Ascomycin Explained
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
Tacrolimus, Pimecrolimus
Further reading
- Griffiths CE . Ascomycin: an advance in the management of atopic dermatitis . The British Journal of Dermatology . 144 . 4 . 679–681 . April 2001 . 11298524 . 10.1046/j.1365-2133.2001.144004679.x . 46503687 .
- Kawai M, Lane BC, Hsieh GC, Mollison KW, Carter GW, Luly JR . Structure-activity profiles of macrolactam immunosuppressant FK-506 analogues . FEBS Letters . 316 . 2 . 107–113 . January 1993 . 7678400 . 10.1016/0014-5793(93)81196-7 . 24298979 . free .
- Zuberbier T, Chong SU, Grunow K, Guhl S, Welker P, Grassberger M, Henz BM . 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 . August 2001 . 11496246 . 10.1067/mai.2001.116865 . free .
- Mollison KW, Fey TA, Krause RA, Thomas VA, Mehta AP, Luly JR . 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 . June 1993 . 7689812 . 10.1111/j.1749-6632.1993.tb35851.x . 28990806 .
- Paul C, Graeber M, Stuetz A . Ascomycins: promising agents for the treatment of inflammatory skin diseases . Expert Opinion on Investigational Drugs . 9 . 1 . 69–77 . January 2000 . 11060661 . 10.1517/13543784.9.1.69 . 19730971 .
External links
Notes and References
- Andexer JN, Kendrew SG, Nur-e-Alam M, Lazos O, Foster TA, Zimmermann AS, Warneck TD, Suthar D, Coates NJ, Koehn FE, Skotnicki JS, Carter GT, Gregory MA, Martin CJ, Moss SJ, Leadlay PF, Wilkinson B . 6 . 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 . March 2011 . 21383123 . 3064383 . 10.1073/pnas.1015773108 . free .
- Paul C, Graeber M, Stuetz A . Ascomycins: promising agents for the treatment of inflammatory skin diseases . Expert Opinion on Investigational Drugs . 9 . 1 . 69–77 . January 2000 . 11060661 . 10.1517/13543784.9.1.69 . 19730971 .
- Yu Z, Lv H, Wu Y, Wei T, Yang S, Ju D, Chen S . Enhancement of FK520 production in Streptomyces hygroscopicus by combining traditional mutagenesis with metabolic engineering . Applied Microbiology and Biotechnology . 103 . 23-24 . 9593–9606 . December 2019 . 31713669 . 10.1007/s00253-019-10192-8 . 207955563 .
- Web site: Anti-agathic drugs . Technovelgy.com . 15 June 2022.
