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Brutons Tyrosine Kinase as Anti-Cancer Drug Target
专利权人:
发明人:
Douglas Conklin,Cheryl Eifert,Antonis Kourtidis,Xianhui Wang,Leila Kokabee
申请号:
US15583313
公开号:
US20170335011A1
申请日:
2017.05.01
申请国别(地区):
US
年份:
2017
代理人:
摘要:
Receptor protein kinases (RPTKs) transmit extracellular signals across the plasma membrane to cytosolic proteins, stimulating formation of complexes that regulate key cellular functions. Over 5 half of the known tyrosine kinases are implicated in human cancers and are therefore highly promising drug targets. A large-scale loss-of-function analysis of tyrosine kinases using RNA interference in the clinically relevant Erb-B2 positive, BT474 breast cancer cell line showed that Brutons tyrosine kinase (BTK), a cytosolic, non-receptor tyrosine kinase that has been extensively studied for its role in B cell development, is required, in altered form, for BT474 10 breast cancer survival. This alternative form contains an amino-terminal extension that is also present in tumorigenic breast cells at significantly higher levels than in normal breast cells.
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