Analysis of binding energy activity of imatinib and Abl tyrosine kinase domain based on simple consideration for conformational change: An explanation for variation in imatinib effect in mutated type.

Wiwanitkit V

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Analysis of binding energy activity of imatinib and Abl tyrosine kinase domain based on simple consideration for conformational change: An explanation for variation in imatinib effect in mutated type.

机译：基于对构象变化的简单考虑，分析伊马替尼和Abl酪氨酸激酶结构域的结合能活性：解释突变型伊马替尼效应的变化。

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Imatinib is a clinically well-tolerated small molecule inhibitor that exerts selective, dual inhibition on the transforming growth factor beta and platelet-derived growth factor pathways. The recognition of an inactive conformation of Abl, in which a catalytically important Asp-Phe-Gly motif is flipped by approximately 180 degrees with respect to the active conformation, underlies the specificity of the cancer drug imatinib, which is used to treat chronic myelogenous leukemia. However, conformational analysis shows that the effect of the drug depends on the potential energy, which varies due to the alpha rotatable angles of the Abl tyrosine kinase domain. In this study, the author determines the change of binding energy between the Abl tyrosine kinase domain, due to the variation in rotatable angles, and bond lengthening. According to this study, the ratio between the required binding energy between the wild and mutated types is equal to 1: 1.16.

机译：伊马替尼是一种临床上耐受良好的小分子抑制剂，对转化生长因子β和血小板衍生的生长因子途径具有选择性，双重抑制作用。 Abl的非活性构象的识别，其中具有催化活性的Asp-Phe-Gly基序相对于活性构象可翻转约180度，这是用于治疗慢性粒细胞性白血病的抗癌药物imatinib的特异性的基础。但是，构象分析表明，药物的作用取决于势能，势能由于Abl酪氨酸激酶域的α可旋转角度而变化。在这项研究中，作者确定了Abl酪氨酸激酶结构域之间的结合能变化，这是由于可旋转角度的变化和键的延长所致。根据这项研究，野生型和突变型之间所需的结合能之比等于1：1.16。

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《Indian journal of cancer.》 |2009年第4期|共2页
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Wiwanitkit V;
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1. Analysis of binding energy activity of imatinib and Abl tyrosine kinase domain based on simple consideration for conformational change: An explanation for variation in imatinib effect in mutated type. [J] . Wiwanitkit V Indian journal of cancer. . 2009,第4期

机译：基于对构象变化的简单考虑，分析伊马替尼和Abl酪氨酸激酶结构域的结合能活性：解释突变型伊马替尼效应的变化。
2. Conformational flexibility and binding energy profile of c-Abl tyrosine kinase complexed with Imatinib: An insight from MD study [J] . Dubey K.D., Ojha R.P. Molecular simulation . 2011,第13a15期

机译：依马替尼复合的c-Abl酪氨酸激酶的构象柔性和结合能谱：MD研究的见解
3. Drug resistance and BCR-ABL kinase domain mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia from the imatinib to the second-generation tyrosine kinase inhibitor era: The main changes are in the type of mutations, but not in the frequency of mutation involvement. [J] . Simona Soverini, Caterina De Benedittis, Cristina Papayannidis, Cancer: A Journal of the American Cancer Society . 2014,第7期

机译：从伊马替尼到第二代酪氨酸激酶抑制剂时代的费城染色体阳性急性淋巴细胞白血病的耐药性和BCR-ABL激酶结构域突变：主要变化在于突变类型，但不涉及突变的发生频率。
4. The effects of mutation and inhibitor binding on Abl kinase conformation by hydrogen deuterium exchange mass spectrometry [C] . Roxana E. Iacob, Teodora Pene-Dumitrescu, Jianming Zhang, ASMS Conference on Mass Spectrometry and Allied Topics . 2008

机译：抗突变与抑制剂对氢氘交换质谱法的α细胞α构象的影响
5. Conformational analysis of breast tumor kinase SH2 domain by hydrogen exchange mass spectrometry. [D] . Reiser, Kelly A. 2011

机译：通过氢交换质谱法对乳腺肿瘤激酶SH2结构域进行构象分析。
6. Choosing the Best Second-Line Tyrosine Kinase Inhibitor in Imatinib-Resistant Chronic Myeloid Leukemia Patients Harboring Bcr-Abl Kinase Domain Mutations: How Reliable Is the IC50? [O] . Simona Soverini, Gianantonio Rosti, Ilaria Iacobucci, 2011

机译：在具有Bcr-Abl激酶结构域突变的伊马替尼耐药的慢性粒细胞白血病患者中选择最佳的二线酪氨酸激酶抑制剂：IC50的可靠性如何？
7. Drug resistance and BCR-ABL kinase domain mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia from the imatinib to the second-generation tyrosine kinase inhibitor era: The main changes are in the type of mutations, but not in the frequency of mutation involvement [O] . Soverini Simona, De Benedittis Caterina, Papayannidis Cristina, 2014

机译：从伊马替尼到第二代酪氨酸激酶抑制剂时代的费城染色体阳性急性淋巴细胞白血病的耐药性和BCR-ABL激酶结构域突变：主要变化在于突变类型，但不涉及突变发生的频率

Analysis of binding energy activity of imatinib and Abl tyrosine kinase domain based on simple consideration for conformational change: An explanation for variation in imatinib effect in mutated type.

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