FR235222, a fungal metabolite, is a novel immunosuppressant that inhibits mammalian histone deacetylase (HDAC). I. Taxonomy, fermentation, isolation and biological activities.
A cyclic tetrapeptide FR235222, a novel immunosuppressant, has been isolated from the fermentation broth of a fungus, Acremonium sp. No. 27082. FR235222 showed potent and selective inhibitory effects on both T cell proliferation and lymphokine production. Further study has revealed this compound exhibits potent inhibitory effects on the activity of mammalian histone deacetylases (HDACs).
Mori
Hiroaki
H
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2635, Japan. hiroaki_mori@po.fujisawa.co.jp
Urano
Yasuharu
Y
Abe
Fumie
F
Furukawa
Satoko
S
Furukawa
Shigetada
S
Tsurumi
Yasuhisa
Y
Sakamoto
Kazutoshi
K
Hashimoto
Michizane
M
Takase
Shigehiro
S
Hino
Motohiro
M
Fujii
Takashi
T
D000164:Acremonium / Q000737:chemistry / Q000145:classification / Q000276:immunology / Q000378:metabolism*; D000818:Animals; D004791:Enzyme Inhibitors / Q000276:immunology / Q000302:isolation & purification* / Q000494:pharmacology; D005260:Female; D005285:Fermentation; D022781:Hepatocytes / Q000187:drug effects / Q000276:immunology; D056572:Histone Deacetylase Inhibitors; D007166:Immunosuppressive Agents / Q000276:immunology / Q000302:isolation & purification* / Q000494:pharmacology; D007376:Interleukin-2 / Q000276:immunology / Q000378:metabolism; D015847:Interleukin-4 / Q000276:immunology / Q000378:metabolism; D008213:Lymphocyte Activation / Q000187:drug effects / Q000276:immunology; D007959:Lymphocyte Culture Test, Mixed; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D008819:Mice, Nude; D010456:Peptides, Cyclic / Q000276:immunology / Q000302:isolation & purification* / Q000494:pharmacology; D051381:Rats; D012988:Soil Microbiology; D013601:T-Lymphocytes / Q000166:cytology / Q000187:drug effects / Q000276:immunology
D004791:Enzyme Inhibitors; C474179:FR 235222; D056572:Histone Deacetylase Inhibitors; D007166:Immunosuppressive Agents; D007376:Interleukin-2; D010456:Peptides, Cyclic; D015847:Interleukin-4