Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy

F Rossari, F Minutolo, E Orciuolo - Journal of hematology & oncology, 2018 - Springer
Bcr-Abl inhibitors paved the way of targeted therapy epoch. Imatinib was the first tyrosine
kinase inhibitor to be discovered with high specificity for Bcr-AblBcr-Abl-dependent and Bcr-Abl

BCR-ABL tyrosine kinase inhibitors for chronic myelogenous leukemia

CA Schiffer - New England Journal of Medicine, 2007 - Mass Medical Soc
… These more potent BCR-ABL inhibitors may have a more profound effect … Combinations of
BCR-ABL inhibitors, used either … There has been speculation that inhibition of normal tyrosine …

The ins and outs of bcr-abl inhibition

EP Reddy, AK Aggarwal - Genes & cancer, 2012 - journals.sagepub.com
inhibitors are active against many of the mutations in the Abl kinase that confer resistance to
imatinib. However, resistance remains a major problem, and new inhibitors … of Abl inhibition

[HTML][HTML] Flying under the radar: the new wave of BCRABL inhibitors

A Quintás-Cardama, H Kantarjian… - Nature Reviews Drug …, 2007 - nature.com
… negligible activity against the frequent BCRABL T315I mutation and modest … the ABL
kinase–imatinib complex have resulted in the synthesis of a new generation of BCRABL inhibitors

Molecular pathways: Bcr-abl

D Cilloni, G Saglio - Clinical Cancer Research, 2012 - AACR
… investigated the possibility of inhibiting BCR-ABL activity in a more … Several highly potent
next-generation BCR-ABL inhibitorsBCR-ABL and Src inhibitor, and potent selective BCR-ABL

Bcr-Abl tyrosine kinase inhibitors: a patent review

A Desogus, S Schenone, C Brullo… - Expert Opinion on …, 2015 - Taylor & Francis
… has prompted the search for novel Bcr-Abl inhibitors. … The body of the article deals with
Bcr-Abl inhibitors patented since … Overall, Bcr-Abl inhibitors constitute a very appealing research …

Bcr-Abl allosteric inhibitors: where we are and where we are going to

F Carofiglio, D Trisciuzzi, N Gambacorta, F Leonetti… - Molecules, 2020 - mdpi.com
… the discovery of new Bcr-Abl inhibitors based on allosteric control. … of the discovery of new
Bcr-Abl allosteric inhibitors. Next, we … of potential Bcr-Abl allosteric inhibitors whose structures, …

[HTML][HTML] 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
BCR-ABL inhibitors in clinical trials include ABL inhibitors (nilotinib), dual Src family and ABL
kinase inhibitors (… -ATP competitive inhibitors of BCR-ABL (ON012380) and Aurora kinase …

[HTML][HTML] Allosteric inhibitors of Bcr-abl–dependent cell proliferation

FJ Adrián, Q Ding, T Sim, A Velentza, C Sloan… - Nature chemical …, 2006 - nature.com
… To uncover new inhibitors of cellular Bcr-abl kinase, we performed a differential
cytotoxicity … new class of Bcr-abl inhibitors that possess excellent selectivity toward Bcr-abl–transformed …

New insights into small‐molecule inhibitors of BcrAbl

S Schenone, O Bruno, M Radi… - Medicinal research …, 2011 - Wiley Online Library
… act as dual inhibitors, targeting not only Bcr-Abl but also other … by the non-ATP-competitive
inhibitors, which may bind to the … Bcr-Abl ATP-competitive and non-ATP-competitive inhibitors