Rationally designed BCR-ABL kinase inhibitors for improved leukemia treatment via covalent and pro-/dual-drug targeting strategies
We have successfully developed a chemical biology approach to convert a known noncovalent BCR-ABL inhibitor into more potent and safer inhibitors through covalent and pro-/dual-drug targeting strategies. Our "OH-implant" approach and the resulting drug design strategies have general applicability and hold promise for improvement the performance of various other reported drugs/drug candidates, thereby providing advanced medicines for disease treatment.
Authors
- Liqian Gao (ORCID: https://orcid.org/0000-0002-0085-7683)
- Shao Qin Yao (ORCID: https://orcid.org/0000-0003-4715-769X)
- Liang Lou (ORCID: https://orcid.org/0009-0005-0318-1083)
- Qicai Xiao (ORCID: https://orcid.org/0000-0001-9383-4052)
- Xiao Dong (ORCID: https://orcid.org/0000-0002-4687-8324)
- Zhimin Zhang (ORCID: https://orcid.org/0000-0002-5088-5869)
- Jie Sun (ORCID: https://orcid.org/0000-0001-5869-1412)
- Chengjun Zhu (ORCID: https://orcid.org/0000-0002-2867-562X)
- Guanghui Tang (ORCID: https://orcid.org/0000-0003-4585-9161)
- Mingxi Gu
- Shu Xia (ORCID: https://orcid.org/0009-0002-6562-4204)
- Peng Chen (ORCID: https://orcid.org/0000-0002-0635-9220)
Institutions
- Shanghai University (CN)
- Shanghai University of Engineering Science (CN)
- Sun Yat-sen University (CN)
- Jinan University (CN)
- National University of Singapore (SG)
- Theranostics (New Zealand) (NZ)
Publication Details
- Journal
- Journal of Advanced Research
- Published
- 2024-09-08
- DOI
- https://doi.org/10.1016/j.jare.2024.09.008
- Citations
- 4
- Primary Topic
- Chronic Myeloid Leukemia Treatments
- Type
- article
- Field-Weighted Citation Impact
- 1.82
Funders
- National Natural Science Foundation of China
- Science and Technology Commission of Shanghai Municipality
- Natural Science Foundation of Guangdong Province
- Science, Technology and Innovation Commission of Shenzhen Municipality
- Guangxi Medical University
- Guangdong Provincial Pearl River Talents Program
- Science and Technology Innovation Plan Of Shanghai Science and Technology Commission