Chaetochromin, also known as 4548-G05, is an orally active, small-molecule, selective

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

of the

insulin receptor The insulin receptor (IR) is a transmembrane receptor that is activated by insulin, IGF-I, IGF-II and belongs to the large class of receptor tyrosine kinase. Metabolically, the insulin receptor plays a key role in the regulation of glucose h ...

. It has potent and long-lasting

antidiabetic Drugs used in diabetes treat types of diabetes mellitus by decreasing glucose levels in the blood. With the exception of insulin, most GLP-1 receptor agonists ( liraglutide, exenatide, and others), and pramlintide, all diabetes medications a ...

activity ''

in vivo Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, an ...

'' in mice. The drug may represent a novel potential therapeutic agent for the treatment of

diabetes Diabetes mellitus, commonly known as diabetes, is a group of common endocrine diseases characterized by sustained high blood sugar levels. Diabetes is due to either the pancreas not producing enough of the hormone insulin, or the cells of th ...

which is more convenient and tolerable to administer than injected

insulin Insulin (, from Latin ''insula'', 'island') is a peptide hormone produced by beta cells of the pancreatic islets encoded in humans by the insulin (''INS)'' gene. It is the main Anabolism, anabolic hormone of the body. It regulates the metabol ...

. It was discovered in 1981 in ''

Chaetomium ''Chaetomium'' is a genus of fungi in the Chaetomiaceae family. It is a dematiaceous (dark-walled) Mold (fungus), mold normally found in soil, air, cellulose and plant debris. According to the ''Dictionary of the Fungi'' (10th edition, 2008), th ...

gracile'' fungi, and its interaction with the insulin receptor was identified in 2014.

Stereochemistry

Chaetochromin A and B are

stereoisomer In stereochemistry, stereoisomerism, or spatial isomerism, is a form of isomerism in which molecules have the same molecular formula and sequence of bonded atoms (constitution), but differ in the three-dimensional orientations of their atoms in ...

s of this structure, while chaetochromin C and D are related but different compounds. It is not known whether the insulin mimetic effect was found in chaetochromin A or B, or in a mixture.

References

{{Reflist Polyphenols Benzochromenes Diketones Heterocyclic compounds with 3 rings Insulin receptor agonists 3-Hydroxypropenals Resorcinols Biphenyls

Stereochemistry

See also

References