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Page 1
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
Sells TB, Chau R, Ecsedy JA, Gershman RE, Hoar K, Huck J, Janowick DA, Kadambi VJ, LeRoy PJ, Stirling M, Stroud SG, Vos TJ, Weatherhead GS, Wysong DR, Zhang M, Balani SK, Bolen JB, Manfredi MG, Claiborne CF. Sells TB, et al. Among authors: claiborne cf. ACS Med Chem Lett. 2015 Apr 22;6(6):630-4. doi: 10.1021/ml500409n. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101564 Free PMC article.
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase.
Manfredi MG, Ecsedy JA, Meetze KA, Balani SK, Burenkova O, Chen W, Galvin KM, Hoar KM, Huck JJ, LeRoy PJ, Ray ET, Sells TB, Stringer B, Stroud SG, Vos TJ, Weatherhead GS, Wysong DR, Zhang M, Bolen JB, Claiborne CF. Manfredi MG, et al. Among authors: claiborne cf. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. doi: 10.1073/pnas.0608798104. Epub 2007 Feb 23. Proc Natl Acad Sci U S A. 2007. PMID: 17360485 Free PMC article.
Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.
Manfredi MG, Ecsedy JA, Chakravarty A, Silverman L, Zhang M, Hoar KM, Stroud SG, Chen W, Shinde V, Huck JJ, Wysong DR, Janowick DA, Hyer ML, Leroy PJ, Gershman RE, Silva MD, Germanos MS, Bolen JB, Claiborne CF, Sells TB. Manfredi MG, et al. Among authors: claiborne cf. Clin Cancer Res. 2011 Dec 15;17(24):7614-24. doi: 10.1158/1078-0432.CCR-11-1536. Epub 2011 Oct 20. Clin Cancer Res. 2011. PMID: 22016509
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.
Langston SP, Grossman S, England D, Afroze R, Bence N, Bowman D, Bump N, Chau R, Chuang BC, Claiborne C, Cohen L, Connolly K, Duffey M, Durvasula N, Freeze S, Gallery M, Galvin K, Gaulin J, Gershman R, Greenspan P, Grieves J, Guo J, Gulavita N, Hailu S, He X, Hoar K, Hu Y, Hu Z, Ito M, Kim MS, Lane SW, Lok D, Lublinsky A, Mallender W, McIntyre C, Minissale J, Mizutani H, Mizutani M, Molchinova N, Ono K, Patil A, Qian M, Riceberg J, Shindi V, Sintchak MD, Song K, Soucy T, Wang Y, Xu H, Yang X, Zawadzka A, Zhang J, Pulukuri SM. Langston SP, et al. J Med Chem. 2021 Mar 11;64(5):2501-2520. doi: 10.1021/acs.jmedchem.0c01491. Epub 2021 Feb 25. J Med Chem. 2021. PMID: 33631934 Free article.
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.
Vos TJ, Caracoti A, Che JL, Dai M, Farrer CA, Forsyth NE, Drabic SV, Horlick RA, Lamppu D, Yowe DL, Balani S, Li P, Zeng H, Joseph IB, Rodriguez LE, Maguire MP, Patane MA, Claiborne CF. Vos TJ, et al. Among authors: claiborne cf. J Med Chem. 2004 Mar 25;47(7):1602-4. doi: 10.1021/jm034244g. J Med Chem. 2004. PMID: 15027849
An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer.
Soucy TA, Smith PG, Milhollen MA, Berger AJ, Gavin JM, Adhikari S, Brownell JE, Burke KE, Cardin DP, Critchley S, Cullis CA, Doucette A, Garnsey JJ, Gaulin JL, Gershman RE, Lublinsky AR, McDonald A, Mizutani H, Narayanan U, Olhava EJ, Peluso S, Rezaei M, Sintchak MD, Talreja T, Thomas MP, Traore T, Vyskocil S, Weatherhead GS, Yu J, Zhang J, Dick LR, Claiborne CF, Rolfe M, Bolen JB, Langston SP. Soucy TA, et al. Among authors: claiborne cf. Nature. 2009 Apr 9;458(7239):732-6. doi: 10.1038/nature07884. Nature. 2009. PMID: 19360080
Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ.
Brownell JE, Sintchak MD, Gavin JM, Liao H, Bruzzese FJ, Bump NJ, Soucy TA, Milhollen MA, Yang X, Burkhardt AL, Ma J, Loke HK, Lingaraj T, Wu D, Hamman KB, Spelman JJ, Cullis CA, Langston SP, Vyskocil S, Sells TB, Mallender WD, Visiers I, Li P, Claiborne CF, Rolfe M, Bolen JB, Dick LR. Brownell JE, et al. Among authors: claiborne cf. Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024. Mol Cell. 2010. PMID: 20129059 Free article.
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
Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).
Marsilje TH, Roses JB, Calderwood EF, Stroud SG, Forsyth NE, Blackburn C, Yowe DL, Miao W, Drabic SV, Bohane MD, Daniels JS, Li P, Wu L, Patane MA, Claiborne CF. Marsilje TH, et al. Among authors: claiborne cf. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3721-5. doi: 10.1016/j.bmcl.2004.05.003. Bioorg Med Chem Lett. 2004. PMID: 15203150
17 results