Cargando…

Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR

EGFR is a protein kinase whose aberrant activity is frequently involved in the development of non-small lung cancer (NSCLC) drug resistant forms. The allosteric inhibition of this enzyme is currently one among the most attractive approaches to design and develop anticancer drugs. In a previous study...

Descripción completa

Detalles Bibliográficos
Autores principales:	Foschi, Francesca, Tinivella, Annachiara, Crippa, Valentina, Pinzi, Luca, Mologni, Luca, Passarella, Daniele, Rastelli, Giulio
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Taylor & Francis 2022
Materias:	Brief Report
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9665079/ https://www.ncbi.nlm.nih.gov/pubmed/36373202 http://dx.doi.org/10.1080/14756366.2022.2145284

Ejemplares similares

Prediction of activity and selectivity profiles of human Carbonic Anhydrase inhibitors using machine learning classification models
por: Tinivella, Annachiara, et al.
Publicado: (2021)

Chemoinformatics Analyses of Tau Ligands Reveal Key Molecular Requirements for the Identification of Potential Drug Candidates against Tauopathies
por: Pinzi, Luca, et al.
Publicado: (2021)

Drug Repurposing and Polypharmacology to Fight SARS-CoV-2 Through Inhibition of the Main Protease
por: Pinzi, Luca, et al.
Publicado: (2021)

LigAdvisor: a versatile and user-friendly web-platform for drug design
por: Pinzi, Luca, et al.
Publicado: (2021)

Identification of potential biological targets of oxindole scaffolds via in silico repositioning strategies
por: Tinivella, Annachiara, et al.
Publicado: (2022)

Design and Synthesis of Hsp90 Inhibitors with B‐Raf and PDHK1 Multi‐Target Activity
por: Pinzi, Luca, et al.
Publicado: (2021)

On the Integration of In Silico Drug Design Methods for Drug Repurposing
por: March-Vila, Eric, et al.
Publicado: (2017)

Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFR(WT), EGFR(T790M), and EGFR(L858R))
por: Abo Al-Hamd, Mahmoud G., et al.
Publicado: (2023)

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells
por: Wu, Hong, et al.
Publicado: (2015)

YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFR(L858R, T790M)‐mutant resistance in vitro and in vivo
por: Zhang, Zhang, et al.
Publicado: (2018)

Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors
por: Jia, Yong, et al.
Publicado: (2016)

Simultaneous Detection of the T790M and L858R Mutations in the EGFR Gene by Oligoribonucleotide Interference-PCR
por: Baba, Keisuke, et al.
Publicado: (2019)

Differential MicroRNA Expression between EGFR T790M and L858R Mutated Lung Cancer
por: Kim, Ji Yeon, et al.
Publicado: (2018)

A Radiobrominated Tyrosine Kinase Inhibitor for EGFR with L858R/T790M Mutations in Lung Carcinoma
por: Fawwaz, Muammar, et al.
Publicado: (2021)

AI-Based Drug Discovery of TKIs Targeting L858R/T790M/C797S-Mutant EGFR in Non-small Cell Lung Cancer
por: Choi, Geunho, et al.
Publicado: (2021)

Leptomeningeal Metastatic L858R EGFR-mutant Lung Cancer: Prompt Response to Osimertinib in the Absence of T790M-mutation and Effective Subsequent Pulsed Erlotinib
por: Kanbour, Aladdin, et al.
Publicado: (2022)

Unusual metachronous lung adenocarcinomas harboring EGFR L858R/T790M mutations: A case report
por: Pei, Guotian, et al.
Publicado: (2020)

Synthesis of potent and selective HDAC6 inhibitors led to unexpected opening of a quinazoline ring
por: Moi, Davide, et al.
Publicado: (2022)

Computational identification of natural product inhibitors against EGFR double mutant (T790M/L858R) by integrating ADMET, machine learning, molecular docking and a dynamics approach
por: Agarwal, Subhash M., et al.
Publicado: (2022)

Computational polypharmacology comes of age
por: Rastelli, Giulio, et al.
Publicado: (2015)

Refinement and Rescoring of Virtual Screening Results
por: Rastelli, Giulio, et al.
Publicado: (2019)

Molecular Docking: Shifting Paradigms in Drug Discovery
por: Pinzi, Luca, et al.
Publicado: (2019)

Trends and Applications in Computationally Driven Drug Repurposing
por: Pinzi, Luca, et al.
Publicado: (2023)

Gossypol Inhibits Non-small Cell Lung Cancer Cells Proliferation by Targeting EGFR(L858R/T790M)
por: Wang, Yuwei, et al.
Publicado: (2018)

Design and Synthesis of New Hydantoin Acetanilide Derivatives as Anti-NSCLC Targeting EGFR(L858R/T790M) Mutations
por: Hassanin, Moamen A., et al.
Publicado: (2022)

De Novo T790M Mutation in an L858R Epidermal Growth Factor Receptor Mutant-Associated Lung Adenocarcinoma
por: Fujiwara, Takumi, et al.
Publicado: (2020)

Afatinib overcoming resistance to icotinib and osimertinib in NSCLC with leptomeningeal metastasis in patients with acquired EGFR L858R/T790M or L858R/S768I mutations: Two case reports
por: Li, Guangrui, et al.
Publicado: (2023)

Wighteone exhibits an antitumor effect against EGFR L858R/T790M mutation non-small cell lung cancer
por: Sun, Peiyuan, et al.
Publicado: (2021)

Deciphering the molecular mechanism of enhanced tumor activity of the EGFR variant T790M/L858R using melanoma cell lines
por: Shao, Hanshuang, et al.
Publicado: (2023)

Transtinib, a potent tyrosine kinase inhibitor inhibits L858R/T790M mutant NSCLC cell lines and xenografts
por: Hu, Peng, et al.
Publicado: (2016)

Identification of Promising Drug Candidates against Prostate Cancer through Computationally-Driven Drug Repurposing
por: Bernal, Leonardo, et al.
Publicado: (2023)

Development of machine learning classifiers to predict compound activity on prostate cancer cell lines
por: Bonanni, Davide, et al.
Publicado: (2022)

Ferumoxytol and CpG oligodeoxynucleotide 2395 synergistically enhance antitumor activity of macrophages against NSCLC with EGFR(L858R/T790M) mutation
por: Wang, Guoqun, et al.
Publicado: (2019)

Triple targeting of mutant EGFR(L858R/T790M), COX-2, and 15-LOX: design and synthesis of novel quinazolinone tethered phenyl urea derivatives for anti-inflammatory and anticancer evaluation
por: Kothayer, Hend, et al.
Publicado: (2023)

Design of Dual Inhibitors of Histone Deacetylase 6 and Heat Shock Protein 90
por: Pinzi, Luca, et al.
Publicado: (2020)

Promising Non-cytotoxic Monosubstituted Chalcones to Target Monoamine Oxidase-B
por: Iacovino, Luca G., et al.
Publicado: (2021)

Quinoxalinones as A Novel Inhibitor Scaffold for EGFR (L858R/T790M/C797S) Tyrosine Kinase: Molecular Docking, Biological Evaluations, and Computational Insights
por: Suriya, Utid, et al.
Publicado: (2022)

Repositioning Natural Products in Drug Discovery
por: Rastelli, Giulio, et al.
Publicado: (2020)

Combined therapy with EGFR TKI and gambogic acid for overcoming resistance in EGFR-T790M mutant lung cancer
por: WANG, CHENGDE, et al.
Publicado: (2015)

Mutational monitoring of EGFR T790M in cfDNA for clinical outcome prediction in EGFR-mutant lung adenocarcinoma
por: Su, Kang-Yi, et al.
Publicado: (2018)

Cannot write session to /tmp/vufind_sessions/sess_681qkmae73u3hskh9cpl1inljs