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Macrolide lactams

Compounds that are analog of macrolides that contain lactam rings in place of lactone rings; they are a class of antibiotics. Lactam rings are nitrogen analogs of lactone rings.

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AdipoGen FK-506 Tacrolimus
SDP

Chemical. CAS 109581-93-3. Formula C44H69NO12 . H2O. MW 804.0 . 18.0. Isolated from Streptomyces FCZ0311. Potent immunosuppressant as cyclosporin A and rapamycin. Suppresses proliferation of cytotoxic T cells and inhibits the production of T cell-derived mediators such as interleukin-2 IL-2. Forms a complex with FK-506 binding protein 12 FKBP12. Inhibits the activity of the calcium/calmodulin-dependent protein phosphatase 2B PP2B calcineurin, leading to disruption of T cell activation. Prevents rejection of transplanted organs. Anti-inflammatory compound in the treatment of several inflammatory skin diseases e.g. atopic dermatitis and with potential anti-rheumatic activity rheumatoid arthritis. Neuroprotective. Regulates nitric oxide neurotoxicity. Neurotransmitter. Ca2 release compound. NF-kappaB suppressor by induction of unfolded protein response UPR. Anti-cancer compound. Apoptosis inducer.

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