Design and synthesis of novel bispecific molecules for inducing BRD4 protein degradation
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Compound 22f displayed potent anti-proliferative activity in RS4-11 leukemia cells.
“Interestingly, in an earlier report by the same group, a BI2536 derivative was used to build a PROTAC (compound 22f), which also displayed potent anti-proliferative activity in RS4-11 leukemia cells [146].”
From Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies (2020) · cites this paper as [146]
Compound 22f only degraded BRD4.
“In that study, compound 22f only degraded BRD4.”
From Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies (2020) · cites this paper as [146]
Cites
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Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
He, Y., Khan, S., Huo, Z., Lv, D., Zhang, X., Liu, X., Yuan, Y., Hromas, R., Xu, M., Zheng, G., et al. (2020) · Journal of Hematology & Oncology · doi:10.1186/s13045-020-00924-z · Cited by 126 · see citing works
- Authors
- Wang, S., Song, Y., Wang, Y., Gao, Y., Yu, S., Zhao, Q., Jin, X., & Lu, H.
- Affiliations
- Jilin University (CN)
- Corresponding author
- Jin, Xiangqun
- Lu, Haibin
- Venue
- Chemical Research in Chinese Universities
- Published
- 2018-01-03
- Volume
- 34
- Issue
- 1
- Pages
- 67-74
- ISSN
- 1005-9040 (ISSN-L)
- 2210-3171
- OpenAlex
- W2782495371
- Cited by
- 6
- References
- 15
- Citations by year
- 2024: 1 · 2023: 1 · 2020: 3 · 2019: 1
- FWCI
- 0.35
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Chemical Research in Chinese Universities (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Keywords
- PROTACs, BRD4, protein degradation, bispecific molecules, bromodomain inhibitors, linker design, RS4, cell proliferation inhibition
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Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
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