Journal ArticleDOI
The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation
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TLDR
The recent advances in medicinal chemistry of fourth-generation EGFR-TKIs are discussed, as well as further discussed the clinical challenges and future prospects of treating patients with EGFR mutations resistant to third-generationEGFR- TKIs.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2021-01-15. It has received 34 citations till now. The article focuses on the topics: EGFR inhibitors & Epidermal growth factor receptor.read more
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Therapeutic potential and limitations of curcumin as antimetastatic agent.
Petr Dytrych,Zdeněk Kejík,Jan Hajduch,Robert Kaplánek,Katerina Vesela,Markéta Skaličková,Anna Venhauerová,David Hoskovec,Pavel Martásek,Milan Jakubek +9 more
TL;DR: In this paper , the potential of curcumin as an antimetastatic agent and potential mechanisms of its antimetastic activity are discussed. And possible strategies (curcumin formulation, optimization of the method of administration and modification of its structure motif) to overcome its limitation such as low solubility and bioactivity are also presented.
Journal ArticleDOI
Novel anilinopyrimidine derivatives as potential EGFRT790M/C797S Inhibitors: Design, Synthesis, biological activity study.
TL;DR: In this paper , a series of anilinopyrimidine derivatives targeting EGFRT790M/C797S were designed, synthesized, and evaluated in vitro for the inhibitory effect on triple mutations kinases and cell lines.
Journal ArticleDOI
Design, Synthesis, and Antitumor Activity Evaluation of 2,4,6-Trisubstituted Quinazoline Derivatives Containing Acrylamide
S. Lihong,Robbie Sittel +1 more
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Designing strategies, structural activity relationship and biological activity of recently developed nitrogen containing heterocyclic compounds as epidermal growth factor receptor tyrosinase inhibitors
TL;DR: In this article , the authors summarized the research progress of EGFR inhibitors to overcome the restrictions of presently available drugs by understanding the history, anatomy, mutation, and its role in different types of cancer.
Journal ArticleDOI
Consensus scoring model: A novel approach to the study of EGFR kinase inhibitors
TL;DR: In this paper , a total of twelve EGFR consensus scoring models were trained and compared to any single scoring function, model 3 exhibited potent scoring power for various types of EGFR inhibitors.
References
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Cancer statistics, 2017
TL;DR: The American Cancer Society estimates the numbers of new cancer cases and deaths that will occur in the United States in the current year and compiles the most recent data on cancer incidence, mortality, and survival.
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Non-small cell lung cancer, version 5.2017: Clinical practice guidelines in oncology
David S. Ettinger,Douglas E. Wood,Dara L. Aisner,Wallace Akerley,Jessica Bauman,Lucian R. Chirieac,Thomas A. D'Amico,Malcolm M. DeCamp,Thomas J. Dilling,Michael C. Dobelbower,Robert C. Doebele,Ramaswamy Govindan,Matthew A. Gubens,Mark Hennon,Leora Horn,Ritsuko Komaki,Rudy P. Lackner,Michael Lanuti,Ticiana A. Leal,Leah J. Leisch,Rogerio Lilenbaum,Jules Lin,Billy W. Loo,Renato Martins,Gregory A. Otterson,Karen L. Reckamp,Gregory J. Riely,Steven E. Schild,Theresa A. Shapiro,James P. Stevenson,Scott J. Swanson,Kurt Tauer,Stephen C. Yang,Kristina M. Gregory,Miranda Hughes +34 more
TL;DR: This selection from the NCCN Guidelines for Non-Small Cell Lung Cancer (NSCLC) focuses on targeted therapies and immunotherapies for metastatic NSCLC, because therapeutic recommendations are rapidly changing for metastasis disease.
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Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
Yong Jia,Cai-Hong Yun,Eun Young Park,Dalia Ercan,Mari Manuia,Jose Juarez,Chunxiao Xu,Kevin Rhee,Ting Chen,Haikuo Zhang,Sangeetha Palakurthi,Jaebong Jang,Gerald Lelais,Michael DiDonato,Badry Bursulaya,Pierre-Yves Michellys,Robert Epple,Thomas H. Marsilje,Matthew McNeill,Wenshuo Lu,Jennifer L. Harris,Bender Steven Lee,Kwok-Kin Wong,Pasi A. Jänne,Michael J. Eck +24 more
TL;DR: Rational discovery of EAI045 is described, an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild type receptor and shows dramatic synergy of cetuximab, an antibody therapeutic that blocks EGFR dimerization, rendering the kinase uniformly susceptible to theAllosteric agent.
Journal ArticleDOI
The allelic context of the C797S mutation acquired upon treatment with third generation EGFR inhibitors impacts sensitivity to subsequent treatment strategies
Matthew J. Niederst,Haichuan Hu,Hillary E. Mulvey,Elizabeth L. Lockerman,Angel R. Garcia,Zofia Piotrowska,Lecia V. Sequist,Jeffrey A. Engelman +7 more
TL;DR: The results demonstrate that the allelic context in which C797S was acquired may predict responsiveness to alternative treatments, and are a novel mechanism of acquired resistance to third-generation TKIs.
Journal ArticleDOI
Investigating Novel Resistance Mechanisms to Third-Generation EGFR Tyrosine Kinase Inhibitor Osimertinib in Non–Small Cell Lung Cancer Patients
Zhe Yang,Nong Yang,Qiuxiang Ou,Yi Xiang,Tao Jiang,Xue Wu,Hua Bao,Xiaoling Tong,Xiaonan Wang,Yang W. Shao,Yunpeng Liu,Yan Wang,Caicun Zhou +12 more
TL;DR: Novel secondary mutations of EGFR L718 and L792 residues confer osimertinib resistance, both in vitro and in vivo, and are of great clinical and pharmaceutical relevance.