Small-Molecule Kinase Downregulators

被引：45
|
作者：
Jones, Lyn H. [1 ]
机构：
[1] Jnana Therapeut, 50 Northern Ave, Boston, MA 02210 USA
来源：
CELL CHEMICAL BIOLOGY | 2018年 / 25卷 / 01期
关键词：
PROTEIN-DEGRADATION; STRUCTURAL BASIS; CANCER; INHIBITORS; DISCOVERY; JAK2;
D O I：
10.1016/j.chembiol.2017.10.011
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：
New opportunities to advance small-molecule kinase ligands that downregulate their cognate target binding proteins are discussed. Rationally designed heterobifunctional kinase degraders are compared with ATP site ligands that were serendipitously found to cause kinase downregulation. These approaches could be particularly useful in the treatment of cancers since many kinases are known to remodel pro-oncogenic protein-protein interactions, which could be destroyed by small-molecule-mediated kinase depletion.
引用
收藏
页码：30 / 35
页数：6
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