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Orthogonal IMiD-Degron Pairs Induce Selective Protein Degradation in Cells.
Brennan PJ, Saunders RE, Spanou M, Serafini M, Sun L, Heger GP, Konopacka A, Beveridge RD, Gordon L, Bunally SB, Saudemont A, Benowitz AB, Martinez-Fleites C, Queisser MA, An H, Deane CM, Hann MM, Brayshaw LL, Conway SJ. Brennan PJ, et al. Among authors: benowitz ab. bioRxiv [Preprint]. 2024 Mar 16:2024.03.15.585309. doi: 10.1101/2024.03.15.585309. bioRxiv. 2024. PMID: 38559242 Free PMC article. Preprint.
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Among authors: benowitz ab. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Challenges and opportunities for in vivo PROTAC delivery.
Benowitz AB, Scott-Stevens PT, Harling JD. Benowitz AB, et al. Future Med Chem. 2022 Jan;14(3):119-121. doi: 10.4155/fmc-2021-0223. Epub 2021 Sep 16. Future Med Chem. 2022. PMID: 34528453 No abstract available.
Discovery and Characterisation of Highly Cooperative FAK-Degrading PROTACs.
Law RP, Nunes J, Chung CW, Bantscheff M, Buda K, Dai H, Evans JP, Flinders A, Klimaszewska D, Lewis AJ, Muelbaier M, Scott-Stevens P, Stacey P, Tame CJ, Watt GF, Zinn N, Queisser MA, Harling JD, Benowitz AB. Law RP, et al. Among authors: benowitz ab. Angew Chem Int Ed Engl. 2021 Oct 18;60(43):23327-23334. doi: 10.1002/anie.202109237. Epub 2021 Sep 17. Angew Chem Int Ed Engl. 2021. PMID: 34416073
The PROTACtable genome.
Schneider M, Radoux CJ, Hercules A, Ochoa D, Dunham I, Zalmas LP, Hessler G, Ruf S, Shanmugasundaram V, Hann MM, Thomas PJ, Queisser MA, Benowitz AB, Brown K, Leach AR. Schneider M, et al. Among authors: benowitz ab. Nat Rev Drug Discov. 2021 Oct;20(10):789-797. doi: 10.1038/s41573-021-00245-x. Epub 2021 Jul 20. Nat Rev Drug Discov. 2021. PMID: 34285415 Review.
A Phenotypic Approach for the Identification of New Molecules for Targeted Protein Degradation Applications.
Stacey P, Lithgow H, Lewell X, Konopacka A, Besley S, Green G, Whatling R, Law R, Röth S, Sapkota GP, Smith IED, Burley GA, Harling J, Benowitz AB, Queisser MA, Muelbaier M. Stacey P, et al. Among authors: benowitz ab. SLAS Discov. 2021 Aug;26(7):885-895. doi: 10.1177/24725552211017517. Epub 2021 May 27. SLAS Discov. 2021. PMID: 34041938 Free article.
The therapeutic potential of PROTACs.
Benowitz AB, Jones KL, Harling JD. Benowitz AB, et al. Expert Opin Ther Pat. 2021 Jan;31(1):1-24. doi: 10.1080/13543776.2021.1840553. Epub 2021 Jan 11. Expert Opin Ther Pat. 2021. PMID: 33081540 Review.
Structural Insights into PROTAC-Mediated Degradation of Bcl-xL.
Chung CW, Dai H, Fernandez E, Tinworth CP, Churcher I, Cryan J, Denyer J, Harling JD, Konopacka A, Queisser MA, Tame CJ, Watt G, Jiang F, Qian D, Benowitz AB. Chung CW, et al. Among authors: benowitz ab. ACS Chem Biol. 2020 Sep 18;15(9):2316-2323. doi: 10.1021/acschembio.0c00266. Epub 2020 Aug 13. ACS Chem Biol. 2020. PMID: 32697072
In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor.
Gilmartin AG, Groy A, Gore ER, Atkins C, Long ER, Montoute MN, Wu Z, Halsey W, McNulty DE, Ennulat D, Rueda L, Pappalardi M, Kruger RG, McCabe MT, Raoof A, Butlin R, Stowell A, Cockerill M, Waddell I, Ogilvie D, Luengo J, Jordan A, Benowitz AB. Gilmartin AG, et al. Among authors: benowitz ab. Haematologica. 2021 Jul 1;106(7):1979-1987. doi: 10.3324/haematol.2020.248658. Haematologica. 2021. PMID: 32586904 Free PMC article.
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2.
Mares A, Miah AH, Smith IED, Rackham M, Thawani AR, Cryan J, Haile PA, Votta BJ, Beal AM, Capriotti C, Reilly MA, Fisher DT, Zinn N, Bantscheff M, MacDonald TT, Vossenkamper A, Dace P, Churcher I, Benowitz AB, Watt G, Denyer J, Scott-Stevens P, Harling JD. Mares A, et al. Among authors: benowitz ab. Commun Biol. 2020 Mar 20;3(1):140. doi: 10.1038/s42003-020-0868-6. Commun Biol. 2020. PMID: 32198438 Free PMC article.
16 results