Identification of TRE‐130 as Reversible Inhibitor of Pan‐EGFR Mutants while Sparing EGFR Wild‐Type Activity

Krishna Babu Duggirala; Hyeonjeong Choe; Byeong Uk Jeon; Myoung Eun Jung; Areum Go; Byungho Lim; Chaewon Park; Jiyeun Yoon; Chong Hak Chae; Byoung Chul Cho; Gildon Choi; Kwangho Lee

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Identification of TRE‐130 as Reversible Inhibitor of Pan‐EGFR Mutants while Sparing EGFR Wild‐Type Activity

机译：鉴定TRE-130作为泛egfr突变体的可逆抑制剂，同时保留EGFR野生型活性

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Proposed binding mode of TRE‐130 (thick cyan sticks) in the EGFR.

机译：在EGFR中提出的TRE-130（厚青色棒）的结合模式。

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《Bulletin of the Korean Chemical Society》 |2019年第12期|共4页
作者
Krishna Babu Duggirala; Hyeonjeong Choe; Byeong Uk Jeon; Myoung Eun Jung; Areum Go; Byungho Lim; Chaewon Park; Jiyeun Yoon; Chong Hak Chae; Byoung Chul Cho; Gildon Choi; Kwangho Lee;
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中图分类化学;
关键词
EGFR T790M/C797SKinasesNSCLCDiaminopyrimidinesSulfonylurea;

机译：EGFR T790M / C797SKINASENSNSCLCDIAMINOPYRIMIDINESTULFONYLUREA;

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专利

1. Identification of TRE-130 as Reversible Inhibitor of Pan-EGFR Mutants while Sparing EGFR Wild-Type Activity [J] . Krishna Babu Duggirala, Hyeonjeong Choe, Byeong Uk Jeon Bulletin of the Korean Chemical Society . 2019,第12期

机译：鉴定TRE-130作为泛egfr突变体的可逆抑制剂，同时保留EGFR野生型活性
2. Activity of the EGFR-HER2 Dual Inhibitor Afatinib in EGFR-Mutant Lung Cancer Patients With Acquired Resistance to Reversible EGFR Tyrosine Kinase Inhibitors [J] . Landi Lorenza, Tiseo Marcello, Chiari Rita, Clinical lung cancer . 2014,第6期

机译：EGFR-突变型肺癌对可逆EGFR酪氨酸激酶抑制剂具有耐药性的EGFR突变型肺癌患者中EGFR-HER2双重抑制剂Afatinib的活性
3. Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR(L858R/T790M/C797S)) [J] . Shen Jiayi, Zhang Tao, Zhu Su-Jie, Journal of Medicinal Chemistry . 2019,第15期

机译：5-甲基吡啶吡啶酮衍生物的基于结构的设计，作为表皮生长因子受体三重突变体的新型野生型备用抑制剂（EGFR（L858R / T790M / C797S））
4. Proteomic analyses of EGFR-interacting proteins to elucidate differences in signal transduction downstream of lung cancer-specific mutant EGFRs [C] . Udayan Guha, Todd M. Greco, Abhilash Venugopalan, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2011

机译：EGFR-相互作用蛋白的蛋白质组学分析，以阐明肺癌特异性突变蛋白的信号转导差异
5. RB1 Loss Accelerates acquired Therapeutic Resistance in EGFR Mutant Lung Adenocarcinoma via Lineage Plasticity [D] . Zhang, Letian. 2021

机译：RB1损失通过谱系可塑性加速EGFR突变体肺腺癌的获得性抗性
6. The HSP90 inhibitor ganetespib potentiates the antitumor activity of EGFR tyrosine kinase inhibition in mutant and wild-type non-small cell lung cancer [O] . Donald L. Smith, Jaime Acquaviva, Manuel Sequeira, -1

机译：HSP90抑制剂ganetespib增强EGFR酪氨酸激酶抑制在突变型和野生型非小细胞肺癌中的抗肿瘤活性
7. Activity of the EGFR-HER2 Dual Inhibitor Afatinib in EGFR-Mutant Lung Cancer Patients With Acquired Resistance to Reversible EGFR Tyrosine Kinase Inhibitors [O] . Lorenza Landi, Marcello Tiseo, Rita Chiari, 2014

机译：EGFR-HER2双重抑制剂AFATINIB在EGFR-突变体肺癌患者中获得可逆EGFR酪氨酸激酶抑制剂的抗性

Identification of TRE‐130 as Reversible Inhibitor of Pan‐EGFR Mutants while Sparing EGFR Wild‐Type Activity

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