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Page 1
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. Among authors: fleming p. Nat Med. 2018 Feb;24(2):186-193. doi: 10.1038/nm.4474. Epub 2018 Jan 15. Nat Med. 2018. PMID: 29334375
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: fleming 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
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: fleming p. 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: fleming 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
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: fleming 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.
Precision Targeted Therapy with BLU-667 for RET-Driven Cancers.
Subbiah V, Gainor JF, Rahal R, Brubaker JD, Kim JL, Maynard M, Hu W, Cao Q, Sheets MP, Wilson D, Wilson KJ, DiPietro L, Fleming P, Palmer M, Hu MI, Wirth L, Brose MS, Ou SI, Taylor M, Garralda E, Miller S, Wolf B, Lengauer C, Guzi T, Evans EK. Subbiah V, et al. Among authors: fleming p. Cancer Discov. 2018 Jul;8(7):836-849. doi: 10.1158/2159-8290.CD-18-0338. Epub 2018 Apr 15. Cancer Discov. 2018. PMID: 29657135
An ALK2 inhibitor, BLU-782, prevents heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva.
Davis AJ, Brooijmans N, Brubaker JD, Stevison F, LaBranche TP, Albayya F, Fleming P, Hodous BL, Kim JL, Kim S, Lobbardi R, Palmer M, Sheets MP, Vassiliadis J, Wang R, Williams BD, Wilson D, Xu L, Zhu XJ, Bouchard K, Hunter JW, Graul C, Greenblatt E, Hussein A, Lyon M, Russo J, Stewart R, Dorsch M, Guzi TJ, Kadambi V, Lengauer C, Garner AP. Davis AJ, et al. Among authors: fleming p. Sci Transl Med. 2024 May 29;16(749):eabp8334. doi: 10.1126/scitranslmed.abp8334. Epub 2024 May 29. Sci Transl Med. 2024. PMID: 38809966
1,297 results