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
Citations
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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
Recent Development of the Second and Third Generation Irreversible Epidermal Growth Factor Receptor Inhibitors.
Weiwei Han,Yongli Du +1 more
TL;DR: A novel class of ‘third generation’ EGFR TKIs have been developed that is sensitising and T790M mutant‐specific whilst sparing WT EGFR, representing a significant breakthrough in the treatment in NSCLC patients with acquired resistance harboring these genotypes.
Journal ArticleDOI
Treatment in EGFR-mutated non-small cell lung cancer: how to block the receptor and overcome resistance mechanisms.
Claudia Proto,Giuseppe Lo Russo,Giulia Corrao,Monica Ganzinelli,Francesco Facchinetti,Roberta Minari,Marcello Tiseo,Marina Chiara Garassino +7 more
TL;DR: The aim of this review is to report recent advances and future perspectives in the treatment of EGFR-mutated NSCLC, highlighting the resistance mechanisms that underlie disease progression.
Journal ArticleDOI
Retrospective study of adjuvant icotinib in postoperative lung cancer patients harboring epidermal growth factor receptor mutations.
TL;DR: The efficacy and safety of adjuvant icotinib without chemotherapy in EGFR‐mutated NSCLC patients undergoing resection of stage IB–IIIA are assessed.
Patent
Spiro-aryl-phosphorus-oxygen compound as fourth generation of egfr kinase inhibitor
Wu Lingyun,Liu Xile,Ding Charles Z,Chen Shuhui,Hu Lihong,Zhao Lele,Pan Wei,Hu Guoping,Li Jian +8 more
TL;DR: In this paper, the fourth generation (T790M/C797S) mutation of an EGFR kinase inhibitor, i.e. a spiro-aryl-phosphorous-oxygen compound, was revealed.
Journal ArticleDOI
Osimertinib as first-line treatment of EGFR mutant advanced non-small-cell lung cancer.
TL;DR: The epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors (TKIs) gefitinib, erlotinib and afatinib are currently recommended for first-line treatment of patients with advanced non-small cell lung cancer harboring EGFR-TKI-sensitizing mutations ( EGFRm).