【求助】酪氨酸激酶抑制剂PP1和PP2有什么区别?
丁香园论坛
急切想知道,谢谢!
The Src-selective Kinase Inhibitor PP1 Also Inhibits Kit and Bcr-Abl Tyrosine Kinases (http://www.ncbi.nlm.nih.gov/pubmed/12475982)
PP2也可抑制EGFR.
要非要说区别,大概是PP1对Src mutant比对wild type Src的选择性更强,而PP2则抑制Lck、Fyn、Hck。
(参见http://books.google.com/books?id=g52MY3XLGK4C&pg=PA180&lpg=PA180&dq=pp2+is+a+competitive+inhibitor+of+src&source=bl&ots=8Qvjs5DS1Q&sig=sdGYHI0fjVb3xYUeBc83JQmcBpA&hl=en&ei=OBqYTIK3IMuinQfrw-0g&sa=X&oi=book_result&ct=result&resnum=6&sqi=2&ved=0CDAQ6AEwBQ#v=onepage&q&f=false)
ylhuang0502 wrote:
首先纠正一下, PP1和PP2都不是酪氨酸激酶的通用抑制剂,两者均为Src family kinase的选择性抑制剂。其中PP2更常用些,两者的差异很小,化学结构非常相似,两者均不是Src family kinase 特异性抑制剂,两者均可抑制别的激酶的活性,,比如:
The Src-selective Kinase Inhibitor PP1 Also Inhibits Kit and Bcr-Abl Tyrosine Kinases (http://www.ncbi.nlm.nih.gov/pubmed/12475982)
PP2也可抑制EGFR.
要非要说区别,大概是PP1对Src mutant比对wild type Src的选择性更强,而PP2则抑制Lck、Fyn、Hck。
(参见http://books.google.com/books?id=g52MY3XLGK4C&pg=PA180&lpg=PA180&dq=pp2+is+a+competitive+inhibitor+of+src&source=bl&ots=8Qvjs5DS1Q&sig=sdGYHI0fjVb3xYUeBc83JQmcBpA&hl=en&ei=OBqYTIK3IMuinQfrw-0g&sa=X&oi=book_result&ct=result&resnum=6&sqi=2&ved=0CDAQ6AEwBQ#v=onepage&q&f=false)
请问pp2是抑制了src的表达还是磷酸化位点,能一直416的磷酸化位点吗?
如果要抑制416位点,请问用什么抑制剂呢?
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