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 …

Response and resistance to BCR-ABL1-targeted therapies

TP Braun, CA Eide, BJ Druker - Cancer cell, 2020 - cell.com
Chronic myeloid leukemia (CML), caused by constitutively active BCR-ABL1 fusion tyrosine
kinase, has served as a paradigm for successful application of molecularly targeted cancer …

[HTML][HTML] Asciminib in chronic myeloid leukemia after ABL kinase inhibitor failure

TP Hughes, MJ Mauro, JE Cortes… - … England Journal of …, 2019 - Mass Medical Soc
Background Asciminib is an allosteric inhibitor that binds a myristoyl site of the BCR-ABL1
protein, locking BCR-ABL1 into an inactive conformation through a mechanism distinct from …

Modulating ROS to overcome multidrug resistance in cancer

Q Cui, JQ Wang, YG Assaraf, L Ren, P Gupta… - Drug Resistance …, 2018 - Elsevier
The successful treatment of cancer has significantly improved as a result of targeted therapy
and immunotherapy. However, during chemotherapy, cancer cells evolve and can acquire …

Anthracycline chemotherapy and cardiotoxicity

JV McGowan, R Chung, A Maulik, I Piotrowska… - … drugs and therapy, 2017 - Springer
Anthracycline chemotherapy maintains a prominent role in treating many forms of cancer.
Cardiotoxic side effects limit their dosing and improved cancer outcomes expose the cancer …

Acute lymphoblastic leukemia in children

SP Hunger, CG Mullighan - New England Journal of Medicine, 2015 - Mass Medical Soc
Acute Lymphoblastic Leukemia in Children | New England Journal of Medicine Skip to main
content The New England Journal of Medicine homepage Advanced Search SEARCH …

YAP/TAZ signaling and resistance to cancer therapy

CDK Nguyen, C Yi - Trends in cancer, 2019 - cell.com
Drug resistance is a major challenge in cancer treatment. Emerging evidence indicates that
deregulation of YAP/TAZ signaling may be a major mechanism of intrinsic and acquired …

[HTML][HTML] CRISPR/Cas9 for cancer research and therapy

T Zhan, N Rindtorff, J Betge, MP Ebert… - Seminars in cancer …, 2019 - Elsevier
CRISPR/Cas9 has become a powerful method for making changes to the genome of many
organisms. First discovered in bacteria as part of an adaptive immune system …

Oncogene ablation-resistant pancreatic cancer cells depend on mitochondrial function

A Viale, P Pettazzoni, CA Lyssiotis, H Ying, N Sánchez… - Nature, 2014 - nature.com
Pancreatic ductal adenocarcinoma (PDAC) is one of the deadliest cancers in western
countries, with a median survival of 6 months and an extremely low percentage of long-term …

[HTML][HTML] Cancer biomarker discovery and validation

N Goossens, S Nakagawa, X Sun… - Translational cancer …, 2015 - ncbi.nlm.nih.gov
With the emergence of genomic profiling technologies and selective molecular targeted
therapies, biomarkers play an increasingly important role in the clinical management of …