THE AFFINITY OF THE EXCISED BINDING DOMAIN OF FK-506 FOR THE IMMUNOPHILIN FKBP12

被引:15
|
作者
TEAGUE, SJ
STOCKS, MJ
机构
[1] Fisons Pharmaceuticals PLC, Loughborough, LE11 ORH, Bakewell Road
关键词
D O I
10.1016/S0960-894X(01)80992-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The affinity of the binding domain of FK-506 was determined, in the absence of the constraints imposed upon it by the macrocyclic framework. Removal of those parts of FK-506 not involved in the binding of FK-506 to FKBP12 results in a 50-fold drop in affinity.
引用
收藏
页码:1947 / 1950
页数:4
相关论文
共 50 条
  • [31] IS FKBP INVOLVED IN THE IMMUNOSUPPRESSIVE AND OR TOXIC MECHANISM OF ACTION OF FK-506
    SIGAL, NH
    DUMONT, FJ
    SIEKIERKA, JJ
    WIEDERRECHT, G
    PARENT, SA
    BRIZUELA, L
    TRANSPLANTATION PROCEEDINGS, 1991, 23 (06) : 2846 - 2849
  • [32] Molecular characterization of a plant FKBP12 that does not mediate action of FK506 and rapamycin
    Xu, Qiang
    Liang, Shuping
    Kudla, Jorg
    Luan, Sheng
    Plant Journal, 15 (04): : 511 - 519
  • [34] The role of an immunophilin, FKBP12, in chick embryonic cardiac development
    Obata, K
    Koide, M
    Harayama, H
    Iida, M
    Iio, A
    Ono, T
    Yokota, M
    Tuan, RS
    CIRCULATION, 1996, 94 (08) : 695 - 695
  • [35] Functional targets for an immunophilin, FKBP12, in chick embryonic heart
    Koide, M
    Obata, K
    Iio, A
    Ausma, J
    Somura, F
    Yazawa, S
    Ishiki, R
    Yokota, N
    Tuan, RS
    CIRCULATION, 1998, 98 (17) : 604 - 604
  • [36] INTERACTION OF FKBP12-FK506 WITH CALCINEURIN-A AT THE B-SUBUNIT-BINDING DOMAIN
    KAWAMURA, A
    SU, MSS
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1995, 270 (26) : 15463 - 15466
  • [37] Structural basis of conformational transitions in the active site and 80's loop in the FK506-binding protein FKBP12
    Mustafi, Sourajit M.
    Brecher, Matthew
    Zhang, Jing
    Li, Hongmin
    Lemaster, David M.
    Hernandez, Griselda
    BIOCHEMICAL JOURNAL, 2014, 458 : 525 - 536
  • [38] Conformational Entropy of FK506 Binding to FKBP12 Determined by Nuclear Magnetic Resonance Relaxation and Molecular Dynamics Simulations
    Solomentsev, Gleb
    Diehl, Carl
    Akke, Mikael
    BIOCHEMISTRY, 2018, 57 (09) : 1451 - 1461
  • [39] Co-expression of cyclophilin A, FK506-binding protein (FKBP12) and calcineurin by normal and psoriatic keratinocytes.
    Grant, KR
    Todd, C
    Reynolds, NJ
    JOURNAL OF INVESTIGATIVE DERMATOLOGY, 1998, 110 (04) : 529 - 529
  • [40] FK506-binding protein, FKBP12, promotes serine utilization and negatively regulates threonine deaminase in fission yeast
    Sasaki, Mayuki
    Nishimura, Shinichi
    Yashiroda, Yoko
    Matsuyama, Akihisa
    Kakeya, Hideaki
    Yoshida, Minoru
    ISCIENCE, 2022, 25 (12)