A small molecule inhibitor, OGP46, is effective against imatinib-resistant BCR-ABL mutations via the BCR-ABL/JAK-STAT pathway

L Wei, Y Yang, P Gupta, A Wang, M Zhao… - Molecular Therapy …, 2020 - cell.com
Chronic myeloid leukemia (CML) is caused by the Philadelphia (Ph+) chromosome carrying
the BCR-ABL oncogene, a constitutively active tyrosine kinase. The discovery of imatinib …

Preclinical development of a novel BCR-ABL T315I inhibitor against chronic myeloid leukemia

P Gupta, GN Zhang, AM Barbuti, X Zhang… - Cancer Letters, 2020 - Elsevier
Abstract Chronic Myeloid Leukemia (CML) is a myeloproliferative neoplasm primarily due to
the presence of the BCR-ABL fusion gene that produces the constitutively active protein …

Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia

E Weisberg, PW Manley, SW Cowan-Jacob… - Nature Reviews …, 2007 - nature.com
Imatinib, a small-molecule ABL kinase inhibitor, is a highly effective therapy for early-phase
chronic myeloid leukaemia (CML), which has constitutively active ABL kinase activity owing …

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML

T O'Hare, R Pollock, EP Stoffregen, JA Keats… - Blood, 2004 - ashpublications.org
The deregulated, oncogenic tyrosine kinase Bcr-Abl causes chronic myeloid leukemia
(CML). Imatinib mesylate (Gleevec, STI571), a Bcr-Abl kinase inhibitor, selectively inhibits …

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance

T O'Hare, WC Shakespeare, X Zhu, CA Eide… - Cancer cell, 2009 - cell.com
Inhibition of BCR-ABL by imatinib induces durable responses in many patients with chronic
myeloid leukemia (CML), but resistance attributable to kinase domain mutations can lead to …

Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571)

P La Rosée, AS Corbin, EP Stoffregen, MW Deininger… - Cancer research, 2002 - AACR
Imatinib mesylate, a selective inhibitor of the Abl tyrosine kinase, is effective as a single-
agent therapy for chronic myelogenous leukemia. However, resistance has been reported …

HS-438, a new inhibitor of imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia

SM Yun, KH Jung, SJ Kim, Z Fang, MK Son, HH Yan… - Cancer letters, 2014 - Elsevier
Imatinib is a selective breakpoint cluster region–Abelson (BCR-ABL) tyrosine kinase
inhibitor (TKI) that has significantly improved the prognosis of patients with chronic myeloid …

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 …

A winning combination against BCR–ABL

MH Flight - Nature Reviews Drug Discovery, 2010 - nature.com
In chronic myelogenous leukaemia (CML), a reciprocal translocation between chromosomes
9 and 22 results in a gene encoding BCR–ABL, a fused deregulated kinase that stimulates …

The second generation of BCR-ABL tyrosine kinase inhibitors

T Tauchi, K Ohyashiki - International journal of hematology, 2006 - Springer
Imatinib was developed as the first molecularly targeted therapy to specifically inhibit the
BCR-ABL kinase in Philadelphia chromosome (Ph)-positive chronic myeloid leukemia …