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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. Among authors: gabizon r. 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.
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: gabizon r. 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.
Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs.
Gabizon R, Shraga A, Gehrtz P, Livnah E, Shorer Y, Gurwicz N, Avram L, Unger T, Aharoni H, Albeck S, Brandis A, Shulman Z, Katz BZ, Herishanu Y, London N. Gabizon R, et al. J Am Chem Soc. 2020 Jul 8;142(27):11734-11742. doi: 10.1021/jacs.9b13907. Epub 2020 May 19. J Am Chem Soc. 2020. PMID: 32369353 Free PMC article.
A Fast and Clean BTK Inhibitor.
Gabizon R, London N. Gabizon R, et al. J Med Chem. 2020 May 28;63(10):5100-5101. doi: 10.1021/acs.jmedchem.0c00597. Epub 2020 May 13. J Med Chem. 2020. PMID: 32401033 Free PMC article. Review.
Hitting KRAS When It's Down.
Gabizon R, London N. Gabizon R, et al. J Med Chem. 2020 Jul 9;63(13):6677-6678. doi: 10.1021/acs.jmedchem.0c00785. Epub 2020 Jun 22. J Med Chem. 2020. PMID: 32568546 Free PMC article.
The rise of covalent proteolysis targeting chimeras.
Gabizon R, London N. Gabizon R, et al. Curr Opin Chem Biol. 2021 Jun;62:24-33. doi: 10.1016/j.cbpa.2020.12.003. Epub 2021 Feb 4. Curr Opin Chem Biol. 2021. PMID: 33549806 Review.
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. Among authors: gabizon r. 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.
126 results