[HTML][HTML] Molecular targeted therapy for anticancer treatment
HY Min, HY Lee - Experimental & molecular medicine, 2022 - nature.com
Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …
Properties of FDA-approved small molecule protein kinase inhibitors
R Roskoski Jr - Pharmacological research, 2019 - Elsevier
Because mutations, overexpression, and dysregulation of protein kinases play essential
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most …
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most …
Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers
R Roskoski Jr - Pharmacological research, 2019 - Elsevier
The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …
owing to its general role in signal transduction and in oncogenesis. This family consists of …
[HTML][HTML] Intrinsic Resistance to EGFR-Tyrosine Kinase Inhibitors in EGFR-Mutant Non-Small Cell Lung Cancer: Differences and Similarities with Acquired Resistance
E Santoni-Rugiu, LC Melchior, EM Urbanska… - Cancers, 2019 - mdpi.com
Activating mutations in the epidermal growth factor receptor gene occur as early cancer-
driving clonal events in a subset of patients with non-small cell lung cancer (NSCLC) and …
driving clonal events in a subset of patients with non-small cell lung cancer (NSCLC) and …
[HTML][HTML] Structural insight and development of EGFR tyrosine kinase inhibitors
T Amelia, RE Kartasasmita, T Ohwada, DH Tjahjono - Molecules, 2022 - mdpi.com
Lung cancer has a high prevalence, with a growing number of new cases and mortality
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …
[HTML][HTML] Tyrosine kinase inhibitors for the treatment of EGFR mutation-positive non–small-cell lung cancer: a clash of the generations
R Shah, JF Lester - Clinical lung cancer, 2020 - Elsevier
The availability of 3 generations of epidermal growth factor receptor (EGFR) tyrosine kinase
inhibitors (TKIs) with different pharmacologic characteristics and clinical profiles has …
inhibitors (TKIs) with different pharmacologic characteristics and clinical profiles has …
Development of hypoxia-activated PROTAC exerting a more potent effect in tumor hypoxia than in normoxia
W Cheng, S Li, X Wen, S Han, S Wang, H Wei… - Chemical …, 2021 - pubs.rsc.org
Hypoxia is a hallmark of many solid tumors, and it causes the overexpression of a variety of
proteins including the epidermal growth factor receptor (EGFR). Many antitumor prodrugs …
proteins including the epidermal growth factor receptor (EGFR). Many antitumor prodrugs …
Orally effective FDA-approved protein kinase targeted covalent inhibitors (TCIs)
R Roskoski Jr - Pharmacological Research, 2021 - Elsevier
Because dysregulation of protein kinases owing to mutations or overexpression plays
causal roles in human diseases, this family of enzymes has become one of the most …
causal roles in human diseases, this family of enzymes has become one of the most …
Afatinib for the treatment of EGFR mutation-positive NSCLC: A review of clinical findings
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors represent the standard of
care in patients with EGFR mutation-positive (EGFR m+) non-small cell lung cancer …
care in patients with EGFR mutation-positive (EGFR m+) non-small cell lung cancer …
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 …