Kinase drug discovery 20 years after imatinib: progress and future directions

P Cohen, D Cross, PA Jänne - Nature reviews drug discovery, 2021 - nature.com
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or
mutations in their genes, cause cancer and other diseases. Here, we review the remarkable …

[HTML][HTML] Anticancer drug resistance: An update and perspective

R Nussinov, CJ Tsai, H Jang - Drug Resistance Updates, 2021 - Elsevier
Driver mutations promote initiation and progression of cancer. Pharmacological treatment
can inhibit the action of the mutant protein; however, drug resistance almost invariably …

A phase 3, open-label, randomized study of asciminib, a STAMP inhibitor, vs bosutinib in CML after 2 or more prior TKIs

D Rea, MJ Mauro, C Boquimpani… - Blood, The Journal …, 2021 - ashpublications.org
Patients with chronic myeloid leukemia in chronic phase (CML-CP) resistant/intolerant to≥ 2
tyrosine kinase inhibitors (TKIs) are at high risk of experiencing poor outcomes because of …

Cancer multidrug-resistance reversal by ABCB1 inhibition: A recent update

K Engle, G Kumar - European journal of medicinal chemistry, 2022 - Elsevier
Chemotherapy is one of the most common treatments for cancer that uses one or more anti-
cancer drugs as a part of the standardized chemotherapy regimen. Cytotoxic chemicals …

An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer

C To, TS Beyett, J Jang, WW Feng, M Bahcall… - Nature cancer, 2022 - nature.com
Epidermal growth factor receptor (EGFR) therapy using small-molecule tyrosine kinase
inhibitors (TKIs) is initially efficacious in patients with EGFR-mutant lung cancer, although …

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 …

The leukaemia stem cell: similarities, differences and clinical prospects in CML and AML

D Vetrie, GV Helgason, M Copland - Nature Reviews Cancer, 2020 - nature.com
For two decades, leukaemia stem cells (LSCs) in chronic myeloid leukaemia (CML) and
acute myeloid leukaemia (AML) have been advanced paradigms for the cancer stem cell …

Chronic Myeloid Leukemia: Modern therapies, current challenges and future directions

AEG Osman, MW Deininger - Blood reviews, 2021 - Elsevier
Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm caused by a reciprocal
translocation [t (9; 22)(q34; q11. 2)] that leads to the fusion of ABL1 gene sequences (9q34) …

Resistance to tyrosine kinase inhibitors in chronic myeloid leukemia—from molecular mechanisms to clinical relevance

R Alves, AC Gonçalves, S Rutella, AM Almeida… - Cancers, 2021 - mdpi.com
Simple Summary Chronic myeloid leukemia (CML) is a myeloproliferative neoplasia
associated with a molecular alteration, the fusion gene BCR-ABL1, that encodes the tyrosine …

European LeukemiaNet laboratory recommendations for the diagnosis and management of chronic myeloid leukemia

NCP Cross, T Ernst, S Branford, JM Cayuela… - Leukemia, 2023 - nature.com
From the laboratory perspective, effective management of patients with chronic myeloid
leukemia (CML) requires accurate diagnosis, assessment of prognostic markers, sequential …