Dasatinib（达沙替尼）基础信息 中文名：Src家族酪氨酸激酶抑制剂;SFK抑制剂;Bcl-Abl激酶抑制剂;达沙替尼 英文名：Dasatinib; Src family tyrosine kinase (SFK)/Bcl-Abl kinase inhibitor ;Src family tyrosine kinase inhibitor;SFK inhibitor;Bcl-Abl kinase inhibitor;BMS-354825 CAS号：302962-49-8 结构式：Cc1...
英文名:Dasatinib; Src family tyrosine kinase (SFK)/Bcl-Abl kinase inhibitor ;Src family tyrosine kinase inhibitor;SFK inhibitor;Bcl-Abl kinase inhibitor;BMS-354825 CAS号:302962-49-8 结构式:Cc1cccc(c1NC(=O)c2cnc(s2)Nc3cc(nc(n3)C)N4CCN(CC4)CCO)Cl 分子式:C22H26ClN7O2S 分子量:488.01 ...
Definition Tyrosine kinase inhibitors ( TKIs ) are small molecules that bind to and inhibit the activity of tyrosine kinases. The latter are enzymes that catalyze the phosphorylation of a protein on the tyrosine residue using adenosine triphosphate as a substrate. The activities of tyrosine kinases ...
SFK, Src-family kinase; TK, tyrosine kinase. The modular structure of Src-kinases comprises a short N-terminal segment where a myristoylation (or more rarely palmitoylation) site occurs, which is sequentially followed by the so-called Unique domain, an SH3 domain, an SH2 domain, and the TK...
Src family kinases, key regulators of signal transduction. Oncogene. 2004;23(48):7906-7909. 2.Roskoski R. Src protein-tyrosine kinase structure, mechanism, and small molecule inhibitors. Pharmacol Res. 2015;94:9-25. 3.Frame MC. Src in cancer: deregulation and consequences for cell behaviour...
Here, we show that the SRC-family tyrosine kinase hematopoietic cell kinase (HCK), which is primarily expressed in the hematopoietic lineage but not in mature B cells, is aberrantly expressed in MCL, and that high expression of HCK is associated with inferior prognosis of MCL patients. HCK ...
如细胞内钙离子浓度上调可直接通过钙调蛋白或蛋白激酶C(PKC)调节一些腺苷酸环化酶的活性,最终影响胞内cAMP的浓度。既往研究已证实在一些组织中Src家族酪氨酸激酶(Src family tyrosine kinase,SFK)的激活呈cAMP依赖或蛋白激酶A(PKA)依赖性,本研究旨在晶状体上皮中去探究是否存在cAMP依赖或者是PKA依赖的SFK的激活。
(G14V) elevated JNK activity in HEK 293 cells. The Gα12Q229L-stimulated activation of JNK was blocked by a specific inhibitor of protein tyrosine kinases (PP2), and C-terminal Src kinase (Csk). Moreover, we observed that Gα12Q229L stimulated Src family kinase activity and v-Src ...
4. Boggon T J , Eck M J . Structure and regulation of Srcfamily kinases[J]. Oncogene.5.Roskoski, Robert.Src protein-tyrosine kinase structure, mechanism, and small moleculeinhibitors[J]. Pharmacological Research, 2015, 94:9-25.6.Aleshin, A, Finn, etal. SRC: a century of science ...
Dasatinib, Src family tyrosine kinase (SFK)/Bcl-Abl kinase inhibitor是非受体酪氨酸激酶 Abl 和 Src 以及 Src 家族其他成员的有效抑制剂。 它在亚纳摩尔浓度下有效,抑制 Src、Abl 和 Lck,IC50 值分别为 0.05、0.5 和 0.4 nM。在纳摩尔浓度下,达沙替尼还阻断其他几种受体和非受体酪氨酸激酶的活性, 加上...