Dibefurin, a novel fungal metabolite inhibiting calcineurin phosphatase activity

被引:11
作者
Brill, GM
Premachandran, U
Karwowski, JP
Henry, R
Cwik, DK
Traphagen, LM
Humphrey, PE
Jackson, M
Clement, JJ
Burres, NS
Kadam, S
Chen, RH
McAlpine, JB
机构
[1] New Lead Discovery, Pharmaceutical Prod. R. and D., Abbott Laboratories, Abbott Park
关键词
LYMPHOCYTE;
D O I
10.7164/antibiotics.49.124
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
The novel calcineurin inhibitor, dibefurin, has been isolated from the fungal culture AB 1650I-759. The isolation was bioactivity-directed fractionation using an assay which measures the phosphatase activity of calcineurin. The compound was purified by countercurrent, reverse phase and gel filtration chromatographies. Several studies, including crystallographic, NMR and MS, revealed that dibefurin is a novel dimeric compound of a unique structural type.
引用
收藏
页码:124 / 128
页数:5
相关论文
共 9 条
  • [1] SIMPLE AROMATICS IDENTIFIED WITH A NFAT-LACZ TRANSCRIPTION ASSAY FOR THE DETECTION OF IMMUNOSUPPRESSANTS
    BURRES, NS
    PREMACHANDRAN, U
    HOSELTON, S
    CWIK, D
    HOCHLOWSKI, JE
    YE, QM
    SUNGA, GN
    KARWOWSKI, JP
    JACKSON, M
    WHITTERN, DN
    MCALPINE, JB
    [J]. JOURNAL OF ANTIBIOTICS, 1995, 48 (05) : 380 - 386
  • [2] IDENTIFICATION OF CALCINEURIN AS A KEY SIGNALING ENZYME IN LYMPHOCYTE-T ACTIVATION
    CLIPSTONE, NA
    CRABTREE, GR
    [J]. NATURE, 1992, 357 (6380) : 695 - 697
  • [3] CLIPSTONE NA, 1993, ANN NY ACAD SCI, V696, P20
  • [4] ASPERLICIN, A NOVEL NON-PEPTIDAL CHOLECYSTOKININ ANTAGONIST FROM ASPERGILLUS-ALLIACEUS - FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES
    GOETZ, MA
    LOPEZ, M
    MONAGHAN, RL
    CHANG, RSL
    LOTTI, VJ
    CHEN, TB
    [J]. JOURNAL OF ANTIBIOTICS, 1985, 38 (12) : 1633 - 1637
  • [5] ASELACINS, NOVEL COMPOUNDS THAT INHIBIT BINDING OF ENDOTHELIN TO ITS RECEPTOR .1. THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL-ACTIVITY
    JACKSON, M
    BURRES, NS
    KARWOWSKI, JP
    ALDER, LA
    HUMPHREY, PE
    KOHL, WL
    MCALPINE, JB
    [J]. JOURNAL OF ANTIBIOTICS, 1994, 47 (05) : 523 - 527
  • [6] MLR-52, (4'-DEMETHYLAMINO-4',5'-DIHYDROXYSTAUROSPORINE), A NEW INHIBITOR OF PROTEIN-KINASE-C WITH IMMUNOSUPPRESSIVE ACTIVITY
    MCALPINE, JB
    KARWOWSKI, JP
    JACKSON, M
    MULLALLY, MM
    HOCHLOWSKI, JE
    PREMACHANDRAN, U
    BURRES, NS
    [J]. JOURNAL OF ANTIBIOTICS, 1994, 47 (03) : 281 - 288
  • [7] MILLER MW, 1961, PFIZER HDB MICROBIAL, P185
  • [9] OBSERVATIONS ON THE MECHANISM OF ACTION OF FK-506 - A PHARMACOLOGICAL PROBE OF LYMPHOCYTE SIGNAL TRANSDUCTION
    SIGAL, NH
    SIEKIERKA, JJ
    DUMONT, FJ
    [J]. BIOCHEMICAL PHARMACOLOGY, 1990, 40 (10) : 2201 - 2208