PAK'n it in: Identification of a selective PAK inhibitor

被引:7
作者
Bokoch, Gary M. [1 ]
机构
[1] Scripps Res Inst, Dept Cell Biol, La Jolla, CA 92037 USA
来源
CHEMISTRY & BIOLOGY | 2008年 / 15卷 / 04期
关键词
D O I
10.1016/j.chembiol.2008.03.011
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
p21-activated kinases are important signaling kinases for which no specific chemical inhibitors are known. In this issue of Chemistry & Biology, Deacon et al. target allosteric transitions undergone during PAK activation to identify a selective inhibitor (Deacon et al., 2008).
引用
收藏
页码:305 / 306
页数:2
相关论文
共 11 条
[1]   A tale of two Paks [J].
Arias-Romero, Luis E. ;
Chernoff, Jonathan .
BIOLOGY OF THE CELL, 2008, 100 (02) :97-108
[2]   Central nervous system functions of PAK protein family - From spine morphogenesis to mental retardation [J].
Boda, Bernadett ;
Nikonenko, Irina ;
Alberi, Stefano ;
Muller, Dominique .
MOLECULAR NEUROBIOLOGY, 2006, 34 (01) :67-80
[3]   Biology of the p21-activated kinases [J].
Bokoch, GM .
ANNUAL REVIEW OF BIOCHEMISTRY, 2003, 72 :743-781
[4]   The mechanism of PAK activation - Autophosphorylation events in both regulatory and kinase domains control activity [J].
Chong, C ;
Tan, L ;
Lim, L ;
Manser, E .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (20) :17347-17353
[5]   An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase [J].
Deacon, Sean W. ;
Beeser, Alexander ;
Fukui, Jami A. ;
Rennefahrt, Ulrike E. E. ;
Myers, Cynthia ;
Chernoff, Jonathan ;
Peterson, Jeffrey R. .
CHEMISTRY & BIOLOGY, 2008, 15 (04) :322-331
[6]   A quantitative analysis of kinase inhibitor selectivity [J].
Karaman, Mazen W. ;
Herrgard, Sanna ;
Treiber, Daniel K. ;
Gallant, Paul ;
Atteridge, Corey E. ;
Campbell, Brian T. ;
Chan, Katrina W. ;
Ciceri, Pietro ;
Davis, Mindy I. ;
Edeen, Philip T. ;
Faraoni, Raffaella ;
Floyd, Mark ;
Hunt, Jeremy P. ;
Lockhart, Daniel J. ;
Milanov, Zdravko V. ;
Morrison, Michael J. ;
Pallares, Gabriel ;
Patel, Hitesh K. ;
Pritchard, Stephanie ;
Wodicka, Lisa M. ;
Zarrinkar, Patrick P. .
NATURE BIOTECHNOLOGY, 2008, 26 (01) :127-132
[7]   p21-activated kinases in cancer [J].
Kumar, Rakesh ;
Gururaj, Anupama E. ;
Barnes, Christopher J. .
NATURE REVIEWS CANCER, 2006, 6 (06) :459-471
[8]   Structure of PAK1 in an autoinhibited conformation reveals a multistage activation switch [J].
Lei, M ;
Lu, WG ;
Meng, WY ;
Parrini, MC ;
Eck, MJ ;
Mayer, BJ ;
Harrison, SC .
CELL, 2000, 102 (03) :387-397
[9]   Chemical inhibition of N-WASP by stabilization of a native autoinhibited conformation [J].
Peterson, JR ;
Bickford, LC ;
Morgan, D ;
Kim, AS ;
Ouerfelli, O ;
Kirschner, MW ;
Rosen, MK .
NATURE STRUCTURAL & MOLECULAR BIOLOGY, 2004, 11 (08) :747-755
[10]   The kinase-inhibitory domain of p21-activated kinase 1 (PAK1) inhibits cell cycle progression independent of PAK1 kinase activity [J].
Thullberg, M. ;
Gad, A. ;
Beeser, A. ;
Chernoff, J. ;
Stromblad, S. .
ONCOGENE, 2007, 26 (12) :1820-1828