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Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S beta5-subunit.
Blackburn C, Gigstad KM, Hales P, Garcia K, Jones M, Bruzzese FJ, Barrett C, Liu JX, Soucy TA, Sappal DS, Bump N, Olhava EJ, Fleming P, Dick LR, Tsu C, Sintchak MD, Blank JL. Blackburn C, et al. Among authors: dick lr. Biochem J. 2010 Sep 15;430(3):461-76. doi: 10.1042/BJ20100383. Biochem J. 2010. PMID: 20632995 Free PMC article.
Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Blackburn C, Barrett C, Blank JL, Bruzzese FJ, Bump N, Dick LR, Fleming P, Garcia K, Hales P, Hu Z, Jones M, Liu JX, Sappal DS, Sintchak MD, Tsu C, Gigstad KM. Blackburn C, et al. Among authors: dick lr. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6581-6. doi: 10.1016/j.bmcl.2010.09.032. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20875739
Cleavage Specificity of Mycobacterium tuberculosis ClpP1P2 Protease and Identification of Novel Peptide Substrates and Boronate Inhibitors with Anti-bacterial Activity.
Akopian T, Kandror O, Tsu C, Lai JH, Wu W, Liu Y, Zhao P, Park A, Wolf L, Dick LR, Rubin EJ, Bachovchin W, Goldberg AL. Akopian T, et al. Among authors: dick lr. J Biol Chem. 2015 Apr 24;290(17):11008-20. doi: 10.1074/jbc.M114.625640. Epub 2015 Mar 10. J Biol Chem. 2015. PMID: 25759383 Free PMC article.
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.
Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA, Charron CL, Bruzzese F, Yang X, Zhao X, Huang SC, Hutton CA, Burrows JN, Winzeler EA, Avery VM, Dick LR, Tilley L. Xie SC, et al. Among authors: dick lr. J Med Chem. 2018 Nov 21;61(22):10053-10066. doi: 10.1021/acs.jmedchem.8b01161. Epub 2018 Nov 7. J Med Chem. 2018. PMID: 30373366 Free PMC article.
214 results