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Trends in kinase drug discovery: targets, indications and inhibitor design
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …
EGFR signaling pathway as therapeutic target in human cancers
Abstract Epidermal Growth Factor Receptor (EGFR) enacts major roles in the maintenance
of epithelial tissues. However, when EGFR signaling is altered, it becomes the grand …
of epithelial tissues. However, when EGFR signaling is altered, it becomes the grand …
Challenges and opportunities in cancer drug resistance
RA Ward, S Fawell, N Floc'h, V Flemington… - Chemical …, 2020 - ACS Publications
There has been huge progress in the discovery of targeted cancer therapies in recent years.
However, even for the most successful and impactful cancer drugs which have been …
However, even for the most successful and impactful cancer drugs which have been …
Discovery of BLU-945, a reversible, potent, and wild-type-sparing next-generation EGFR mutant inhibitor for treatment-resistant non-small-cell lung cancer
MS Eno, JD Brubaker, JE Campbell… - Journal of medicinal …, 2022 - ACS Publications
While epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have
changed the treatment landscape for EGFR mutant (L858R and ex19del)-driven non-small …
changed the treatment landscape for EGFR mutant (L858R and ex19del)-driven non-small …
20 years since the approval of first EGFR-TKI, gefitinib: Insight and foresight
Epidermal growth factor receptor (EGFR) actively involves in modulation of various cancer
progression related mechanisms including angiogenesis, differentiation and migration …
progression related mechanisms including angiogenesis, differentiation and migration …
EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research
RF Dong, ML Zhu, MM Liu, YT Xu, LL Yuan… - Pharmacological …, 2021 - Elsevier
With the development of precision medicine, molecular targeted therapy has been widely
used in the field of cancer, especially in non-small-cell lung cancer (NSCLC). Epidermal …
used in the field of cancer, especially in non-small-cell lung cancer (NSCLC). Epidermal …
Macrocycles and macrocyclization in anticancer drug discovery: Important pieces of the puzzle
C Zhang, F Liu, Y Zhang, C Song - European Journal of Medicinal …, 2024 - Elsevier
Increasing disease-related proteins have been identified as novel therapeutic targets.
Macrocycles are emerging as potential solutions, bridging the gap between conventional …
Macrocycles are emerging as potential solutions, bridging the gap between conventional …
CH7233163 overcomes osimertinib-resistant EGFR-Del19/T790M/C797S mutation
K Kashima, H Kawauchi, H Tanimura… - Molecular Cancer …, 2020 - aacrjournals.org
Osimertinib is the only EGFR-tyrosine kinase inhibitor (TKI) capable of overcoming EGFR-
T790M–mutated NSCLC, but osimertinib-resistant EGFR triple mutations …
T790M–mutated NSCLC, but osimertinib-resistant EGFR triple mutations …
Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors
Lung cancer is frequently caused by activating mutations in the epidermal growth factor
receptor (EGFR). Allosteric EGFR inhibitors offer promise as the next generation of …
receptor (EGFR). Allosteric EGFR inhibitors offer promise as the next generation of …
How many kinases are druggable? A review of our current understanding
There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …