[HTML][HTML] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives
L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …
Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis
CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …
including cancer, has fostered incremental efforts on drug discovery programs over the past …
[HTML][HTML] Recent advances in non-small cell lung cancer targeted therapy; an update review
Lung cancer continues to be the leading cause of cancer-related death worldwide. In the last
decade, significant advancements in the diagnosis and treatment of lung cancer, particularly …
decade, significant advancements in the diagnosis and treatment of lung cancer, particularly …
ROS1-dependent cancers—biology, diagnostics and therapeutics
A Drilon, C Jenkins, S Iyer, A Schoenfeld… - Nature reviews Clinical …, 2021 - nature.com
The proto-oncogene ROS1 encodes a receptor tyrosine kinase with an unknown
physiological role in humans. Somatic chromosomal fusions involving ROS1 produce …
physiological role in humans. Somatic chromosomal fusions involving ROS1 produce …
[HTML][HTML] Molecular characterization of cancers with NTRK gene fusions
Z Gatalica, J Xiu, J Swensen, S Vranic - Modern Pathology, 2019 - Elsevier
Targeted inhibitors of neurotropic tyrosine kinases are highly effective in selected patients
with gene fusions involving NTRK1, NTRK2, or NTRK3. These fusions are consistently …
with gene fusions involving NTRK1, NTRK2, or NTRK3. These fusions are consistently …
Safety and antitumor activity of the multitargeted pan-TRK, ROS1, and ALK inhibitor entrectinib: combined results from two phase I trials (ALKA-372-001 and …
Entrectinib, a potent oral inhibitor of the tyrosine kinases TRKA/B/C, ROS1, and ALK, was
evaluated in two phase I studies in patients with advanced or metastatic solid tumors …
evaluated in two phase I studies in patients with advanced or metastatic solid tumors …
Entrectinib in ROS1 fusion-positive non-small-cell lung cancer: integrated analysis of three phase 1–2 trials
Background Recurrent gene fusions, such as ROS1 fusions, are oncogenic drivers of
various cancers, including non-small-cell lung cancer (NSCLC). Up to 36% of patients with …
various cancers, including non-small-cell lung cancer (NSCLC). Up to 36% of patients with …
Targeting ALK: precision medicine takes on drug resistance
JJ Lin, GJ Riely, AT Shaw - Cancer discovery, 2017 - AACR
Anaplastic lymphoma kinase (ALK) is a validated molecular target in several ALK-
rearranged malignancies, including non–small cell lung cancer. However, the clinical …
rearranged malignancies, including non–small cell lung cancer. However, the clinical …
The TP53 apoptotic network is a primary mediator of resistance to BCL2 inhibition in AML cells
To study mechanisms underlying resistance to the BCL2 inhibitor venetoclax in acute
myeloid leukemia (AML), we used a genome-wide CRISPR/Cas9 screen to identify gene …
myeloid leukemia (AML), we used a genome-wide CRISPR/Cas9 screen to identify gene …
[HTML][HTML] TRK inhibitors in TRK fusion-positive cancers
A Drilon - Annals of Oncology, 2019 - Elsevier
TRK fusions are oncogenic drivers of various adult and paediatric cancers. The first-
generation TRK inhibitors, larotrectinib and entrectinib, were granted landmark, tumour …
generation TRK inhibitors, larotrectinib and entrectinib, were granted landmark, tumour …