Modulators of melanocortin receptors
View Patent ↗Modulators of melanocortin receptors (MCR) are provided herein. An MC5R peptide ligand is represented by to Formula 1: R 1 -Nle 4 - c [Xaa 5 -Yaa 6 -(NMe)D-Nal(2′) 7 -Arg 8 -Trp 9 -(NMe)Zaa 10 ]-R 2 . R 1 can be an acetyl, a glycosylated amino acid, —CO—(CH 2 ) n CH 3 , or —CO—(CH 2 ) n CF 3 with n ranging from 1 to 6. R 2 can be an —CONH 2 , —COOH, or —CH 2 OH. Xaa, Yaa, and Zaa can each be a natural amino acid or an unnatural amino acid.
1. A melanocortin 5 receptor (MC5R) peptide ligand according to the formula:
R 1 -Nle 4 - c [Asp 5 -Pro 6 -(NMe)D-Nal(2′) 7 -Arg 8 -Trp 9 -(NMe)Lys 10 ]-R 2 ,
wherein R 1 is an acetyl, a glycosylated amino acid, or —CO—(CH 2 ) n CH 3 , wherein n ranges from 1 to 6, wherein R 2 is an —CONH 2 , —COOH, or —CH 2 OH, and wherein the MC5R peptide ligand is an MC5R antagonist.
2. The MC5R peptide ligand of claim 1 , wherein the glycosylated amino acid comprises a saccharide O-linked to a natural amino acid, wherein the natural amino acid is Ser, Thr, or Tyr.
3. The MC5R peptide ligand of claim 1 , wherein the glycosylated amino acid comprises a saccharide N-linked to a natural amino acid, wherein the natural amino acid is Asn or Lys.
4. A melanocortin 5 receptor (MC5R) peptide ligand according to the formula:
Ac-Nle 4 - c [Asp 5 -Pro 6 -(NMe)D-Nal(2′) 7 -Arg 8 -Trp 9 -(NMe)Lys 10 ]-NH 2 ,
wherein the MC5R peptide ligand is an MC5R antagonist.