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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 10期

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.

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页码：1947 / 1950

页数：4

相关论文

共 22 条

[1]

ALDAPE RA, 1992, J BIOL CHEM, V267, P16029

[2] A NOVEL APPLICATION OF THE DESS-MARTIN REAGENT TO THE SYNTHESIS OF AN FK506 ANALOG AND OTHER TRICARBONYL COMPOUNDS [J].

BATCHELOR, MJ ;

GILLESPIE, RJ ;

GOLEC, JMC ;

HEDGECOCK, CJR .

TETRAHEDRON LETTERS, 1993, 34 (01) :167-170

[3] 2 DISTINCT SIGNAL TRANSMISSION PATHWAYS IN LYMPHOCYTES-T ARE INHIBITED BY COMPLEXES FORMED BETWEEN AN IMMUNOPHILIN AND EITHER FK506 OR RAPAMYCIN [J].

BIERER, BE ;

MATTILA, PS ;

STANDAERT, RF ;

HERZENBERG, LA ;

BURAKOFF, SJ ;

CRABTREE, G ;

SCHREIBER, SL .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1990, 87 (23) :9231-9235

[4] C10 N-ACYL MODIFIED FK-506 - A POSSIBLE HYBRID ANALOG OF THE TRANSITION-STATE OF PEPTIDYL-PROLYL CIS-TRANS ISOMERIZATION [J].

DONALD, DK ;

COOPER, ME ;

FURBER, M ;

WELLS, E ;

HUTCHINSON, R ;

BLACK, FM .

TETRAHEDRON LETTERS, 1991, 32 (10) :1375-1378

[5] EQUILIBRIUM DENATURATION OF RECOMBINANT HUMAN FK BINDING-PROTEIN IN UREA [J].

EGAN, DA ;

LOGAN, TM ;

LIANG, H ;

MATAYOSHI, E ;

FESIK, SW ;

HOLZMAN, TF .

BIOCHEMISTRY, 1993, 32 (08) :1920-1927

[6] A SYNTHESIS OF THE C(1)-C(15) SEGMENT OF TSUKUBAENOLIDE (FK 506) [J].

KOCIENSKI, P ;

STOCKS, M ;

DONALD, D ;

COOPER, M ;

MANNERS, A .

TETRAHEDRON LETTERS, 1988, 29 (35) :4481-4484

[7]

KOCIENSKI P, 1990, SYNLETT, V1, P38

[8] STRAIGHTFORWARD SYNTHESIS OF 1,2,3-TRICARBONYL SYSTEMS [J].

LINDE, RG ;

JERONCIC, LO ;

DANISHEFSKY, SJ .

JOURNAL OF ORGANIC CHEMISTRY, 1991, 56 (07) :2534-2538

[9] CALCINEURIN IS A COMMON TARGET OF CYCLOPHILIN-CYCLOSPORINE-A AND FKBP-FK506 COMPLEXES [J].

LIU, J ;

FARMER, JD ;

LANE, WS ;

FRIEDMAN, J ;

WEISSMAN, I ;

SCHREIBER, SL .

CELL, 1991, 66 (04) :807-815

[10] INHIBITION OF T-CELL SIGNALING BY IMMUNOPHILIN LIGAND COMPLEXES CORRELATES WITH LOSS OF CALCINEURIN PHOSPHATASE-ACTIVITY [J].

LIU, J ;

ALBERS, MW ;

WANDLESS, TJ ;

LUAN, S ;

ALBERG, DG ;

BELSHAW, PJ ;

COHEN, P ;

MACKINTOSH, C ;

KLEE, CB ;

SCHREIBER, SL .

BIOCHEMISTRY, 1992, 31 (16) :3896-3901