Two-Headed PROTAC: An Effective New Tool for Targeted Protein Degradation

被引：47
作者：
Cyrus, Kedra [1 ]
Wehenkel, Marie [1 ]
Choi, Eun-Young [2 ]
Swanson, Hollie [2 ]
Kim, Kyung-Bo [1 ]
机构：
[1] Univ Kentucky, Dept Pharmaceut Sci, Lexington, KY 40536 USA
[2] Univ Kentucky, Dept Mol & Biomed Pharmacol, Lexington, KY 40536 USA
来源：
CHEMBIOCHEM | 2010年 / 11卷 / 11期
关键词：
estrogen receptor; ligases; PROTAC; proteomics; ubiquitin-proteasome pathway; ARYL-HYDROCARBON RECEPTOR; CHIMERIC MOLECULES; CHEMICAL GENETICS; UBIQUITINATION; BINDING; SCF;
D O I：
10.1002/cbic.201000222
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：
Better than one: A novel class of PROTAC that recruits target protein for ubiquitination and subsequent degradation by the proteasome has been successfully synthesized and tested for its activity to degrade a target protein. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码：1531 / 1534
页数：4
相关论文
共 21 条
[1]   Chemical genetics: exploring and controlling cellular processes with chemical probes [J].
Crews, CM ;
Splittgerber, U .
TRENDS IN BIOCHEMICAL SCIENCES, 1999, 24 (08) :317-320
[2]   SCF and cullin/RING H2-based ubiquitin ligases [J].
Deshaies, RJ .
ANNUAL REVIEW OF CELL AND DEVELOPMENTAL BIOLOGY, 1999, 15 :435-467
[3]   The ubiquitin system [J].
Hershko, A ;
Ciechanover, A .
ANNUAL REVIEW OF BIOCHEMISTRY, 1998, 67 :425-479
[4]   Protein Knockdown Using Methyl Bestatin-Ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-Mediated Degradation of Cellular Retinoic Acid-Binding Proteins [J].
Itoh, Yukihiro ;
Ishikawa, Minoru ;
Naito, Mikihiko ;
Hashimoto, Yuichi .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2010, 132 (16) :5820-5826
[5]   Trace elements in regulation of NF-κB activity [J].
Kudrin, AV .
JOURNAL OF TRACE ELEMENTS IN MEDICINE AND BIOLOGY, 2000, 14 (03) :129-142
[6]   Synthesis and evaluation of geldanamycin-testosterone hybrids [J].
Kuduk, SD ;
Harris, CR ;
Zheng, FZF ;
Sepp-Lorenzino, L ;
Ouerfelli, Q ;
Rosen, N ;
Danishefsky, SJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (11) :1303-1306
[7]   Targeted degradation of the aryl hydrocarbon receptor by the PROTAC approach: A useful chemical genetic tool [J].
Lee, Hyosung ;
Puppala, Dinesh ;
Choi, Eun-Young ;
Swanson, Hollie ;
Kim, Kyung-Bo .
CHEMBIOCHEM, 2007, 8 (17) :2058-2062
[8]   Development of an aryl hydrocarbon receptor antagonist using the proteolysis-targeting chimeric molecules approach: A potential tool for chemoprevention [J].
Puppala, Dinesh ;
Lee, Hyosung ;
Kim, Kyung Bo ;
Swanson, Hollie I. .
MOLECULAR PHARMACOLOGY, 2008, 73 (04) :1064-1071
[9]   Targeting steroid hormone receptors for ubiquitination and degradation in breast and prostate cancer [J].
Rodriguez-Gonzalez, A. ;
Cyrus, K. ;
Salcius, M. ;
Kim, K. ;
Crews, C. M. ;
Deshaies, R. J. ;
Sakamoto, K. M. .
ONCOGENE, 2008, 27 (57) :7201-7211
[10]   Development of protacs to target cancer-promoting proteins for ubiquitination and degradation [J].
Sakamoto, KM ;
Kim, KB ;
Verma, R ;
Ransick, A ;
Stein, B ;
Crews, CM ;
Deshaies, RJ .
MOLECULAR & CELLULAR PROTEOMICS, 2003, 2 (12) :1350-1358
123