Arg8-Trp9-(NMe)Zaa10]—R2,
- wherein R1 is an acetyl, a glycosylated amino acid, or —CO—(CH2)nCH3, wherein n ranges from 1 to 6, wherein R2 is an —CONH2, —COOH, or —CH2OH,
- wherein Xaa is Asp, Glu or Abu, wherein Yaa is Pro, Oic, Ioc, Tic, Cpe, Che, Aic, or Acpc, wherein Zaa is Lys, Orn, or Dab, and
- wherein the MC5R peptide ligand binds to MC5R.
A melanocortin 5 receptor (MC5R) peptide ligand according to the formula:
- R1-Nle4-c[Asp5-Pro6-(NMe)D-Nal(2′)7-Arg8-Trp9-(NMe)Lys10]-R2,
- wherein R1 is an acetyl, a glycosylated amino acid, or —CO—(CH2)nCH3, wherein n ranges from 1 to 6, wherein R2 is an —CONH2, —COOH, or —CH2OH, and wherein the MC5R peptide ligand binds to MC5R.
A melanocortin 5 receptor (MC5R) peptide ligand according to the formula:
- Ac-Nle4-c[Asp5-Pro6-(NMe)D-Nal(2′)7-Arg8-Trp9-(NMe)Lys10]-NH2,
- wherein the MC5R peptide ligand binds to MC5R.
Dependencies are inferred from the claim text.