Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

@article{Huang2014DesignOP,
  title={Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.},
  author={Qinhua Huang and Ted W Johnson and Simon Bailey and Alexei Brooun and Kevin D Bunker and Benjamin J Burke and Michael R. Collins and Andrew S. Cook and J Jean Cui and Kevin N. Dack and Judith G Deal and Ya-li Deng and Dac Dinh and Lars D. Engstrom and Mingying He and Jacqui E. Hoffman and Robert L. Hoffman and Patrick S Johnson and Robert S Kania and Hieu Lam and Justine L. Lam and Phuong Thi‐Bich Le and Qiuhua Li and Laura Lingardo and Wei Liu and Melissa West Lu and Michele A. McTigue and Cynthia L Palmer and Paul Richardson and Neal W Sach and Hong Shen and Tod Smeal and Graham L Smith and Albert E Stewart and Sergei L Timofeevski and Konstantinos E Tsaparikos and Hongyu Wang and Huichun Zhu and Jinjiang Zhu and Helen Y. Zou and Martin P Edwards},
  journal={Journal of medicinal chemistry},
  year={2014},
  volume={57 4},
  pages={1170-87}
}
Crizotinib (1), an anaplastic lymphoma kinase (ALK) receptor tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration in 2011, is efficacious in ALK and ROS positive patients. Under pressure of crizotinib treatment, point mutations arise in the kinase domain of ALK, resulting in resistance and progressive disease. The successful application of both structure-based and lipophilic-efficiency-focused drug design resulted in aminopyridine 8e, which was potent across a broad panel… CONTINUE READING
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