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Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening.
Resnick E, Bradley A, Gan J, Douangamath A, Krojer T, Sethi R, Geurink PP, Aimon A, Amitai G, Bellini D, Bennett J, Fairhead M, Fedorov O, Gabizon R, Gan J, Guo J, Plotnikov A, Reznik N, Ruda GF, Díaz-Sáez L, Straub VM, Szommer T, Velupillai S, Zaidman D, Zhang Y, Coker AR, Dowson CG, Barr HM, Wang C, Huber KVM, Brennan PE, Ovaa H, von Delft F, London N. Resnick E, et al. Among authors: barr hm. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22. J Am Chem Soc. 2019. PMID: 31060360 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.
An automatic pipeline for the design of irreversible derivatives identifies a potent SARS-CoV-2 Mpro inhibitor.
Zaidman D, Gehrtz P, Filep M, Fearon D, Gabizon R, Douangamath A, Prilusky J, Duberstein S, Cohen G, Owen CD, Resnick E, Strain-Damerell C, Lukacik P; Covid-Moonshot Consortium; Barr H, Walsh MA, von Delft F, London N. Zaidman D, et al. Cell Chem Biol. 2021 Dec 16;28(12):1795-1806.e5. doi: 10.1016/j.chembiol.2021.05.018. Epub 2021 Jun 25. Cell Chem Biol. 2021. PMID: 34174194 Free PMC article.
Site-Specific Labeling of Endogenous Proteins Using CoLDR Chemistry.
Reddi RN, Rogel A, Resnick E, Gabizon R, Prasad PK, Gurwicz N, Barr H, Shulman Z, London N. Reddi RN, et al. J Am Chem Soc. 2021 Dec 8;143(48):20095-20108. doi: 10.1021/jacs.1c06167. Epub 2021 Nov 24. J Am Chem Soc. 2021. PMID: 34817989 Free PMC article.
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.
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.
83 results