Literature DB >> 31223440

Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFRL858R/T790M/C797S.

Qiannan Li1, Tao Zhang2, Shiliang Li1, Linjiang Tong2, Junyu Li1, Zhicheng Su1, Fang Feng2, Deheng Sun1, Yi Tong1, Xia Wang1, Zhenjiang Zhao1, Lili Zhu1, Jian Ding2, Honglin Li1, Hua Xie2, Yufang Xu1.   

Abstract

In this paper, we describe the discovery and optimization of a series of noncovalent reversible epidermal growth factor receptor inhibitors of EGFRL858R/T790M/C797S. One of the most promising compounds, 25g, inhibited the enzymatic activity of EGFRL858R/T790M/C797S with an IC50 value of 2.2 nM. Cell proliferation assays showed that 25g effectively and selectively inhibited the growth of EGFRL858R/T790M/C797S-dependent cells. This series of compounds, which occupy both the ATP binding site and the allosteric site of the EGFR kinase, may serve as a basis for the development of fourth-generation EGFR inhibitors for L858R/T790M/C797S mutants.

Entities:  

Year:  2019        PMID： 31223440      PMCID： PMC6580378          DOI： 10.1021/acsmedchemlett.8b00564

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  22 in total

1.  The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.

Authors:  Cai-Hong Yun; Kristen E Mengwasser; Angela V Toms; Michele S Woo; Heidi Greulich; Kwok-Kin Wong; Matthew Meyerson; Michael J Eck
Journal:  Proc Natl Acad Sci U S A       Date:  2008-01-28       Impact factor: 11.205

2.  Epidermal growth factor receptor expression and gene amplification in colorectal carcinoma: an immunohistochemical and chromogenic in situ hybridization study.

Authors:  Jinru Shia; David S Klimstra; Allan R Li; Jing Qin; Leonard Saltz; Julie Teruya-Feldstein; Muzaffar Akram; Ki Young Chung; Davis Yao; Philip B Paty; William Gerald; Beiyun Chen
Journal:  Mod Pathol       Date:  2005-10       Impact factor: 7.842

Review 3.  The role of adjuvant monoclonal antibody therapy for breast cancer: rationale and new studies.

Authors:  E A Perez
Journal:  Curr Oncol Rep       Date:  2001-11       Impact factor: 5.075

4.  Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer.

Authors:  Antonio Garofalo; Laurence Goossens; Amelie Lemoine; Amaury Farce; Yannick Arlot; Patrick Depreux
Journal:  J Enzyme Inhib Med Chem       Date:  2010-04       Impact factor: 5.051

Review 5.  Epidermal growth factor receptor mutations in lung cancer.

Authors:  Sreenath V Sharma; Daphne W Bell; Jeffrey Settleman; Daniel A Haber
Journal:  Nat Rev Cancer       Date:  2007-03       Impact factor: 60.716

6.  United States Food and Drug Administration Drug Approval summary: Gefitinib (ZD1839; Iressa) tablets.

Authors:  Martin H Cohen; Grant A Williams; Rajeshwari Sridhara; Gang Chen; W David McGuinn; David Morse; Sophia Abraham; Atiqur Rahman; Chenyi Liang; Richard Lostritto; Amy Baird; Richard Pazdur
Journal:  Clin Cancer Res       Date:  2004-02-15       Impact factor: 12.531

7.  Epidermal growth factor receptor protein expression and gene amplification in small cell carcinoma of the urinary bladder.

Authors:  Xiaoyan Wang; Shaobo Zhang; Gregory T MacLennan; John N Eble; Antonio Lopez-Beltran; Ximing J Yang; Chong-Xian Pan; Honghong Zhou; Rodolfo Montironi; Liang Cheng
Journal:  Clin Cancer Res       Date:  2007-02-01       Impact factor: 12.531

Review 8.  Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitors.

Authors:  A F Gazdar
Journal:  Oncogene       Date:  2009-08       Impact factor: 9.867

9.  Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.

Authors:  Wenjun Zhou; Dalia Ercan; Liang Chen; Cai-Hong Yun; Danan Li; Marzia Capelletti; Alexis B Cortot; Lucian Chirieac; Roxana E Iacob; Robert Padera; John R Engen; Kwok-Kin Wong; Michael J Eck; Nathanael S Gray; Pasi A Jänne
Journal:  Nature       Date:  2009-12-24       Impact factor: 49.962

Review 10.  Vandetanib (ZD6474), a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) tyrosine kinases: current status and future directions.

Authors:  Alessandro Morabito; Maria Carmela Piccirillo; Fabiano Falasconi; Gianfranco De Feo; Antonia Del Giudice; Jane Bryce; Massimo Di Maio; Ermelinda De Maio; Nicola Normanno; Francesco Perrone
Journal:  Oncologist       Date:  2009-04-06
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  9 in total

Review 1.  Emerging strategies to overcome resistance to third-generation EGFR inhibitors.

Authors:  Kunyu Shi; Guan Wang; Junping Pei; Jifa Zhang; Jiaxing Wang; Liang Ouyang; Yuxi Wang; Weimin Li
Journal:  J Hematol Oncol       Date:  2022-07-15       Impact factor: 23.168

2.  Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites.

Authors:  Florian Wittlinger; David E Heppner; Ciric To; Marcel Günther; Bo Hee Shin; Jaimin K Rana; Anna M Schmoker; Tyler S Beyett; Lena M Berger; Benedict-Tilman Berger; Nicolas Bauer; James D Vasta; Cesear R Corona; Matthew B Robers; Stefan Knapp; Pasi A Jänne; Michael J Eck; Stefan A Laufer
Journal:  J Med Chem       Date:  2021-10-20       Impact factor: 8.039

Review 3.  Overcoming Cancer Drug Resistance Utilizing PROTAC Technology.

Authors:  Matthew R Burke; Alexis R Smith; Guangrong Zheng
Journal:  Front Cell Dev Biol       Date:  2022-04-25

Review 4.  Development of small molecule extracellular signal-regulated kinases (ERKs) inhibitors for cancer therapy.

Authors:  Xiaoli Pan; Junping Pei; Aoxue Wang; Wen Shuai; Lu Feng; Faqian Bu; Yumeng Zhu; Lan Zhang; Guan Wang; Liang Ouyang
Journal:  Acta Pharm Sin B       Date:  2022-01-04       Impact factor: 14.903

5.  Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.

Authors:  David E Heppner; Marcel Günther; Florian Wittlinger; Stefan A Laufer; Michael J Eck
Journal:  J Med Chem       Date:  2020-04-14       Impact factor: 7.446

6.  Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.

Authors:  Meng Cheng; Xufen Yu; Kaylene Lu; Ling Xie; Li Wang; Fanye Meng; Xiaoran Han; Xian Chen; Jing Liu; Yue Xiong; Jian Jin
Journal:  J Med Chem       Date:  2020-01-14       Impact factor: 7.446

7.  WX-0593 combined with an epithelial growth factor receptor (EGFR) monoclonal antibody in the treatment of xenograft tumors carrying triple EGFR mutations.

Authors:  Qingmei Zheng; Dongmei Chen; Xinmei Wang; Yingying Yang; Shuyong Zhao; Xin Dong; Cuicui Ma; Xin Zhang; Huicheng Duan; Yan Sun; Shansong Zheng
Journal:  Ann Transl Med       Date:  2022-06

8.  Untangling Dual-Targeting Therapeutic Mechanism of Epidermal Growth Factor Receptor (EGFR) Based on Reversed Allosteric Communication.

Authors:  Yuran Qiu; Xiaolan Yin; Xinyi Li; Yuanhao Wang; Qiang Fu; Renhua Huang; Shaoyong Lu
Journal:  Pharmaceutics       Date:  2021-05-18       Impact factor: 6.321

9.  Design and Synthesis of Non-Covalent Imidazo[1,2-a]quinoxaline-Based Inhibitors of EGFR and Their Anti-Cancer Assessment.

Authors:  Manvendra Kumar; Gaurav Joshi; Sahil Arora; Tashvinder Singh; Sajal Biswas; Nisha Sharma; Zahid Rafiq Bhat; Kulbhushan Tikoo; Sandeep Singh; Raj Kumar
Journal:  Molecules       Date:  2021-03-09       Impact factor: 4.411
  9 in total

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