FR901483, a novel immunosuppressant isolated from Cladobotryum sp. No. 11231. Taxonomy of the producing organism, fermentation, isolation, physico-chemical properties and biological activities.
FR901483, a novel immunosuppressant, has been isolated from the fermentation broth of Cladobotryum sp. No. 11231. The molecular formula of FR901483 has been determined as C20H31N2O6P. FR901483 exerts a potent immunosuppressive activity in vitro and significantly prolongs graft survival time in the rat skin allograft model. This compound has an intriguing tricyclic structure possessing a phosphate ester in its molecule. The ester residue may play an important role in exerting immunosuppressive activity because the desphosphoryl compound is devoid of activity. It is thought that the primary target of immunosuppression by this compound is inhibition of purine nucleotide biosynthesis.
Sakamoto
K
K
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd, Ibaraki 300-26, Japan.
Tsujii
E
E
Abe
F
F
Nakanishi
T
T
Yamashita
M
M
Shigematsu
N
N
Izumi
S
S
Okuhara
M
M
D000818:Animals; D005285:Fermentation; D007166:Immunosuppressive Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D008213:Lymphocyte Activation / Q000187:drug effects; D051379:Mice; D008807:Mice, Inbred BALB C; D003904:Mitosporic Fungi / Q000145:classification* / Q000378:metabolism; D009943:Organophosphorus Compounds / Q000302:isolation & purification*; D051381:Rats; D011916:Rats, Inbred F344; D011917:Rats, Inbred Lew
C098358:FR 901483; D007166:Immunosuppressive Agents; D009943:Organophosphorus Compounds