Overview
- Arai, T. et al. (1962) J. Antibiot. (Tokyo) 15, 231.
- Morisaki, M. and Arai, T. (1992) J. Antibiot. (Tokyo) 45, 126.
- Meadows, R.P. et al. (1993) Biochemistry 32, 754.
Alomone Labs Ascomycin inhibits the proliferation of Jurkat cells.Cells were treated with different concentrations of Ascomycin (#A-800) for 4 days. The number of living cells was measured by XTT and normalized to the control (100%) and plotted against the drug concentration.
- Arai, T. et al. (1962) J. Antibiot. (Tokyo) 15, 231.
- Morisaki, M. and Arai, T. (1992) J. Antibiot. (Tokyo) 45, 126.
- Meadows, R.P. et al. (1993) Biochemistry 32, 754.
- Kawai, M. et al. (1998) Bioorg. Med. Chem. Lett. 8, 935.
- Plath, K.E. et al. (2003) Clin. Exp. Allergy 33, 342.
- Paul, C. et al. (2000) Expert Opin. Investig. Drugs 9, 69.
- Griffiths, C.E. (2001) Br. J. Dermatol. 144, 679.
- Wellington, K. and Jarvis, B. (2002) Drugs 62, 817.
- Quatresooz, P. et al. (2003) Rev. Med. Liege 58, 168.
Ascomycin (FK520) is a structurally complex macrolide with immunosuppressant activity. It is an ethyl analog of the known immune suppressant FK506 (Tacrolimus).1,2 Ascomycin acts by binding to a class of cytosolic proteins, the immunophilins, especially macrophilin-12 (FKBP-12). The immunophilin-FK520 complex inhibits calcineurin, a type 2B phosphatase (PP2B).3
Ascomycin suppresses the production of Th1 and Th2 cytokines in T lymphocytes, and preferentially inhibits the activation of mast cells (principal cells of the allergic response).4 In human basophils, it potently inhibited anti-IgE-induced histamine and cytokine release, and reduced IgE-dependent p38 MAPK activation.5 It seems that Ascomycin inhibits basophil degranulation at the initial phase of allergic skin reactions.6,7 Ascomycin derivatives are currently developed for the clinical treatment of dermatological diseases.8,9
Ascomycin (#A-800) is a highly pure, natural, and biologically active compound.
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