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 …

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 …

Discovery of asciminib (ABL001), an allosteric inhibitor of the tyrosine kinase activity of BCR-ABL1

J Schoepfer, W Jahnke, G Berellini, S Buonamici… - 2018 - ACS Publications
Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1
oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the ATP-binding site have …

European LeukemiaNet recommendations for the management of chronic myeloid leukemia: 2013

M Baccarani, MW Deininger, G Rosti… - Blood, The Journal …, 2013 - ashpublications.org
Advances in chronic myeloid leukemia treatment, particularly regarding tyrosine kinase
inhibitors, mandate regular updating of concepts and management. A European …

Mechanisms and insights into drug resistance in cancer

H Zahreddine, KLB Borden - Frontiers in pharmacology, 2013 - frontiersin.org
Cancer drug resistance continues to be a major impediment in medical oncology. Clinically,
resistance can arise prior to or as a result of cancer therapy. In this review, we discuss …

Ten things you should know about protein kinases: IUPHAR R eview 14

D Fabbro, SW Cowan‐Jacob… - British journal of …, 2015 - Wiley Online Library
Many human malignancies are associated with aberrant regulation of protein or lipid
kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein …

Chronic myeloid leukemia: an update of concepts and management recommendations of European LeukemiaNet

M Baccarani, J Cortes, F Pane… - Journal of clinical …, 2009 - ascopubs.org
Purpose To review and update the European LeukemiaNet (ELN) recommendations for the
management of chronic myeloid leukemia with imatinib and second-generation tyrosine …

BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on …

S Soverini, A Hochhaus, FE Nicolini… - Blood, The Journal …, 2011 - ashpublications.org
Abstract Mutations in the Bcr-Abl kinase domain may cause, or contribute to, resistance to
tyrosine kinase inhibitors (TKIs) in chronic myeloid leukemia patients. Recommendations …

[HTML][HTML] BCR-ABL1 compound mutations combining key kinase domain positions confer clinical resistance to ponatinib in Ph chromosome-positive leukemia

MS Zabriskie, CA Eide, SK Tantravahi, NA Vellore… - Cancer cell, 2014 - cell.com
Ponatinib is the only currently approved tyrosine kinase inhibitor (TKI) that suppresses all
BCR-ABL1 single mutants in Philadelphia chromosome-positive (Ph+) leukemia, including …

The specificity of asciminib, a potential treatment for chronic myeloid leukemia, as a myristate-pocket binding ABL inhibitor and analysis of its interactions with mutant …

PW Manley, L Barys, SW Cowan-Jacob - Leukemia research, 2020 - Elsevier
Asciminib is a potent, orally bioavailable, investigational drug that specifically and potently
inhibits the tyrosine kinase activity of native ABL1, together with that of the chimeric BCR …