The Activity of Novel BCR‐ABL Small‐Molecule Degraders Containing Pyrimidine Rings and Their Role in Overcoming Drug Resistance

X Zhang, L Tu, H Chai, Z Li, Y Fu, X Zheng… - Journal of …, 2022 - Wiley Online Library
Inducing protein degradation by proteolysis‐targeting chimeras (PROTACs) has gained
tremendous momentum in the field for its promise in the discovery and development of new …

Proteolysis-Targeting Chimeras (PROTACs) targeting the BCR-ABL for the treatment of chronic myeloid leukemia–a patent review

ATS Vicente, JAR Salvador - Expert Opinion on Therapeutic …, 2023 - Taylor & Francis
ABSTRACT Introduction PROteolysis-TArgeting Chimeras (PROTACs) allow the selective
degradation of a protein of interest (POI) by the ubiquitin-proteasome system (UPS). With …

[HTML][HTML] Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation

L Jiang, Y Wang, Q Li, Z Tu, S Zhu, S Tu… - … Pharmaceutica Sinica B, 2021 - Elsevier
Bcr-Abl threonine 315 to isoleucine 315 (T315I) gatekeeper mutation induced drug
resistance remains an unmet clinical challenge for the treatment of chronic myeloid …

[HTML][HTML] Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity

D Lv, P Pal, X Liu, Y Jia, D Thummuri, P Zhang… - Nature …, 2021 - nature.com
Abstract PROteolysis-TArgeting Chimeras (PROTACs) have emerged as an innovative drug
development platform. However, most PROTACs have been generated empirically because …

[HTML][HTML] Single amino acid–based PROTACs trigger degradation of the oncogenic kinase BCR–ABL in chronic myeloid leukemia (CML)

J Zhang, C Ma, Y Yu, C Liu, L Fang, H Rao - Journal of Biological Chemistry, 2023 - ASBMB
Proteolysis-targeting chimera (PROTAC) that specifically targets harmful proteins for
destruction by hijacking the ubiquitin–proteasome system is emerging as a potent …

Breakthrough in degradation of BCR-ABL fusion protein for the treatment of cancer

RB Kargbo - ACS Medicinal Chemistry Letters, 2020 - ACS Publications
Disease Area. Cancer Biological Target. Fusion Protein BCR-ABL Summary. The fusion of
the BCR and ABL1 genes on the Philadelphia chromosome (Ph), arising from a reciprocal …

Global PROTAC toolbox for degrading BCR–ABL overcomes drug-resistant mutants and adverse effects

Y Yang, H Gao, X Sun, Y Sun, Y Qiu… - Journal of medicinal …, 2020 - ACS Publications
The BCR–ABL fusion oncoprotein causes chronic myeloid leukemia or acute lymphoblastic
leukemia in Ph+ patients because the ABL kinase is constitutively activated. However …

Development of a potent protein degrader against oncogenic BCR-ABL protein

N Shibata, N Ohoka, T Hattori, M Naito - … and Pharmaceutical Bulletin, 2019 - jstage.jst.go.jp
Chromosomal translocation occurs in some cancer cells, resulting in the expression of
aberrant oncogenic fusion proteins that include BCR-ABL in chronic myelogenous leukemia …

Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation

H Liu, X Ding, L Liu, Q Mi, Q Zhao, YB Shao… - European Journal of …, 2021 - Elsevier
Protein degradation is a promising strategy for drug development. Proteolysis-targeting
chimeras (PROTACs) hijacking the E3 ligase cereblon (CRBN) exhibit enormous potential …

Targeting oncoproteins for degradation by small molecules in myeloid leukemia

H Lei, W Wang, Y Wu - Leukemia & Lymphoma, 2018 - Taylor & Francis
Oncoproteins play a vital role in the pathogenesis of myeloid leukemia. Most targeted
therapies for myeloid leukemia are small molecules or monoclonal antibodies that inhibit the …