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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Journal ArticleDOI
Acquired resistance to third-generation EGFR-TKIs and emerging next-generation EGFR inhibitors.
TL;DR: The molecular mechanisms underlying resistance to third-generation EGFR inhibitors and the ongoing efforts to address and overcome this chemoresistance are summarized.
Journal ArticleDOI
A sulfonyl fluoride derivative inhibits EGFRL858R/T790M/C797S by covalent modification of the catalytic lysine.
Francesca Ferlenghi,Laura Scalvini,Federica Vacondio,Riccardo Castelli,Nicole Bozza,Giuseppe Marseglia,Silvia Rivara,Alessio Lodola,Silvia La Monica,Roberta Minari,Pier Giorgio Petronini,Roberta Alfieri,Marcello Tiseo,Marco Mor +13 more
TL;DR: UPR1444 (compound 11) is a new sulfonyl fluoride derivative which potently and irreversibly inhibits EGFRL858R/T790M/C797S through the formation of a sulfonamide bond with the catalytic residue Lys745.
Journal ArticleDOI
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Hao Chen,Mengzhen Lai,Tao Zhang,Yuqing Chen,Linjiang Tong,Sujie Zhu,Yang Zhou,Xiaomei Ren,Jianping Ding,Hua Xie,Xiaoyun Lu,Ke Ding +11 more
TL;DR: The structure-based design of conformational constrained 4-(1-ethylsufonyl-3-indolyl)-2-phenylaminopyrimidines as new EGFRT790M/C797S inhibitors are reported by using a macrocyclization strategy to combat EGFRC797S-mediated resistance in NSCLC patients.
Journal ArticleDOI
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation.
TL;DR: The design and synthesis of a series of EGFR proteolysis-targeting chimeras (PROTACs) that can rapidly and potently induce EGFR degradation in Ba/F3 cells expressing the EGFRDel19/T790M/C797S mutant are presented.
Journal ArticleDOI
Recent advances in the development of EGFR degraders: PROTACs and LYTACs.
TL;DR: In this paper , the structural properties of EGFR, the inhibitors that have been developed against WT/mutated EGFR and then mainly focuses on the recent advances of EGfr-targeting degraders along with its limitations and unlimited prospects.
References
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Journal ArticleDOI
Editor named for new acs journal
TL;DR: Kiessling was named the first editor of ACS Chemical Biology as mentioned in this paper, a journal dedicated to the chemistry-biology interface, which was established by the American Chemical Society (ACS).
Journal Article
[Molecular targeted therapy--non-small-cell lung cancer and gefitinib].
TL;DR: In the future, there must demonstrated benefits of gefitinib treatment in prospective clinical trials by recruiting patients selected on the basis of biological characteristics, and it is also important to further elucidate various issues that include other determinants of g EFITinib sensitivity, other mechanisms of resistance to gef itinib or mechanisms or predictive factors of interstitial lung disease by close collaboration among clinicians and basic researchers.
Patent
N2,n4-diphenylpyrimidine-2,4-diamine derivative, method for preparing same, and pharmaceutical composition containing same as active ingredient for prevention or treatment of cancer
Lee Kwangho,Shin Inji,Gildon Choi,Chong Hak Chae,Choe Hyeon Jeong,Myoung Eun Jung,Byeong Uk Jeon,Byoung Chul Cho,Chae Won Park,Hwan Kim,Duggirala Krishna Babu +10 more
TL;DR: In this article, a N2,N4-diphenylpyrimidine-2, 4-diamine derivative was used as an active ingredient for the prevention or treatment of cancer.
Patent
Fourth-generation egfr tyrosine kinase inhibitor
Masatomo Iwao,Tsutomu Fukuda,Fumito Ishibashi,Yoshimasa Uehara,Naoyuki Nishiya,Yusukef Oku,Shingo Dan,Takao Yamori +7 more
TL;DR: In this paper, a compound represented by formula (I) [in the formula, X represents O or NH, R1 and R2 each independently represent a hydrogen atom or an optionally substituted hydrocarbon group, R3 and R4 each independently represented a hydrogen atoms, a halogen atom, and R5 and R6 each represented an optional substituted hydrocar group] (excluding compounds represented by the formula (II)) or a salt thereof.
Journal ArticleDOI
[Mechanisms of Resistance to the Third-generation Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors in Non-small Cell Lung Cancer].
Lianfang Ni,Ligong Nie +1 more
TL;DR: In this paper, the authors reviewed the principle mechanisms of acquired resistance to third-generation EGFR-TKIs in non-small cell lung cancer (NSCLC) and showed that acquired resistance inevitably develops after application of approximately 10 months.