GSK4112

GSK4112 is a synthetic ligand that selectively modulates the Rev-ErbA alpha protein, a nuclear receptor involved in the regulation of circadian rhythms and metabolism. It was developed by GlaxoSmithKline, a British multinational pharmaceutical company, hence the name GSK4112.

Chemistry

GSK4112 is a small molecule that binds to the ligand-binding domain of Rev-ErbA alpha. Its chemical structure consists of a heterocyclic core, with various functional groups attached. The exact structure is proprietary information of GlaxoSmithKline.

Mechanism of Action

GSK4112 acts as an agonist for the Rev-ErbA alpha protein. When it binds to this protein, it causes a conformational change that allows the protein to bind to specific DNA sequences known as Rev-ErbA response elements. This binding represses the transcription of certain genes, altering the expression of proteins involved in circadian rhythms and metabolism.

Applications

Research into the applications of GSK4112 is ongoing. It has been suggested that it could be used to treat disorders related to circadian rhythms, such as sleep disorders, jet lag, and certain metabolic disorders. However, more research is needed to confirm these potential uses and to understand the possible side effects and risks.

Research

Several studies have been conducted to understand the effects of GSK4112. These studies have shown that it can alter the expression of genes involved in circadian rhythms and metabolism in cells and in animal models. However, these are preliminary findings, and more research is needed to fully understand the effects of GSK4112 in humans.

See Also

• Rev-ErbA alpha
• GlaxoSmithKline
• Circadian rhythm
• Metabolism