Ascomycin, also called Immunomycin, FR-900520, FK520, is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. It has been researched for the treatment of autoimmune diseases and skin diseases, and to prevent rejection after an organ transplant.[1]
Ascomycin acts by binding to immunophilins, especially macrophilin-12. It appears that Ascomycin inhibits the production of Th1 (interferon- and IL-2) and Th2 (IL-4 and IL-10) cytokines. Additionally, ascomycin preferentially inhibits the activation of mast cells, an important cellular component of the atopic response. Ascomycin produces a more selective immunomodulatory effect in that it inhibits the elicitation phase of allergic contact dermatitis but does not impair the primary immune response when administered systemically.[2]
Ascomycin is produced by the fermentation of certain strains of Streptomyces hygroscopicus.[3]
In fiction
Ascomycin is also the name of a fictional "antiagathic" (anti-aging) drug in James Blish's future history Cities in Flight.[4] and in its component novel They Shall Have Stars.
Related compounds
References
- ^ Andexer JN, Kendrew SG, Nur-e-Alam M, Lazos O, Foster TA, Zimmermann AS, et al. (March 2011). "Biosynthesis of the immunosuppressants FK506, FK520, and rapamycin involves a previously undescribed family of enzymes acting on chorismate". Proceedings of the National Academy of Sciences of the United States of America. 108 (12): 4776–4781. doi:10.1073/pnas.1015773108. PMC 3064383. PMID 21383123.
- ^ Paul C, Graeber M, Stuetz A (January 2000). "Ascomycins: promising agents for the treatment of inflammatory skin diseases". Expert Opinion on Investigational Drugs. 9 (1): 69–77. doi:10.1517/13543784.9.1.69. PMID 11060661. S2CID 19730971.
- ^ Yu Z, Lv H, Wu Y, Wei T, Yang S, Ju D, Chen S (December 2019). "Enhancement of FK520 production in Streptomyces hygroscopicus by combining traditional mutagenesis with metabolic engineering". Applied Microbiology and Biotechnology. 103 (23–24): 9593–9606. doi:10.1007/s00253-019-10192-8. PMID 31713669. S2CID 207955563.
- ^ "Anti-agathic drugs". Technovelgy.com. Retrieved 15 June 2022.
Further reading
- Griffiths CE (April 2001). "Ascomycin: an advance in the management of atopic dermatitis". The British Journal of Dermatology. 144 (4): 679–681. doi:10.1046/j.1365-2133.2001.144004679.x. PMID 11298524. S2CID 46503687.
- Kawai M, Lane BC, Hsieh GC, Mollison KW, Carter GW, Luly JR (January 1993). "Structure-activity profiles of macrolactam immunosuppressant FK-506 analogues". FEBS Letters. 316 (2): 107–113. doi:10.1016/0014-5793(93)81196-7. PMID 7678400. S2CID 24298979.
- Zuberbier T, Chong SU, Grunow K, Guhl S, Welker P, Grassberger M, Henz BM (August 2001). "The ascomycin macrolactam pimecrolimus (Elidel, SDZ ASM 981) is a potent inhibitor of mediator release from human dermal mast cells and peripheral blood basophils". The Journal of Allergy and Clinical Immunology. 108 (2): 275–280. doi:10.1067/mai.2001.116865. PMID 11496246.
- Mollison KW, Fey TA, Krause RA, Thomas VA, Mehta AP, Luly JR (June 1993). "Comparison of FK-506, rapamycin, ascomycin, and cyclosporine in mouse models of host-versus-graft disease and heterotopic heart transplantation". Annals of the New York Academy of Sciences. 685: 55–57. doi:10.1111/j.1749-6632.1993.tb35851.x. PMID 7689812. S2CID 28990806.
- Paul C, Graeber M, Stuetz A (January 2000). "Ascomycins: promising agents for the treatment of inflammatory skin diseases". Expert Opinion on Investigational Drugs. 9 (1): 69–77. doi:10.1517/13543784.9.1.69. PMID 11060661. S2CID 19730971.
External links
- Exciting New Eczema Treatment Expected This Year By Jane Schwanke, WebMD Medical News March 17, 2000 (San Francisco)
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