Overcoming IMiD resistance in T-cell lymphomas through potent degradation of ZFP91 and IKZF1.
Blood.
2022 Mar 31;139(13):2024-2037. doi: 10.1182/blood.2021014701. PubMed PMID:
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INK4 Tumor Suppressor Proteins Mediate Resistance to CDK4/6 Kinase Inhibitors.
Cancer Discov.
2022 Feb;12(2):356-371. doi: 10.1158/2159-8290.CD-20-1726. Epub 2021 Sep 20. PubMed PMID:
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Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216.
J Med Chem.
2022 Jan 13;65(1):747-756. doi: 10.1021/acs.jmedchem.1c01832. Epub 2021 Dec 29. PubMed PMID:
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Attenuated response to SARS-CoV-2 vaccine in patients with asymptomatic precursor stages of multiple myeloma and Waldenstrom macroglobulinemia.
Cancer Cell.
2022 Jan 10;40(1):6-8. doi: 10.1016/j.ccell.2021.12.003. Epub 2021 Dec 9. PubMed PMID:
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Potent Ikaros Degradation By the Cereblon E3 Ligase Modulator CC- 92480 Is Effective in Combination with Menin-MLL1 Inhibition in MLL1-Rearranged and NPM1-Mutant AML.
Blood. 2021 November; 138. doi: https://doi.org/10.1182/blood-2021-150971.
Chemo-proteomics exploration of HDAC degradability by small molecule degraders.
Cell Chem Biol.
2021 Oct 21;28(10):1514-1527.e4. doi: 10.1016/j.chembiol.2021.07.002. Epub 2021 Jul 26. PubMed PMID:
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Early cross-coronavirus reactive signatures of humoral immunity against COVID-19.
Sci Immunol.
2021 Oct 15;6(64):eabj2901. doi: 10.1126/sciimmunol.abj2901. Epub 2021 Oct 15. PubMed PMID:
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PMC8943686.
TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma.
Cancer Cell.
2021 Sep 13;39(9):1262-1278.e7. doi: 10.1016/j.ccell.2021.07.003. Epub 2021 Jul 29. PubMed PMID:
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Solenoid architecture of HUWE1 contributes to ligase activity and substrate recognition.
Mol Cell.
2021 Sep 2;81(17):3468-3480.e7. doi: 10.1016/j.molcel.2021.06.032. Epub 2021 Jul 26. PubMed PMID:
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Targeted Degradation of the Oncogenic Phosphatase SHP2.
Biochemistry.
2021 Aug 31;60(34):2593-2609. doi: 10.1021/acs.biochem.1c00377. Epub 2021 Aug 19. PubMed PMID:
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PMC8410664.
METTL1-mediated m7G modification of Arg-TCT tRNA drives oncogenic transformation.
Mol Cell.
2021 Aug 19;81(16):3323-3338.e14. doi: 10.1016/j.molcel.2021.06.031. Epub 2021 Aug 4. PubMed PMID:
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PMC8380730.
Selective degradation-inducing probes for studying cereblon (CRBN) biology.
RSC Med Chem.
2021 Aug 18;12(8):1381-1390. doi: 10.1039/d0md00382d. eCollection 2021 Aug 18. PubMed PMID:
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PMC8372211.
Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development.
ACS Med Chem Lett.
2021 Aug 12;12(8):1302-1307. doi: 10.1021/acsmedchemlett.1c00285. eCollection 2021 Aug 12. PubMed PMID:
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PMC8366001.
Structure-Guided Design of a "Bump-and-Hole" Bromodomain-Based Degradation Tag.
J Med Chem.
2021 Aug 12;64(15):11637-11650. doi: 10.1021/acs.jmedchem.1c00958. Epub 2021 Jul 19. PubMed PMID:
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Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2.
Angew Chem Int Ed Engl.
2021 Jul 12;60(29):15905-15911. doi: 10.1002/anie.202101328. Epub 2021 Jun 14. PubMed PMID:
33915015; PubMed Central PMCID:
PMC8324087.
A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders.
Eur J Med Chem.
2021 Jul 5;219:113435. doi: 10.1016/j.ejmech.2021.113435. Epub 2021 Apr 8. PubMed PMID:
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PMC8846605.
Local Deuteration Enables NMR Observation of Methyl Groups in Proteins from Eukaryotic and Cell-Free Expression Systems.
Angew Chem Int Ed Engl.
2021 Jun 14;60(25):13783-13787. doi: 10.1002/anie.202016070. Epub 2021 May 6. PubMed PMID:
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Acute pharmacological degradation of Helios destabilizes regulatory T cells.
Nat Chem Biol.
2021 Jun;17(6):711-717. doi: 10.1038/s41589-021-00802-w. Epub 2021 May 25. PubMed PMID:
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Early cross-coronavirus reactive signatures of protective humoral immunity against COVID-19.
bioRxiv.
2021 May 12;. doi: 10.1101/2021.05.11.443609. PubMed PMID:
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PMC8132219.
Humoral signatures of protective and pathological SARS-CoV-2 infection in children.
Nat Med.
2021 Mar;27(3):454-462. doi: 10.1038/s41591-021-01263-3. Epub 2021 Feb 12. PubMed PMID:
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Targeting oncoproteins with a positive selection assay for protein degraders.
Sci Adv.
2021 Feb;7(6). doi: 10.1126/sciadv.abd6263. Print 2021 Feb. PubMed PMID:
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Proteomics-Based Identification of DUB Substrates Using Selective Inhibitors.
Cell Chem Biol.
2021 Jan 21;28(1):78-87.e3. doi: 10.1016/j.chembiol.2020.09.005. Epub 2020 Oct 1. PubMed PMID:
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Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins.
Cell Rep.
2021 Jan 5;34(1):108532. doi: 10.1016/j.celrep.2020.108532. PubMed PMID:
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Methods for Quantitative Assessment of Protein Degradation.
Methods Mol Biol.
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Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development.
Cell.
2020 Dec 10;183(6):1714-1731.e10. doi: 10.1016/j.cell.2020.10.038. Epub 2020 Dec 3. PubMed PMID:
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Small-molecule-induced polymerization triggers degradation of BCL6.
Nature.
2020 Dec;588(7836):164-168. doi: 10.1038/s41586-020-2925-1. Epub 2020 Nov 18. PubMed PMID:
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Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library.
ACS Chem Biol.
2020 Oct 16;15(10):2722-2730. doi: 10.1021/acschembio.0c00520. Epub 2020 Sep 28. PubMed PMID:
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Rapid 'mix and read' assay for scalable detection of SARS-CoV-2 antibodies in patient plasma.
medRxiv.
2020 Sep 3;. doi: 10.1101/2020.09.01.20184101. PubMed PMID:
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The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.
Nature.
2020 Sep;585(7824):293-297. doi: 10.1038/s41586-020-2374-x. Epub 2020 Jun 3. PubMed PMID:
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Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations.
Angew Chem Int Ed Engl.
2020 Aug 17;59(34):14481-14489. doi: 10.1002/anie.202003500. Epub 2020 Jul 9. PubMed PMID:
32510788; PubMed Central PMCID:
PMC7686272.
Development of CDK2 and CDK5 Dual Degrader TMX-2172.
Angew Chem Int Ed Engl.
2020 Aug 10;59(33):13865-13870. doi: 10.1002/anie.202004087. Epub 2020 Jun 3. PubMed PMID:
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Targeted protein degradation as a powerful research tool in basic biology and drug target discovery.
Nat Struct Mol Biol.
2020 Jul;27(7):605-614. doi: 10.1038/s41594-020-0438-0. Epub 2020 Jun 15. Review. PubMed PMID:
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Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.
ACS Med Chem Lett.
2020 Jun 11;11(6):1269-1273. doi: 10.1021/acsmedchemlett.0c00111. eCollection 2020 Jun 11. PubMed PMID:
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PMC7294706.
Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2.
Cell.
2020 Apr 30;181(3):702-715.e20. doi: 10.1016/j.cell.2020.03.051. Epub 2020 Apr 20. PubMed PMID:
32315619; PubMed Central PMCID:
PMC7397863.
Tubulin Resists Degradation by Cereblon-Recruiting PROTACs.
Cells.
2020 Apr 27;9(5). doi: 10.3390/cells9051083. PubMed PMID:
32349222; PubMed Central PMCID:
PMC7290497.
Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling.
Cell Chem Biol.
2020 Jan 16;27(1):66-73.e7. doi: 10.1016/j.chembiol.2019.11.014. Epub 2019 Dec 16. PubMed PMID:
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PMC6980747.
Development and Characterization of a Wee1 Kinase Degrader.
Cell Chem Biol.
2020 Jan 16;27(1):57-65.e9. doi: 10.1016/j.chembiol.2019.10.013. Epub 2019 Nov 14. PubMed PMID:
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Exploring Targeted Degradation Strategy for Oncogenic KRASG12C.
Cell Chem Biol.
2020 Jan 16;27(1):19-31.e6. doi: 10.1016/j.chembiol.2019.12.006. Epub 2019 Dec 26. PubMed PMID:
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Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15.
Nat Chem Biol.
2020 Jan;16(1):7-14. doi: 10.1038/s41589-019-0378-3. Epub 2019 Nov 4. PubMed PMID:
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Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations.
Nat Commun.
2019 Aug 1;10(1):3468. doi: 10.1038/s41467-019-11429-w. PubMed PMID:
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Bismaleimide cross-linked anthrax toxin forms functional octamers with high specificity in tumor targeting.
Protein Sci.
2019 Jun;28(6):1059-1070. doi: 10.1002/pro.3613. Epub 2019 Apr 17. PubMed PMID:
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Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.
Angew Chem Int Ed Engl.
2019 May 6;58(19):6321-6326. doi: 10.1002/anie.201901336. Epub 2019 Mar 29. PubMed PMID:
30802347; PubMed Central PMCID:
PMC7678623.
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models.
Elife.
2019 Mar 25;8. doi: 10.7554/eLife.45457. PubMed PMID:
30907729; PubMed Central PMCID:
PMC6450673.
Bruton tyrosine kinase degradation as a therapeutic strategy for cancer.
Blood.
2019 Feb 28;133(9):952-961. doi: 10.1182/blood-2018-07-862953. Epub 2018 Dec 13. PubMed PMID:
30545835; PubMed Central PMCID:
PMC6396177.
Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML.
Cell Chem Biol.
2019 Feb 21;26(2):300-306.e9. doi: 10.1016/j.chembiol.2018.11.006. Epub 2018 Dec 27. PubMed PMID:
30595531; PubMed Central PMCID:
PMC6444916.
Genome-wide screen identifies cullin-RING ligase machinery required for lenalidomide-dependent CRL4CRBN activity.
Blood.
2018 Sep 20;132(12):1293-1303. doi: 10.1182/blood-2018-01-821769. Epub 2018 Jul 24. PubMed PMID:
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PMC6148446.
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome.
Elife.
2018 Aug 1;7. doi: 10.7554/eLife.38430. PubMed PMID:
30067223; PubMed Central PMCID:
PMC6156078.
Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance.
Cell.
2018 Jul 12;174(2):300-311.e11. doi: 10.1016/j.cell.2018.06.026. PubMed PMID:
30007416; PubMed Central PMCID:
PMC6084792.
Plasticity in binding confers selectivity in ligand-induced protein degradation.
Nat Chem Biol.
2018 Jul;14(7):706-714. doi: 10.1038/s41589-018-0055-y. Epub 2018 Jun 11. PubMed PMID:
29892083; PubMed Central PMCID:
PMC6202246.
Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).
J Med Chem.
2018 May 10;61(9):4249-4255. doi: 10.1021/acs.jmedchem.7b01655. Epub 2018 Apr 24. PubMed PMID:
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PMC6294449.
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