SYNTHETIC FKBP12 LIGANDS - DESIGN AND SYNTHESIS OF PYRANOSE REPLACEMENTS

被引：9

作者：

BIRKENSHAW, TN ^{[1
]}

CAFFREY, MV ^{[1
]}

CLADINGBOEL, DE ^{[1
]}

COOPER, ME ^{[1
]}

DONALD, DK ^{[1
]}

FURBER, M ^{[1
]}

HARDERN, DN ^{[1
]}

HARRISON, RP ^{[1
]}

MARRIOTT, DP ^{[1
]}

PERRY, MWD ^{[1
]}

STOCKS, MJ ^{[1
]}

TEAGUE, SJ ^{[1
]}

WITHNALL, WJ ^{[1
]}

机构：

[1] FISONS PLC,DIV PHARMACEUT,LOUGHBOROUGH LE11 0RH,LEICS,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(01)80272-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of FKBP12 ligands were designed and synthesised and their affinity for FKBP12 assessed. In these ligands the pyranose ring of FK506 was replaced by other mole synthetically accessible groups. The preparation of suitable intermediates for the synthesis of ''dual domain'' inhibitors (compounds 6a-c, 15 and 22) is also described.

引用

页码：2501 / 2506

页数：6

共 14 条

[1] INTERLEUKIN-2 STIMULATION OF P70 S6 KINASE-ACTIVITY IS INHIBITED BY THE IMMUNOSUPPRESSANT RAPAMYCIN [J].

CALVO, V ;

CREWS, CM ;

VIK, TA ;

BIERER, BE .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (16) :7571-7575

[2] CYCLOSPORINE-A SPECIFICALLY INHIBITS FUNCTION OF NUCLEAR PROTEINS INVOLVED IN T-CELL ACTIVATION [J].

EMMEL, EA ;

VERWEIJ, CL ;

DURAND, DB ;

HIGGINS, KM ;

LACY, E ;

CRABTREE, GR .

SCIENCE, 1989, 246 (4937) :1617-1620

[3] STRUCTURE-ACTIVITY STUDIES OF SYNTHETIC FKBP LIGANDS AS PEPTIDYL-PROLYL ISOMERASE INHIBITORS [J].

HOLT, DA ;

KONIALIANBECK, AL ;

OH, HJ ;

YEN, HK ;

ROZAMUS, LW ;

KROG, AJ ;

ERHARD, KF ;

ORTIZ, E ;

LEVY, MA ;

BRANDT, M ;

BOSSARD, MJ ;

LUENGO, JI .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (02) :315-320

[4] THE T-CELL TRANSCRIPTION FACTOR NFAT(P) IS A SUBSTRATE FOR CALCINEURIN AND INTERACTS WITH FOS AND JUN [J].

JAIN, JN ;

MCCAFFREY, PG ;

MINER, Z ;

KERPPOLA, TK ;

LAMBERT, JN ;

VERDINE, GL ;

CURRAN, T ;

RAO, A .

NATURE, 1993, 365 (6444) :352-355

[5]

KAY JE, 1991, IMMUNOLOGY, V72, P544

[6] DEVELOPMENT OF TETRAHYDROFURAN CHIRAL SYNTHONS BY ENZYMATIC APPROACH - IMPROVED SYNTHESIS OF A STRONG AGONIST OF PLATELET-ACTIVATING-FACTOR [J].

KOBAYASHI, S ;

SATO, M ;

EGUCHI, Y ;

OHNO, M .

TETRAHEDRON LETTERS, 1992, 33 (08) :1081-1084

[7] 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

[8] SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF MACROCYCLIC FKBP LIGANDS [J].

LUENGO, JI ;

KONIALIANBECK, A ;

LEVY, MA ;

BRANDT, M ;

EGGLESTON, DS ;

HOLT, DA .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (02) :321-324

[9] CYCLOSPORINE-A, FK-506, AND RAPAMYCIN - PHARMACOLOGICAL PROBES OF LYMPHOCYTE SIGNAL TRANSDUCTION [J].

SIGAL, NH ;

DUMONT, FJ .

ANNUAL REVIEW OF IMMUNOLOGY, 1992, 10 :519-560

[10] THE AFFINITY OF THE EXCISED BINDING DOMAIN OF FK-506 FOR THE IMMUNOPHILIN FKBP12 [J].

TEAGUE, SJ ;

STOCKS, MJ .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (10) :1947-1950

← 1 2 →