Structure-based design of novel calcineurin (PP2B) inhibitors

被引：38

作者：

Tatlock, JH

Linton, MA

Hou, XJ

Kissinger, CR

Pelletier, LA

Showalter, RE

Tempczyk, A

Villafranca, JE

机构：

[1] Agouron Pharmaceuticals Inc., 3565 General Atomics Court, San Diego

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(97)00141-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design, synthesis, and evaluation of small molecule, in vitro, inhibitors of human calcineurin is described. These ligands were derived from the known nonspecific phosphatase inhibitor endothall, and were modified to enhance binding and selectivity toward calcineurin using protein crystal structure information. (C) 1997 Elsevier Science Ltd.

引用

页码：1007 / 1012

页数：6

共 49 条

[1] Design, synthesis and X-ray crystallographic studies of [7.3.1] and [8.3.1] macrocyclic FKBP-12 ligands
Babine, RE
Bleckman, TM
Littlefield, ES
Parge, HE
Pelletier, LAK
Lewis, CT
French, JV
Imbacuan, M
Katoh, S
Tatlock, JH
Showalter, RE
Ernest, J
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (04) : 385 - 390
[2] INHIBITORY EFFECT OF A MARINE-SPONGE TOXIN, OKADAIC ACID, ON PROTEIN PHOSPHATASES - SPECIFICITY AND KINETICS
BIALOJAN, C
TAKAI, A
[J]. BIOCHEMICAL JOURNAL, 1988, 256 (01) : 283 - 290
[3] STRUCTURAL STUDIES ON CYANOGINOSIN-LR, CYANOGINOSIN-YR, CYANOGINOSIN-YA AND -CYANOGINOSIN-YM, PEPTIDE TOXINS FROM MICROCYSTIS-AERUGINOSA
BOTES, DP
WESSELS, PL
KRUGER, H
RUNNEGAR, MTC
SANTIKARN, S
SMITH, RJ
BARNA, JCJ
WILLIAMS, DH
[J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1985, (12): : 2747 - 2748
[4] THE STRUCTURE OF CYANOGINOSIN-LA, A CYCLIC HEPTAPEPTIDE TOXIN FROM THE CYANOBACTERIUM MICROCYSTIS-AERUGINOSA
BOTES, DP
TUINMAN, AA
WESSELS, PL
VILJOEN, CC
KRUGER, H
WILLIAMS, DH
SANTIKARN, S
SMITH, RJ
HAMMOND, SJ
[J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1984, (10): : 2311 - 2318
[5] TARGETS OF IMMUNOPHILIN-IMMUNOSUPPRESSANT COMPLEXES ARE DISTINCT HIGHLY CONSERVED REGIONS OF CALCINEURIN-A
CARDENAS, ME
MUIR, RS
BREUDER, T
HEITMAN, J
[J]. EMBO JOURNAL, 1995, 14 (12) : 2772 - 2783
[6] CHENG XC, 1990, J ANTIBIOT, V43, P809, DOI 10.7164/antibiotics.43.809
[7] IDENTIFICATION OF CALCINEURIN AS A KEY SIGNALING ENZYME IN LYMPHOCYTE-T ACTIVATION
CLIPSTONE, NA
CRABTREE, GR
[J]. NATURE, 1992, 357 (6380) : 695 - 697
[8] ORGANIC-REACTIONS AT HIGH-PRESSURE - THE PREPARATIVE SCALE SYNTHESIS OF CANTHARIDIN
DAUBEN, WG
GERDES, JM
SMITH, DB
[J]. JOURNAL OF ORGANIC CHEMISTRY, 1985, 50 (14) : 2576 - 2578
[9] SIMPLE, EFFICIENT TOTAL SYNTHESIS OF CANTHARIDIN VIA A HIGH-PRESSURE DIELS-ALDER REACTION
DAUBEN, WG
KESSEL, CR
TAKEMURA, KH
[J]. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1980, 102 (22) : 6893 - 6894
[10] Structure-based design of novel, urea-containing FKBP12 inhibitors
Dragovich, PS
Barker, JE
French, J
Imbacuan, M
Kalish, VJ
Kissinger, CR
Knighton, DR
Lewis, CT
Moomaw, EW
Parge, HE
Pelletier, LAK
Prins, TJ
Showalter, RE
Tatlock, JH
Tucker, KD
Villafranca, JE
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (09) : 1872 - 1884

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