Melanocortin Receptor Binding Conjugates
The present invention relates to melanocortin receptor binding conjugates and methods of making and using the foregoing.
1 . A method of modulating a biological activity of a melanocortin receptor, comprising contacting an alpha-MSH derivative-Fc conjugate with the melanocortin receptor, wherein the alpha-MSH derivative has a structure shown in Forumula X (SEQ ID NO: 18) and the alpha-MSH derivative is coupled to the Fc via a hydrazine linker.
2 . The method of claim 1 , wherein the melanocortin receptor is a melanocortin 1 receptor (MC1R), a melanocortin 3 receptor (MC3R), a melanocortin 4 receptor (MC4R) or a melanocortin 5 receptor (MC5R).
3 . A method of modulating a melanocortin receptor-mediated condition comprising administering an alpha-MSH derivative-Fc conjugate to a patient in need thereof, wherein the alpha-MSH derivative has a structure shown in Forumula X (SEQ ID NO: 18) and the alpha-MSH derivative is coupled to the Fc via a hydrazine linker.
4 . The method of claim 3 , wherein the melanocortin receptor mediated condition is obesity or type II diabetes.
5 . The method of claim 3 , wherein the melanocortin receptor mediated condition is male erectile dysfunction, female sexual dysfunction, an inflammatory condition or fibrosis.
6 . The method of claim 5 , wherein the inflammatory condition is allergic inflammation, gouty arthritis, rheumatoid arthritis, inflammatory bowel disease, post-ischemia renal injury, liver inflammation, ischemic brain damage or peripheral neuropathies.