Antascomicins A, B, C, D and E. Novel FKBP12 binding compounds from a Micromonospora strain.
5 novel ascomycin-like compounds, antascomicins A, B, C, D and E were isolated from a strain of Micromonospora. The antascomicins bind strongly to the FK506-binding protein FKBP12 and antagonize the immunosuppressive activity of FK506 and rapamycin. The strain description, fermentation, structure elucidation and biological activity of these compounds are described.
Fehr
T
T
Sandoz Pharma Ltd., Basel, Switzerland.
Sanglier
J J
JJ
Schuler
W
W
Gschwind
L
L
Ponelle
M
M
Schilling
W
W
Wioland
C
C
D000818:Animals; D000900:Anti-Bacterial Agents / Q000037:antagonists & inhibitors; D002352:Carrier Proteins / Q000378:metabolism*; D002417:Cattle; D004268:DNA-Binding Proteins / Q000378:metabolism*; D006360:Heat-Shock Proteins / Q000378:metabolism*; D006801:Humans; D007166:Immunosuppressive Agents / Q000037:antagonists & inhibitors; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008847:Micromonospora / Q000378:metabolism*; D015394:Molecular Structure; D011090:Polyenes / Q000037:antagonists & inhibitors / Q000494:pharmacology; D020123:Sirolimus; D016559:Tacrolimus / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D022021:Tacrolimus Binding Proteins
D000900:Anti-Bacterial Agents; D002352:Carrier Proteins; D004268:DNA-Binding Proteins; D006360:Heat-Shock Proteins; D007166:Immunosuppressive Agents; D011090:Polyenes; C099294:antascomicin A; C099295:antascomicin B; C099296:antascomicin C; C099297:antascomicin D; C099298:antascomicin E; D022021:Tacrolimus Binding Proteins; D020123:Sirolimus; D016559:Tacrolimus