Degradation of Bruton’s tyrosine kinase mutants by PROTACs for potential treatment of ibrutinib-resistant non-Hodgkin lymphomas
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Several potent BTK PROTACs aimed at targeting mutant BTK in ibrutinib-resistant B cell malignancies with improved cellular activities and in vivo potencies were reported.
“Subsequently, several potent BTK PROTACs aimed at targeting mutant BTK in ibrutinib-resistant B cell malignancies with improved cellular activities and possessing in vivo potencies were reported by different groups [7, 44, 118–120].”
From Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies (2020) · cites this paper as [118]
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References 19 · Cited by 148
- Authors
- Sun, Y., Ding, N., Song, Y., Yang, Z., Liu, W., Zhu, J., & Rao, Y.
- Affiliations
- Tsinghua University (CN)
- Peking University Cancer Hospital (CN)
- Center for Life Sciences (CN)
- Corresponding author
- Liu, Wanli
- Zhu, Jun
- Rao, Yu
- Venue
- Leukemia
- Published
- 2019-03-11
- Volume
- 33
- Issue
- 8
- Pages
- 2105-2110
- ISSN
- 0887-6924 (ISSN-L)
- 1476-5551
- OpenAlex
- W2921689597
- Cited by
- 148
- References
- 19
- Citations by year
- 2026: 6 · 2025: 21 · 2024: 14 · 2023: 12 · 2022: 37 · 2021: 30 · 2020: 23 · 2019: 5
- FWCI
- 8.10
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Leukemia (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Health Sciences › Medicine › Genetics › Chronic Lymphocytic Leukemia Research
- Health Sciences › Medicine › Pathology and Forensic Medicine › Lymphoma Diagnosis and Treatment
- Keywords
- Bruton's tyrosine kinase, BTK inhibitors, PROTACs, ibrutinib resistance, non-Hodgkin lymphoma, protein degradation, B-cell malignancies, targeted therapy
- MeSH terms
- Agammaglobulinaemia Tyrosine Kinase, Adenine, Humans, Mutation, Piperidines, Pyrazoles, Pyrimidines, Lymphoma, Large B-Cell, Diffuse, Drug Resistance, Neoplasm, Lymphoma, Mantle-Cell
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