PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies
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Several studies reported successful conversion of either a reversible ibrutinib scaffold or a different noncovalent analog derived from a previously published covalent BTK inhibitor into BTK degraders.
“Subsequently, several studies reported successful conversion of either a reversible ibrutinib scaffold 42,43 or a different noncovalent analog derived from a previously published covalent BTK inhibitor 44,45 into BTK degraders.”
From Bruton tyrosine kinase degradation as a therapeutic strategy for cancer (2019) · cites this paper as [43]
The C481S resistance mutation in BTK renders first-generation BTK inhibitors less effective.
“particularly because of emergence of the C481S resistance mutation in BTK that renders first-generation BTK inhibitors less effective169,170.”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [170]
P13I more effectively reduces viability of BTK-dependent wild-type and C418S BTK-expressing HBL-1 DLBCL cells compared to ibrutinib.
“More importantly, P13I more effectively reduced the viability of BTK-dependent wild-type and C418S BTK-expressing HBL-1 DLBCL cells compared to ibrutinib [117].”
From Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies (2020) · cites this paper as [117]
P13I efficiently degrades both wild-type and C418S BTK with DC50 values of 10 nM and 28 nM, respectively.
“Rao’s group reported a BTK degrader, named P13I, which efficiently degraded both wild-type and C418S BTK with DC50 values of 10 nM and 28 nM, respectively.”
From Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies (2020) · cites this paper as [117]
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- Authors
- Sun, Y., Zhao, X., Ding, N., Gao, H., Wu, Y., Yang, Y., Zhao, M., Hwang, J., Song, Y., Liu, W., & Rao, Y.
- Affiliations
- Tsinghua University (CN)
- Peking University Cancer Hospital (CN)
- Corresponding author
- Liu, Wanli
- Rao, Yu
- Venue
- Cell Research
- Published
- 2018-06-06
- Volume
- 28
- Issue
- 7
- Pages
- 779-781
- ISSN
- 1001-0602 (ISSN-L)
- 1748-7838
- PMC
- PMC6028582
- OpenAlex
- W2806694687
- Cited by
- 295
- References
- 12
- Citations by year
- 2026: 25 · 2025: 28 · 2024: 30 · 2023: 31 · 2022: 53 · 2021: 43 · 2020: 48 · 2019: 32 · 2018: 5
- FWCI
- 11.56
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Cell Research (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (#81573277, #81773567, 81622042, 81670187, 81622042, 81773567)
- Tsinghua University (100084)
- Ministry of Education, India
- Peking University
- 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
- PROTACs, Bruton's tyrosine kinase, BTK C481S mutation, ibrutinib resistance, B-cell malignancies, non-Hodgkin lymphoma, protein degradation, B cell receptor signaling, targeted protein degradation
- MeSH terms
- Protein Domains, Agammaglobulinaemia Tyrosine Kinase, Adenine, HeLa Cells, Humans, Mutation, Piperidines, Pyrazoles, Pyrimidines, Thalidomide, Lymphoma, B-Cell, Drug Resistance, Neoplasm, HEK293 Cells, Proteolysis
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