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920 results

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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: garcia k. 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: garcia k. 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
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: garcia k. 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: garcia k. 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
Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
Gould AE, Adams R, Adhikari S, Aertgeerts K, Afroze R, Blackburn C, Calderwood EF, Chau R, Chouitar J, Duffey MO, England DB, Farrer C, Forsyth N, Garcia K, Gaulin J, Greenspan PD, Guo R, Harrison SJ, Huang SC, Iartchouk N, Janowick D, Kim MS, Kulkarni B, Langston SP, Liu JX, Ma LT, Menon S, Mizutani H, Paske E, Renou CC, Rezaei M, Rowland RS, Sintchak MD, Smith MD, Stroud SG, Tregay M, Tian Y, Veiby OP, Vos TJ, Vyskocil S, Williams J, Xu T, Yang JJ, Yano J, Zeng H, Zhang DM, Zhang Q, Galvin KM. Gould AE, et al. Among authors: garcia k. J Med Chem. 2011 Mar 24;54(6):1836-46. doi: 10.1021/jm101479y. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341678
Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.
Duffey MO, Adams R, Blackburn C, Chau RW, Chen S, Galvin KM, Garcia K, Gould AE, Greenspan PD, Harrison S, Huang SC, Kim MS, Kulkarni B, Langston S, Liu JX, Ma LT, Menon S, Nagayoshi M, Rowland RS, Vos TJ, Xu T, Yang JJ, Yu S, Zhang Q. Duffey MO, et al. Among authors: garcia k. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4800-4. doi: 10.1016/j.bmcl.2010.06.113. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20634068
920 results