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Page 1
Protein Degradation via CRL4CRBN Ubiquitin Ligase: Discovery and Structure-Activity Relationships of Novel Glutarimide Analogs That Promote Degradation of Aiolos and/or GSPT1.
Hansen JD, Condroski K, Correa M, Muller G, Man HW, Ruchelman A, Zhang W, Vocanson F, Crea T, Liu W, Lu G, Baculi F, LeBrun L, Mahmoudi A, Carmel G, Hickman M, Lu CC. Hansen JD, et al. J Med Chem. 2018 Jan 25;61(2):492-503. doi: 10.1021/acs.jmedchem.6b01911. Epub 2017 Apr 13. J Med Chem. 2018. PMID: 28358507
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J. Mathieu S, et al. Among authors: hansen jd. J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29. J Med Chem. 2012. PMID: 22335519
Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.
Chamberlain PP, D'Agostino LA, Ellis JM, Hansen JD, Matyskiela ME, McDonald JJ, Riggs JR, Hamann LG. Chamberlain PP, et al. Among authors: hansen jd. ACS Med Chem Lett. 2019 Nov 12;10(12):1592-1602. doi: 10.1021/acsmedchemlett.9b00425. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857833 Free PMC article.
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.
Hansen JD, Correa M, Nagy MA, Alexander M, Plantevin V, Grant V, Whitefield B, Huang D, Kercher T, Harris R, Narla RK, Leisten J, Tang Y, Moghaddam M, Ebinger K, Piccotti J, Havens CG, Cathers B, Carmichael J, Daniel T, Vessey R, Hamann LG, Leftheris K, Mendy D, Baculi F, LeBrun LA, Khambatta G, Lopez-Girona A. Hansen JD, et al. J Med Chem. 2020 Jul 9;63(13):6648-6676. doi: 10.1021/acs.jmedchem.9b01928. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32130004
CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells.
Surka C, Jin L, Mbong N, Lu CC, Jang IS, Rychak E, Mendy D, Clayton T, Tindall E, Hsu C, Fontanillo C, Tran E, Contreras A, Ng SWK, Matyskiela M, Wang K, Chamberlain P, Cathers B, Carmichael J, Hansen J, Wang JCY, Minden MD, Fan J, Pierce DW, Pourdehnad M, Rolfe M, Lopez-Girona A, Dick JE, Lu G. Surka C, et al. Blood. 2021 Feb 4;137(5):661-677. doi: 10.1182/blood.2020008676. Blood. 2021. PMID: 33197925 Free PMC article.
Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005.
Papa P, Whitefield B, Mortensen DS, Cashion D, Huang D, Torres E, Parnes J, Sapienza J, Hansen J, Correa M, Delgado M, Harris R, Hegde S, Norris S, Bahmanyar S, Plantevin-Krenitsky V, Liu Z, Leftheris K, Kulkarni A, Bennett B, Hur EM, Ringheim G, Khambatta G, Chan H, Muir J, Blease K, Burnett K, LeBrun L, Morrison L, Celeridad M, Khattri R, Cathers BE. Papa P, et al. J Med Chem. 2021 Aug 26;64(16):11886-11903. doi: 10.1021/acs.jmedchem.1c00388. Epub 2021 Aug 6. J Med Chem. 2021. PMID: 34355886
Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation.
Norris S, Ba X, Rhodes J, Huang D, Khambatta G, Buenviaje J, Nayak S, Meiring J, Reiss S, Xu S, Shi L, Whitefield B, Alexander M, Horn EJ, Correa M, Tehrani L, Hansen JD, Papa P, Mortensen DS. Norris S, et al. Among authors: hansen jd. J Med Chem. 2023 Dec 14;66(23):16388-16409. doi: 10.1021/acs.jmedchem.3c01848. Epub 2023 Nov 22. J Med Chem. 2023. PMID: 37991844
Correction to "Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation".
Norris S, Ba X, Rhodes J, Huang D, Khambatta G, Buenviaje J, Nayak S, Meiring J, Reiss S, Xu S, Shi L, Whitefield B, Alexander M, Horn EJ, Correa M, Tehrani L, Hansen JD, Papa P, Mortensen DS, Brazeau JF. Norris S, et al. Among authors: hansen jd. J Med Chem. 2024 Aug 22;67(16):14692. doi: 10.1021/acs.jmedchem.4c01356. Epub 2024 Aug 13. J Med Chem. 2024. PMID: 39137243 No abstract available.
Correction to "Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005".
Papa P, Whitefield B, Mortensen DS, Cashion D, Huang D, Torres E, Parnes J, Sapienza J, Hansen J, Correa M, Delgado M, Harris R, Hegde S, Norris S, Bahmanyar S, Plantevin-Krenitsky V, Liu Z, Leftheris K, Kulkarni A, Bennett B, Hur EM, Ringheim G, Khambatta G, Chan H, Muir J, Blease K, Burnett K, LeBrun L, Morrison L, Celeridad M, Khattri R, Cathers BE. Papa P, et al. J Med Chem. 2024 Dec 26;67(24):22344. doi: 10.1021/acs.jmedchem.4c02898. Epub 2024 Dec 12. J Med Chem. 2024. PMID: 39665782 No abstract available.
494 results