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-Abl protein resulting from t (9 …

Fibroblast growth factor receptors (FGFRs): structures and small molecule inhibitors

S Dai, Z Zhou, Z Chen, G Xu, Y Chen - Cells, 2019 - mdpi.com
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases
expressed on the cell membrane that play crucial roles in both developmental and adult …

Circumventing cancer drug resistance in the era of personalized medicine

LA Garraway, PA Jänne - Cancer discovery, 2012 - AACR
All successful cancer therapies are limited by the development of drug resistance. The
increase in the understanding of the molecular and biochemical bases of drug efficacy has …

Pushing the limits of targeted therapy in chronic myeloid leukaemia

T O'hare, MS Zabriskie, AM Eiring… - Nature Reviews …, 2012 - nature.com
Tyrosine kinase inhibitor (TKI) therapy targeting the BCR-ABL1 kinase is effective against
chronic myeloid leukaemia (CML), but is not curative for most patients. Minimal residual …

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

L Tan, J Wang, J Tanizaki, Z Huang… - Proceedings of the …, 2014 - National Acad Sciences
The human FGF receptors (FGFRs) play critical roles in various human cancers, and several
FGFR inhibitors are currently under clinical investigation. Resistance usually results from …

Mechanisms of drug resistance in kinases

R Barouch-Bentov, K Sauer - Expert opinion on investigational …, 2011 - Taylor & Francis
Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

Targeting the BCR-ABL signaling pathway in therapy-resistant Philadelphia chromosome-positive leukemia

T O'Hare, MWN Deininger, CA Eide, T Clackson… - Clinical Cancer …, 2011 - AACR
Beginning with imatinib a decade ago, therapy based on targeted inhibition of the BCR-ABL
kinase has greatly improved the prognosis for chronic myeloid leukemia (CML) patients. The …

Development of protein degradation inducers of oncogenic BCR‐ABL protein by conjugation of ABL kinase inhibitors and IAP ligands

N Shibata, N Miyamoto, K Nagai, K Shimokawa… - Cancer …, 2017 - Wiley Online Library
Chromosomal translocation occurs in some cancer cells, which results in the expression of
aberrant oncogenic fusion proteins that include BCR‐ABL in chronic myelogenous leukemia …

BCR::ABL1 Proteolysis-targeting chimeras (PROTACs): The new frontier in the treatment of Ph+ leukemias?

N Cruz-Rodriguez, H Tang, B Bateman, W Tang… - Leukemia, 2024 - nature.com
BCR:: ABL1 tyrosine kinase inhibitors (TKIs) have turned chronic myeloid leukemia (CML)
from a lethal condition into a chronic ailment. With optimal management, the survival of CML …

Resistant mutations in CML and Ph+ALL – role of ponatinib

GD Miller, BJ Bruno, CS Lim - Biologics: Targets and Therapy, 2014 - Taylor & Francis
In 2012, ponatinib (Iclusig®), an orally available pan-BCR-ABL tyrosine kinase inhibitor
(TKI) developed by ARIAD Pharmaceuticals, Inc., was approved by the US Food and Drug …