FK1012

FK1012 is a synthetic derivative of the immunosuppressive drug Tacrolimus. It is a dimeric form of Tacrolimus and is used in scientific research, particularly in the study of protein-protein interactions.

Chemistry

FK1012 is a dimeric form of Tacrolimus, which is a macrolide immunosuppressant produced by the bacterium Streptomyces tsukubaensis. The dimeric form is created by linking two molecules of Tacrolimus via a non-hydrolysable ether bond. This modification increases the molecular weight of the compound and alters its pharmacological properties.

Pharmacology

FK1012 has been used in scientific research to study protein-protein interactions. It has been particularly useful in the study of calcineurin, a protein phosphatase involved in T-cell activation. FK1012 has been shown to bind to the immunophilin FKBP12, and this complex then binds to calcineurin, inhibiting its activity. This mechanism of action is similar to that of Tacrolimus, but FK1012 has a higher affinity for FKBP12 and a more potent inhibitory effect on calcineurin.

Clinical Use

While FK1012 itself is not used clinically, its parent compound Tacrolimus is widely used in the prevention of organ transplant rejection. The study of FK1012 has contributed to our understanding of the mechanism of action of Tacrolimus and other immunosuppressive drugs.

See Also

• Tacrolimus
• Calcineurin
• Immunosuppressive drug
• Protein-protein interaction