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Optimization of Covalent MKK7 Inhibitors via Crude Nanomole-Scale Libraries.
Gehrtz P, Marom S, Bührmann M, Hardick J, Kleinbölting S, Shraga A, Dubiella C, Gabizon R, Wiese JN, Müller MP, Cohen G, Babaev I, Shurrush K, Avram L, Resnick E, Barr H, Rauh D, London N. Gehrtz P, et al. J Med Chem. 2022 Aug 11;65(15):10341-10356. doi: 10.1021/acs.jmedchem.1c02206. Epub 2022 Jul 30. J Med Chem. 2022. PMID: 35912476 Free PMC article.
Targeting SRSF2 mutations in leukemia with RKI-1447: A strategy to impair cellular division and nuclear structure.
Su M, Fleischer T, Grosheva I, Horev MB, Olszewska M, Mattioli CC, Barr H, Plotnikov A, Carvalho S, Moskovich Y, Minden MD, Chapal-Ilani N, Wainstein A, Papapetrou EP, Dezorella N, Cheng T, Kaushansky N, Geiger B, Shlush LI. Su M, et al. iScience. 2024 Mar 6;27(4):109443. doi: 10.1016/j.isci.2024.109443. eCollection 2024 Apr 19. iScience. 2024. PMID: 38558935 Free PMC article.
Structural basis for producing selective MAP2K7 inhibitors.
Murakawa Y, Valter S, Barr H, London N, Kinoshita T. Murakawa Y, et al. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127546. doi: 10.1016/j.bmcl.2020.127546. Epub 2020 Sep 12. Bioorg Med Chem Lett. 2020. PMID: 32931911
Tunable Methacrylamides for Covalent Ligand Directed Release Chemistry.
Reddi RN, Resnick E, Rogel A, Rao BV, Gabizon R, Goldenberg K, Gurwicz N, Zaidman D, Plotnikov A, Barr H, Shulman Z, London N. Reddi RN, et al. J Am Chem Soc. 2021 Apr 7;143(13):4979-4992. doi: 10.1021/jacs.0c10644. Epub 2021 Mar 24. J Am Chem Soc. 2021. PMID: 33761747 Free PMC article.
Sulfamate Acetamides as Self-Immolative Electrophiles for Covalent Ligand-Directed Release Chemistry.
Reddi RN, Rogel A, Gabizon R, Rawale DG, Harish B, Marom S, Tivon B, Arbel YS, Gurwicz N, Oren R, David K, Liu J, Duberstein S, Itkin M, Malitsky S, Barr H, Katz BZ, Herishanu Y, Shachar I, Shulman Z, London N. Reddi RN, et al. J Am Chem Soc. 2023 Feb 15;145(6):3346-3360. doi: 10.1021/jacs.2c08853. Epub 2023 Feb 4. J Am Chem Soc. 2023. PMID: 36738297 Free PMC article.
Specific quinone reductase 2 inhibitors reduce metabolic burden and reverse Alzheimer's disease phenotype in mice.
Gould NL, Scherer GR, Carvalho S, Shurrush K, Kayyal H, Edry E, Elkobi A, David O, Foqara M, Thakar D, Pavesi T, Sharma V, Walker M, Maitland M, Dym O, Albeck S, Peleg Y, Germain N, Babaev I, Sharir H, Lalzar M, Shklyar B, Hazut N, Khamaisy M, Lévesque M, Lajoie G, Avoli M, Amitai G, Lefker B, Subramanyam C, Shilton B, Barr H, Rosenblum K. Gould NL, et al. J Clin Invest. 2023 Oct 2;133(19):e162120. doi: 10.1172/JCI162120. J Clin Invest. 2023. PMID: 37561584 Free PMC article.
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