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Page 1
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: sappal ds. 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
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: sappal ds. Biochem J. 2010 Sep 15;430(3):461-76. doi: 10.1042/BJ20100383. Biochem J. 2010. PMID: 20632995 Free PMC article.
Nedd8-activating enzyme inhibitor MLN4924 provides synergy with mitomycin C through interactions with ATR, BRCA1/BRCA2, and chromatin dynamics pathways.
Garcia K, Blank JL, Bouck DC, Liu XJ, Sappal DS, Hather G, Cosmopoulos K, Thomas MP, Kuranda M, Pickard MD, Liu R, Bandi S, Smith PG, Lightcap ES. Garcia K, et al. Among authors: sappal ds. Mol Cancer Ther. 2014 Jun;13(6):1625-35. doi: 10.1158/1535-7163.MCT-13-0634. Epub 2014 Mar 26. Mol Cancer Ther. 2014. PMID: 24672057
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: sappal ds. 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
A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment.
Hyer ML, Milhollen MA, Ciavarri J, Fleming P, Traore T, Sappal D, Huck J, Shi J, Gavin J, Brownell J, Yang Y, Stringer B, Griffin R, Bruzzese F, Soucy T, Duffy J, Rabino C, Riceberg J, Hoar K, Lublinsky A, Menon S, Sintchak M, Bump N, Pulukuri SM, Langston S, Tirrell S, Kuranda M, Veiby P, Newcomb J, Li P, Wu JT, Powe J, Dick LR, Greenspan P, Galvin K, Manfredi M, Claiborne C, Amidon BS, Bence NF. Hyer ML, et al. Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15. Nat Med. 2018. PMID: 29334375
Biological characterization of MLN944: a potent DNA binding agent.
Sappal DS, McClendon AK, Fleming JA, Thoroddsen V, Connolly K, Reimer C, Blackman RK, Bulawa CE, Osheroff N, Charlton P, Rudolph-Owen LA. Sappal DS, et al. Mol Cancer Ther. 2004 Jan;3(1):47-58. Mol Cancer Ther. 2004. PMID: 14749475