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83 results

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Page 1
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: hales p. 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
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: hales p. Biochem J. 2010 Sep 15;430(3):461-76. doi: 10.1042/BJ20100383. Biochem J. 2010. PMID: 20632995 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: hales p. 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.
Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer.
Kupperman E, Lee EC, Cao Y, Bannerman B, Fitzgerald M, Berger A, Yu J, Yang Y, Hales P, Bruzzese F, Liu J, Blank J, Garcia K, Tsu C, Dick L, Fleming P, Yu L, Manfredi M, Rolfe M, Bolen J. Kupperman E, et al. Among authors: hales p. Cancer Res. 2010 Mar 1;70(5):1970-80. doi: 10.1158/0008-5472.CAN-09-2766. Epub 2010 Feb 16. Cancer Res. 2010. PMID: 20160034
Genome-wide siRNA screen for modulators of cell death induced by proteasome inhibitor bortezomib.
Chen S, Blank JL, Peters T, Liu XJ, Rappoli DM, Pickard MD, Menon S, Yu J, Driscoll DL, Lingaraj T, Burkhardt AL, Chen W, Garcia K, Sappal DS, Gray J, Hales P, Leroy PJ, Ringeling J, Rabino C, Spelman JJ, Morgenstern JP, Lightcap ES. Chen S, et al. Among authors: hales p. Cancer Res. 2010 Jun 1;70(11):4318-26. doi: 10.1158/0008-5472.CAN-09-4428. Epub 2010 May 11. Cancer Res. 2010. PMID: 20460535
Preclinical evaluation of the antitumor activity of bortezomib in combination with vitamin C or with epigallocatechin gallate, a component of green tea.
Bannerman B, Xu L, Jones M, Tsu C, Yu J, Hales P, Monbaliu J, Fleming P, Dick L, Manfredi M, Claiborne C, Bolen J, Kupperman E, Berger A. Bannerman B, et al. Among authors: hales p. Cancer Chemother Pharmacol. 2011 Nov;68(5):1145-54. doi: 10.1007/s00280-011-1591-2. Epub 2011 Mar 13. Cancer Chemother Pharmacol. 2011. PMID: 21400028 Free PMC article.
Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome.
Xie SC, Metcalfe RD, Mizutani H, Puhalovich T, Hanssen E, Morton CJ, Du Y, Dogovski C, Huang SC, Ciavarri J, Hales P, Griffin RJ, Cohen LH, Chuang BC, Wittlin S, Deni I, Yeo T, Ward KE, Barry DC, Liu B, Gillett DL, Crespo-Fernandez BF, Ottilie S, Mittal N, Churchyard A, Ferguson D, Aguiar ACC, Guido RVC, Baum J, Hanson KK, Winzeler EA, Gamo FJ, Fidock DA, Baud D, Parker MW, Brand S, Dick LR, Griffin MDW, Gould AE, Tilley L. Xie SC, et al. Among authors: hales p. Proc Natl Acad Sci U S A. 2021 Sep 28;118(39):e2107213118. doi: 10.1073/pnas.2107213118. Proc Natl Acad Sci U S A. 2021. PMID: 34548400 Free PMC article.
Antitumor activity of the investigational proteasome inhibitor MLN9708 in mouse models of B-cell and plasma cell malignancies.
Lee EC, Fitzgerald M, Bannerman B, Donelan J, Bano K, Terkelsen J, Bradley DP, Subakan O, Silva MD, Liu R, Pickard M, Li Z, Tayber O, Li P, Hales P, Carsillo M, Neppalli VT, Berger AJ, Kupperman E, Manfredi M, Bolen JB, Van Ness B, Janz S. Lee EC, et al. Among authors: hales p. Clin Cancer Res. 2011 Dec 1;17(23):7313-23. doi: 10.1158/1078-0432.CCR-11-0636. Epub 2011 Sep 8. Clin Cancer Res. 2011. PMID: 21903769 Free PMC article.
83 results