Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy
Lung cancer is the second place among the global cancer population in term of the
morbidity and mortality, while non-small cell lung cancer (NSCLC) accounts for the largest …
morbidity and mortality, while non-small cell lung cancer (NSCLC) accounts for the largest …
Pitfalls and Considerations in Determining the Potency and Mutant Selectivity of Covalent Epidermal Growth Factor Receptor Inhibitors: Miniperspective
KW Hoyt, DA Urul, BC Ogboo, F Wittlinger… - Journal of Medicinal …, 2023 - ACS Publications
Enzyme inhibitors that form covalent bonds with their targets are being increasingly pursued
in drug development. Assessing their biochemical activity relies on time-dependent assays …
in drug development. Assessing their biochemical activity relies on time-dependent assays …
Targeting Epidermal Growth Factor Receptor for Cancer Treatment: Abolishing both Kinase-Dependent and Kinase-Independent Functions of the Receptor
Y Zhang - Pharmacological Reviews, 2023 - ASPET
Epidermal growth factor receptor (EGFR), a receptor tyrosine kinase, is activated by ligand
binding, overexpression, or mutation. It is well known for its tyrosine kinase-dependent …
binding, overexpression, or mutation. It is well known for its tyrosine kinase-dependent …
Discovery of novel allosteric EGFR L858R inhibitors for the treatment of non-small-cell lung cancer as a single agent or in combination with osimertinib
U Obst-Sander, A Ricci, B Kuhn, T Friess… - Journal of medicinal …, 2022 - ACS Publications
Addressing resistance to third-generation EGFR TKIs such as osimertinib via the
EGFRC797S mutation remains a highly unmet need in EGFR-driven non-small-cell lung …
EGFRC797S mutation remains a highly unmet need in EGFR-driven non-small-cell lung …
Discovery and optimization of 4-anilinoquinazoline derivatives spanning ATP binding site and allosteric site as effective EGFR-C797S inhibitors
D Dou, J Wang, Y Qiao, G Wumaier, W Sha, W Li… - European journal of …, 2022 - Elsevier
Epidermal growth factor receptor (EGFR) is an effective drug target for the treatment of non-
small cell lung cancer (NSCLC). However, a tertiary point mutation (C797S) at the ATP …
small cell lung cancer (NSCLC). However, a tertiary point mutation (C797S) at the ATP …
[HTML][HTML] Discovery and current developments of isoindolinone-based fungal natural products
C Bailly - European Journal of Medicinal Chemistry Reports, 2023 - Elsevier
Most fungi generate secondary metabolites essential to their growth or used as chemical
defense systems. They produce a large variety of small molecules, notably alkaloids …
defense systems. They produce a large variety of small molecules, notably alkaloids …
Chemical Scaffolds for the Clinical Development of Mutant-Selective and Reversible Fourth-Generation EGFR-TKIs in NSCLC
E Laudadio, L Mangano, C Minnelli - ACS Chemical Biology, 2024 - ACS Publications
In nonsmall cell lung cancer (NSCLC), as well as in other tumors, the targeted therapy is
mainly represented by tyrosine kinase inhibitors (TKIs), small molecules able to target …
mainly represented by tyrosine kinase inhibitors (TKIs), small molecules able to target …
Structural elements that enable specificity for mutant EGFR kinase domains with next-generation small-molecule inhibitors
Specificity for a desired enzyme target is an essential property of small-molecule inhibitors.
Molecules targeting oncogenic driver mutations in the epidermal growth factor receptor …
Molecules targeting oncogenic driver mutations in the epidermal growth factor receptor …
Next-generation EGFR tyrosine kinase inhibitors to overcome C797S mutation in non-small cell lung cancer (2019–2024)
D Das, L Xie, J Hong - RSC Medicinal Chemistry, 2024 - pubs.rsc.org
Lung cancer is a leading cause of cancer-related deaths worldwide. Non-small cell lung
cancer (NSCLC) accounts for the major portion (80–85%) of all lung cancer cases …
cancer (NSCLC) accounts for the major portion (80–85%) of all lung cancer cases …
A Constitutive EGFR Kinase Dimer to Study Inhibitor Pharmacology
Lung cancer is commonly caused by activating mutations in the epidermal growth factor
receptor (EGFR). Allosteric kinase inhibitors are unaffected by common ATP-site resistance …
receptor (EGFR). Allosteric kinase inhibitors are unaffected by common ATP-site resistance …