Inhibitors of c-Jun N-Terminal Kinases: An Update

被引:79
作者
Koch, Pierre [1 ]
Gehringer, Matthias [1 ]
Laufer, Stefan A. [1 ]
机构
[1] Univ Tubingen, Inst Pharmaceut Sci, Dept Pharmaceut & Med Chem, D-72076 Tubingen, Germany
关键词
SMALL-MOLECULE INHIBITORS; SELECTIVE JNK INHIBITORS; LEUCINE-ZIPPER KINASE; INDUCED CELL-DEATH; PROTEIN-KINASE; BIOLOGICAL EVALUATION; THERAPEUTIC TARGET; PEPTIDE INHIBITOR; STRUCTURAL BASIS; DRUG DISCOVERY;
D O I
10.1021/jm501212r
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The c-Jun N-terminal kinases (JNKs) are serine/threonine kinases implicated in the pathogenesis of various diseases. Recent advances in the development of novel inhibitors of JNKs will be reviewed. Significant progress in the design of JNK inhibitors displaying selectivity versus other kinases has been achieved within the past 4 years. However, the development of isoform selective JNK inhibitors is still an open task.
引用
收藏
页码:72 / 95
页数:24
相关论文
共 165 条
[1]   Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors [J].
Alam, Mahbub ;
Beevers, Rebekah E. ;
Ceska, Tom ;
Davenport, Richard J. ;
Dickson, Karen M. ;
Fortunato, Mara ;
Gowers, Lewis ;
Haughan, Alan F. ;
James, Lynwen A. ;
Jones, Mark W. ;
Kinsella, Natasha ;
Lowe, Christopher ;
Meissner, Johannes W. G. ;
Nicolas, Anne-Lise ;
Perry, Benjamin G. ;
Phillips, David J. ;
Pitt, William R. ;
Platt, Adam ;
Ratcliffe, Andrew J. ;
Sharpe, Andrew ;
Tait, Laura J. .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (12) :3463-3467
[2]   c-Jun N-Terminal Kinase 1 Is Required for the Development of Pulmonary Fibrosis [J].
Alcorn, John F. ;
van der Velden, Jos ;
Brown, Amy L. ;
McElhinney, Brian ;
Irvin, Charles G. ;
Janssen-Heininger, Yvonne M. W. .
AMERICAN JOURNAL OF RESPIRATORY CELL AND MOLECULAR BIOLOGY, 2009, 40 (04) :422-432
[3]   N-(3-cyano-4,5,6,7-tetrahydro-1-benzothien-2-yl)amides as potent, selective, inhibitors of JNK2 and JNK3 [J].
Angell, Richard M. ;
Atkinson, Francis L. ;
Brown, Murray J. ;
Chuang, Tsu Tshen ;
Christopher, John A. ;
Cichy-Knight, Maria ;
Dunn, Allison K. ;
Hightower, Kendra E. ;
Malkakorpi, Susanna ;
Musgrave, James R. ;
Neu, Margarete ;
Rowland, Paul ;
Shea, Robyn L. ;
Smith, Jeffery L. ;
Somers, Donald O. ;
Thomas, Sonia A. ;
Thompson, Gladstone ;
Wang, Ruolan .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (05) :1296-1301
[4]  
[Anonymous], The PyMOL Molecular Graphics System
[5]   Discovery, synthesis and biological evaluation of isoquinolones as novel and highly selective JNK inhibitors (1) [J].
Asano, Yasutomi ;
Kitamura, Shuji ;
Ohra, Taiichi ;
Aso, Kazuyoshi ;
Igata, Hideki ;
Tamura, Tomoko ;
Kawamoto, Tomohiro ;
Tanaka, Toshimasa ;
Sogabe, Satoshi ;
Matsumoto, Shin-ichi ;
Yamaguchi, Masashi ;
Kimura, Hiroyuki ;
Itoh, Fumio .
BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (08) :4715-4732
[6]  
Asano Y, 2008, BIOORGAN MED CHEM, V16, P4699, DOI 10.1016/j.bmc.2008.02.028
[7]   Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition [J].
Backes, A. C. ;
Zech, B. ;
Felber, B. ;
Klebl, B. ;
Mueller, G. .
EXPERT OPINION ON DRUG DISCOVERY, 2008, 3 (12) :1427-1449
[8]   AM-111 reduces hearing loss in a guinea pig model of acute labyrinthitis [J].
Barkdull, Gregory C. ;
Hondarrague, Yannick ;
Meyer, Thomas ;
Harris, Jeffrey P. ;
Keithley, Elizabeth M. .
LARYNGOSCOPE, 2007, 117 (12) :2174-2182
[9]   Novel roles for JNK1 in metabolism [J].
Belgardt, Bengt F. ;
Mauer, Jan ;
Bruening, Jens C. .
AGING-US, 2010, 2 (09) :621-626
[10]   SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase [J].
Bennett, BL ;
Sasaki, DT ;
Murray, BW ;
O'Leary, EC ;
Sakata, ST ;
Xu, WM ;
Leisten, JC ;
Motiwala, A ;
Pierce, S ;
Satoh, Y ;
Bhagwat, SS ;
Manning, AM ;
Anderson, DW .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2001, 98 (24) :13681-13686