Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4

被引：111
作者：
Powers, JP [1 ]
Li, SY [1 ]
Jaen, JC [1 ]
Liu, JQ [1 ]
Walker, NPC [1 ]
Wang, ZL [1 ]
Wesche, H [1 ]
机构：
[1] Amgen Inc, 1120 Vet Blvd, San Francisco, CA 94080 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 11期
关键词：
IRAK-4; kinase; inflammation; kinase inhibitor;
D O I：
10.1016/j.bmcl.2006.03.020
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
High-throughput screening of a small-molecule compound library resulted in the identification of a novel series of N-acyl 2-aminobenzimidazoles that are potent inhibitors of interleukin-1 receptor-associated kinase-4. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2842 / 2845
页数：4
相关论文
共 10 条
  • [1] IRAK: A kinase associated with the interleukin-1 receptor
    Cao, ZD
    Henzel, WJ
    Gao, XO
    [J]. SCIENCE, 1996, 271 (5252) : 1128 - 1131
  • [2] Bringing the clinical experience with anakinra, to the patient
    Cohen, SB
    Rubbert, A
    [J]. RHEUMATOLOGY, 2003, 42 : 36 - 40
  • [3] IRAK-4: A novel member of the IRAK family with the properties of an IRAK-kinase
    Li, SY
    Strelow, A
    Fontana, EJ
    Wesche, H
    [J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2002, 99 (08) : 5567 - 5572
  • [4] The role of interleukin 1 receptor-associated kinase-4 (IRAK-4) kinase activity in IRAK-4-mediated signaling
    Lye, E
    Mirtsos, C
    Suzuki, N
    Suzuki, S
    Yeh, WC
    [J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (39) : 40653 - 40658
  • [5] Distinct mutations in IRAK-4 confer hyporesponsiveness to lipopolysaccharide and interleukin-1 in a patient with recurrent bacterial infections
    Medvedev, AE
    Lentschat, A
    Kuhns, DB
    Blanco, JCG
    Salkowski, C
    Zhang, SL
    Arditi, MH
    Gallin, JI
    Vogel, SN
    [J]. JOURNAL OF EXPERIMENTAL MEDICINE, 2003, 198 (04) : 521 - 531
  • [6] IRAK (Pelle) family member IRAK-2 and MyD88 as proximal mediators of IL-1 signaling
    Muzio, M
    Ni, J
    Feng, P
    Dixit, VM
    [J]. SCIENCE, 1997, 278 (5343) : 1612 - 1615
  • [7] Pyogenic bacterial infections in humans with IRAK-4 deficiency
    Picard, C
    Puel, A
    Bonnet, M
    Ku, CL
    Bustamante, J
    Yang, K
    Soudais, C
    Dupuis, S
    Feinberg, J
    Fieschi, C
    Elbim, C
    Hitchcock, R
    Lammas, D
    Davies, G
    Al-Ghonaium, A
    Al-Rayes, H
    Al-Jumaah, S
    Al-Hajjar, S
    Al-Mohsen, IZ
    Frayha, HH
    Rucker, R
    Hawn, TR
    Aderem, A
    Tufenkeji, H
    Haraguchi, S
    Day, NK
    Good, RA
    Gougerot-Pocidalo, MA
    Ozinsky, A
    Casanova, JL
    [J]. SCIENCE, 2003, 299 (5615) : 2076 - 2079
  • [8] Severe impairment of interleukin-1 and Toll-like receptor signalling in mice lacking IRAK-4
    Suzuki, N
    Suzuki, S
    Duncan, GS
    Millar, DG
    Wada, T
    Mirtsos, C
    Takada, H
    Wakeham, A
    Itie, A
    Li, SY
    Penninger, JM
    Wesche, H
    Ohashi, PS
    Mak, TW
    Yeh, WC
    [J]. NATURE, 2002, 416 (6882) : 750 - 754
  • [9] IRAK-M is a novel member of the pelle/interleukin-1 receptor-associated kinase (IRAK) family
    Wesche, H
    Gao, X
    Li, XX
    Kirschning, CJ
    Stark, GR
    Cao, ZD
    [J]. JOURNAL OF BIOLOGICAL CHEMISTRY, 1999, 274 (27) : 19403 - 19410
  • [10] OXIDATION OF 1,2-DIAMINOBENZIMIDAZOLES TO 3-AMINO-1,2,4-BENZOTRIAZINES
    ZEIGER, AV
    JOULLIE, MM
    [J]. JOURNAL OF ORGANIC CHEMISTRY, 1977, 42 (03) : 542 - 545
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