| 查看: 623 | 回复: 4 | |||
[求助]
麻烦翻译几句医药方面的东西，谢谢啦
|
|
PARP inhibitor program: SC10914 has single digit nanomolar inhibitory IC50 for PARP-1 enzyme and strong inhibition of VC8 cell proliferation. It also demonstrates the superior PK profiles in rat and efficacy in VC8 (BRCA2 deficient) mice zenograft model compared to Olaparib. In addition, SC10914 has low potential for drug-drug interaction with all six major cytochrome P450 IC50>10uM, low potential for cardiac liabilities with hERG IC50>30uM, and low potential for mutagenicity by showing negative in Ames test. FMS-like receptor tyrosine kinase-3(Flt3), a member of class III tyrosine kinase receptor family, is predominantly expressed in hematopoietic progenitor cells and plays an important role in the pathogenesis of acute myeloid leukemia (AML). Flt3 is expressed in blast cells of most patients with AML including wild-type and two forms of Flt3 mutations. These two mutations identified in the AML patients are internal tandem duplication (ITD) mutations in the juxtamembrane domain and point mutations (TKD) in the activation loop of the TKD. The relapse rates in the Flt3/ITD mutation AML patients are significantly increased and the overall survival rates decreased compared with the AML patients without the Flt3 mutation. So development of a drug inhibited both wide type and mutant Flt3 kinase could provide an effective way to treat AML. Flt3 inhibitor program: SC110219 is a highly potent Flt3 inhibitor both in Flt3 enzyme (IC50 = 5nM) and MV4-11(IC50 = 0.5nM) assays. It also demonstrates very strong antitumor effects in subcutaneous MV4-11 AML Xenograft model in NOD/SCID mice at as low as 3mg/kg dose level. Other biological profiling is under progress. |
回复此楼» 猜你喜欢
拟解决的关键科学问题还要不要写
已经有9人回复
-
最失望的一年
已经有17人回复
-
为什么nbs上溴 没有产物点出现呢
已经有6人回复
-
求推荐博导
已经有4人回复
-
存款400万可以在学校里躺平吗
已经有34人回复
-
求助一下有机合成大神
已经有4人回复
-
求推荐英文EI期刊
已经有5人回复
-
26申博
已经有3人回复
-
基金委咋了？2026年的指南还没有出来？
已经有10人回复
-
疑惑？
已经有5人回复
wangpei838
禁虫 (小有名气)
|
本帖内容被屏蔽 |
2楼2012-01-28 20:46:38
wangpei838
禁虫 (小有名气)
|
本帖内容被屏蔽 |
3楼2012-01-28 20:47:55
wangpei838
禁虫 (小有名气)
|
本帖内容被屏蔽 |
4楼2012-01-28 20:50:11
kno3
捐助贵宾 (著名写手)
- 应助: 3 (幼儿园)
- 金币: 13629.2
- 散金: 5
- 红花: 8
- 帖子: 1909
- 在线: 257小时
- 虫号: 946261
- 注册: 2010-01-21
- 专业: 老年病药物药理
【答案】应助回帖
★
爱与雨下(金币+1): 2012-01-29 19:42:37
sltmac(金币+40): 2012-02-13 08:41:04
sltmac(金币+40): 欢迎常来本版交流 2012-02-13 08:41:11
爱与雨下(金币+1): 2012-01-29 19:42:37
sltmac(金币+40): 2012-02-13 08:41:04
sltmac(金币+40): 欢迎常来本版交流 2012-02-13 08:41:11
| FMS酪氨酸激酶样受体-3(Fit3)是酪氨酸激酶受体家族III类受体，主要表达在造血祖细胞上，在急性髓细胞性白血病(AML)发病机制中起重要作用。Fit3在大部分AML患者的胚细胞上表达，这些患者的基因型包括野生型和两种Fit3突变型。经鉴定，这两种AML患者的基因突变是近膜域的内部串联重复(ITD)突变和TKD激活环的点突变(TKD)。AML患者中，与Fit3野生型患者相比，Fit3/ITD突变患者呈现复发率高和整体存活率低的特点。因此，开发能共同抑制Fit3激酶野生型和突变型的药物是治疗AML的有效方式。 |
5楼2012-01-28 21:57:34