BMS-470539 is a
small-molecule
Within the fields of molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs ar ...
experimental drug
An experimental drug is a medicinal product (a drug or vaccine) that has not yet received approval from governmental regulatory authorities for routine use in human or veterinary medicine. A medicinal product may be approved for use in one diseas ...
which acts as a
potent and highly
selective full agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the a ...
of the
MC1 receptor.
It was discovered in 2003 as part of an effort to understand the role of the MC
1 receptor in
immunomodulation, and has since been used in
scientific research
The scientific method is an empirical method for acquiring knowledge that has characterized the development of science since at least the 17th century (with notable practitioners in previous centuries; see the article history of scientific m ...
to determine its role in
inflammatory processes.
The compound was
designed with the intention of
mimicking the central His-Phe-Arg-Trp
pharmacophore
300px, An example of a pharmacophore model.
A pharmacophore is an abstract description of molecular features that are necessary for molecular recognition of a ligand by a biological macromolecule. IUPAC defines a pharmacophore to be "an ensemble o ...
of the
melanocortin
The melanocortins are a family of neuropeptide hormones which are the ligands of the melanocortin receptorsEricson, M.D., et al., ''Bench-top to clinical therapies: A review of melanocortin ligands from 1954 to 2016.'' Biochim Biophys Acta Mol Basi ...
s,
and this proved to be successful based on its favorable
pharmacodynamic profile.
See also
*
Afamelanotide
Afamelanotide, sold under the brand name Scenesse, is a synthetic peptide and analogue of α-melanocyte stimulating hormone. It has been used to prevent skin damage from the sun in people with erythropoietic protoporphyria in the European Un ...
*
Bremelanotide
Bremelanotide, sold under the brand name Vyleesi, is a medication used to treat low sexual desire in women. Specifically it is used for low sexual desire which occurs before menopause and is not due to medical problems, psychiatric problems, or ...
*
Melanotan II
*
Modimelanotide
*
Setmelanotide
Setmelanotide, sold under the brand name Imcivree, is a medication used for the treatment of genetic obesity caused by a rare single-gene mutation.
The most common side effects include injection site reactions, skin hyperpigmentation (skin patc ...
References
Carboxamides
Anti-inflammatory agents
Imidazoles
Immunomodulating drugs
Melanocortin receptor agonists
4-Phenylpiperidines
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