Cargando…

Characterization of Covalent-Reversible EGFR Inhibitors

[Image: see text] Within the spectrum of kinase inhibitors, covalent-reversible inhibitors (CRIs) provide a valuable alternative approach to classical covalent inhibitors. This special class of inhibitors can be optimized for an extended drug-target residence time. For CRIs, it was shown that the fa...

Descripción completa

Detalles Bibliográficos
Autores principales:	Smith, Steven, Keul, Marina, Engel, Julian, Basu, Debjit, Eppmann, Simone, Rauh, Daniel
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	American Chemical Society 2017
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6018958/ https://www.ncbi.nlm.nih.gov/pubmed/29963651 http://dx.doi.org/10.1021/acsomega.7b00157

Ejemplares similares

Reversible covalent direct thrombin inhibitors
por: Sivaraja, Mohanram, et al.
Publicado: (2018)

An update on the discovery and development of reversible covalent inhibitors
por: Faridoon, et al.
Publicado: (2023)

Naphthoquinones as Covalent Reversible Inhibitors of Cysteine Proteases—Studies on Inhibition Mechanism and Kinetics
por: Klein, Philipp, et al.
Publicado: (2020)

Covalent‐Allosteric Inhibitors to Achieve Akt Isoform‐Selectivity
por: Quambusch, Lena, et al.
Publicado: (2019)

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors
por: Vazquez‐Rodriguez, Saleta, et al.
Publicado: (2018)

Prolonged and tunable residence time using reversible covalent kinase inhibitors
por: Bradshaw, J. Michael, et al.
Publicado: (2015)

Overcoming EGFR(G724S)-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
por: Fassunke, Jana, et al.
Publicado: (2018)

Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors
por: Goebel, Lisa, et al.
Publicado: (2023)

Structure and Characterization of a Covalent Inhibitor of Src Kinase
por: Gurbani, Deepak, et al.
Publicado: (2020)

Covalent Reversible Inhibitors of Cysteine Proteases Containing the Nitrile Warhead: Recent Advancement in the Field of Viral and Parasitic Diseases
por: Brogi, Simone, et al.
Publicado: (2022)

Antibody-assisted target identification reveals afatinib, an EGFR covalent inhibitor, down-regulating ribonucleotide reductase
por: Yu, Cheng-Han, et al.
Publicado: (2018)

Covalent Allosteric Inhibitors of Akt Generated Using a Click Fragment Approach
por: van der Westhuizen, Leandi, et al.
Publicado: (2022)

Development of a Continuous Pulsed Electric Field (PEF) Vortex-Flow Chamber for Improved Treatment Homogeneity Based on Hydrodynamic Optimization
por: Schottroff, Felix, et al.
Publicado: (2020)

Optimization of Covalent MKK7 Inhibitors via Crude Nanomole-Scale Libraries
por: Gehrtz, Paul, et al.
Publicado: (2022)

Chitosan Functionalization: Covalent and Non-Covalent Interactions and Their Characterization
por: Nicolle, Laura, et al.
Publicado: (2021)

Structure-guided design and characterization of a clickable, covalent PARP16 inhibitor
por: Bejan, Daniel S., et al.
Publicado: (2022)

Non-covalent and reversible functionalization of carbon nanotubes
por: Di Crescenzo, Antonello, et al.
Publicado: (2014)

Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors
por: Zain, Rula, et al.
Publicado: (2021)

Assessing reversible and irreversible binding effects of kinase covalent inhibitors through ADP-Glo assays
por: Schröder, Martin, et al.
Publicado: (2021)

Mechanistic and thermodynamic characterization of oxathiazolones as potent and selective covalent immunoproteasome inhibitors
por: Mihalovits, Levente M., et al.
Publicado: (2021)

Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S
por: Lategahn, Jonas, et al.
Publicado: (2019)

Targeting Cytotoxic Agents through EGFR-Mediated Covalent Binding and Release
por: Morese, Pasquale A., et al.
Publicado: (2023)

Design and Synthesis of Non-Covalent Imidazo[1,2-a]quinoxaline-Based Inhibitors of EGFR and Their Anti-Cancer Assessment
por: Kumar, Manvendra, et al.
Publicado: (2021)

Rilzabrutinib, a reversible covalent Bruton's tyrosine kinase inhibitor: Absorption, metabolism, excretion, and absolute bioavailability in healthy participants
por: Ucpinar, Sibel, et al.
Publicado: (2023)

Characterization of the non-covalent interaction between the PF-07321332 inhibitor and the SARS-CoV-2 main protease
por: Macchiagodena, Marina, et al.
Publicado: (2022)

CovalentInDB: a comprehensive database facilitating the discovery of covalent inhibitors
por: Du, Hongyan, et al.
Publicado: (2020)

Semisynthetic Nanoreactor for Reversible Single-Molecule Covalent Chemistry
por: Lee, Joongoo, et al.
Publicado: (2016)

Reversible Covalent End‐Capping of Collagen Model Peptides
por: Priem, Christoph, et al.
Publicado: (2019)

Reversible Covalent Stabilization of Stacking Contacts in DNA Assemblies
por: Gerling, Thomas, et al.
Publicado: (2019)

Structural and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt
por: Uhlenbrock, Niklas, et al.
Publicado: (2019)

Cell‐Based Optimization of Covalent Reversible Ketoamide Inhibitors Bridging the Unprimed to the Primed Site of the Proteasome β5 Subunit
por: Stubba, Daniel, et al.
Publicado: (2019)

Designed switch from covalent to non-covalent inhibitors of carboxylesterase Notum activity
por: Atkinson, Benjamin N., et al.
Publicado: (2023)

Nucleotide based covalent inhibitors of KRas can only be efficient in vivo if they bind reversibly with GTP-like affinity
por: Müller, Matthias P., et al.
Publicado: (2017)

Reversal of EGFR inhibitors’ resistance by co-delivering EGFR and integrin αvβ3 inhibitors with nanoparticles in non-small cell lung cancer
por: He, Fei, et al.
Publicado: (2019)

Solid phase chemistry to covalently and reversibly capture thiolated RNA
por: Duffy, Erin E, et al.
Publicado: (2018)

Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs
por: Gabizon, Ronen, et al.
Publicado: (2020)

Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy
por: Yuan, Minghua, et al.
Publicado: (2021)

Close encounter of the covalent kind: Inhibiting MCL1’s proapoptotic activity with covalent inhibitors
por: Lessene, Guillaune
Publicado: (2017)

Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1
por: Hall, Adrian, et al.
Publicado: (2022)

Mutational spectrum of acquired resistance to reversible versus irreversible EGFR tyrosine kinase inhibitors
por: Wagener-Ryczek, Svenja, et al.
Publicado: (2020)

Cannot write session to /tmp/vufind_sessions/sess_lhs1f75c14f37gn427jljp4t6p