Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 → Methionine790 Mutant-Reference-Cited by-同舟云学术

Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 → Methionine790 Mutant

Published:2012-03-01 Issue:6 Volume:55 Page:2711-2723
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Chang Shaohua¹²,Zhang Lianwen³²,Xu Shilin¹²,Luo Jinfeng¹,Lu Xiaoyun¹,Zhang Zhang¹,Xu Tianfeng¹²,Liu Yingxue¹,Tu Zhengchao¹,Xu Yong¹,Ren Xiaomei¹,Geng Meiyu⁴,Ding Jian⁴,Pei Duanqing¹,Ding Ke¹

Affiliation:

1. Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China

2. Graduate School of Chinese Academy of Sciences, # 19 Yuquan Road, Beijing 100049, China

3. School of Life Science, University of Science and Technology of China, # 96 Jinzhai Road, Hefei 230026, China

4. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, # 555 Zu-Chong-Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm201591k

Reference43 articles.

1. NEW EMBO MEMBERS' REVIEW: The ErbB signaling network: receptor heterodimerization in development and cancer

2. EGFR Antagonists in Cancer Treatment

3. Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity

4. Kinetic Analysis of Epidermal Growth Factor Receptor Somatic Mutant Proteins Shows Increased Sensitivity to the Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, Erlotinib

5. Fluorouracil, Leucovorin, and Oxaliplatin With and Without Cetuximab in the First-Line Treatment of Metastatic Colorectal Cancer

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