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Using a Function-First "Scout Fragment"-Based Approach to Develop Allosteric Covalent Inhibitors of Conformationally Dynamic Helicase Mechanoenzymes.
Ramsey JR, Shelton PMM, Heiss TK, Olinares PDB, Vostal LE, Soileau H, Grasso M, Casebeer SW, Adaniya S, Miller M, Sun S, Huggins DJ, Myers RW, Chait BT, Vinogradova EV, Kapoor TM. Ramsey JR, et al. J Am Chem Soc. 2024 Jan 10;146(1):62-67. doi: 10.1021/jacs.3c10581. Epub 2023 Dec 22. J Am Chem Soc. 2024. PMID: 38134034
Structure of the γ-tubulin ring complex-capped microtubule.
Aher A, Urnavicius L, Xue A, Neselu K, Kapoor TM. Aher A, et al. bioRxiv [Preprint]. 2023 Nov 20:2023.11.20.567916. doi: 10.1101/2023.11.20.567916. bioRxiv. 2023. PMID: 38045257 Free PMC article. Updated. Preprint.
Using a function-first 'scout fragment'-based approach to develop allosteric covalent inhibitors of conformationally dynamic helicase mechanoenzymes.
Ramsey JR, Shelton PMM, Heiss TK, Olinares PDB, Vostal LE, Soileau H, Grasso M, Warrington S, Adaniya S, Miller M, Sun S, Huggins DJ, Myers RW, Chait BT, Vinogradova EV, Kapoor TM. Ramsey JR, et al. bioRxiv [Preprint]. 2023 Sep 26:2023.09.25.559391. doi: 10.1101/2023.09.25.559391. bioRxiv. 2023. PMID: 37808863 Free PMC article. Updated. Preprint.
Observing inhibition of the SARS-CoV-2 helicase at single-nucleotide resolution.
Marx SK, Mickolajczyk KJ, Craig JM, Thomas CA, Pfeffer AM, Abell SJ, Carrasco JD, Franzi MC, Huang JR, Kim HC, Brinkerhoff H, Kapoor TM, Gundlach JH, Laszlo AH. Marx SK, et al. Nucleic Acids Res. 2023 Sep 22;51(17):9266-9278. doi: 10.1093/nar/gkad660. Nucleic Acids Res. 2023. PMID: 37560916 Free PMC article.
33 results