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Page 1
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Duffey MO, Vos TJ, Adams R, Alley J, Anthony J, Barrett C, Bharathan I, Bowman D, Bump NJ, Chau R, Cullis C, Driscoll DL, Elder A, Forsyth N, Frazer J, Guo J, Guo L, Hyer ML, Janowick D, Kulkarni B, Lai SJ, Lasky K, Li G, Li J, Liao D, Little J, Peng B, Qian MG, Reynolds DJ, Rezaei M, Scott MP, Sells TB, Shinde V, Shi QJ, Sintchak MD, Soucy F, Sprott KT, Stroud SG, Nestor M, Visiers I, Weatherhead G, Ye Y, D'Amore N. Duffey MO, et al. Among authors: cullis c. J Med Chem. 2012 Jan 12;55(1):197-208. doi: 10.1021/jm2011172. Epub 2011 Dec 5. J Med Chem. 2012. PMID: 22070629
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. Mol Cell. 2010 Jan 15;37(1):102-11. doi: 10.1016/j.molcel.2009.12.024. Mol Cell. 2010. PMID: 20129059 Free article.
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. Nature. 2009 Apr 9;458(7239):732-6. doi: 10.1038/nature07884. Nature. 2009. PMID: 19360080
Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous Route.
Vyskocil S, Cardin D, Ciavarri J, Conlon J, Cullis C, England D, Gershman R, Gigstad K, Gipson K, Gould A, Greenspan P, Griffin R, Gulavita N, Harrison S, Hu Z, Hu Y, Hata A, Huang J, Huang SC, Janowick D, Jones M, Kolev V, Langston SP, Lee HM, Li G, Lok D, Ma L, Mai D, Malley J, Matsuda A, Mizutani H, Mizutani M, Molchanova N, Nunes E, Pusalkar S, Renou C, Rowland S, Sato Y, Shaw M, Shen L, Shi Z, Skene R, Soucy F, Stroud S, Xu H, Xu T, Abu-Yousif AO, Zhang J. Vyskocil S, et al. Among authors: cullis c. J Med Chem. 2021 May 27;64(10):6902-6923. doi: 10.1021/acs.jmedchem.1c00374. Epub 2021 May 17. J Med Chem. 2021. PMID: 34000802 Free article.
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Blackburn C, LaMarche MJ, Brown J, Che JL, Cullis CA, Lai S, Maguire M, Marsilje T, Geddes B, Govek E, Kadambi V, Doherty C, Dayton B, Brodjian S, Marsh KC, Collins CA, Kym PR. Blackburn C, et al. Among authors: cullis ca. Bioorg Med Chem Lett. 2006 May 15;16(10):2621-7. doi: 10.1016/j.bmcl.2006.02.044. Epub 2006 Mar 9. Bioorg Med Chem Lett. 2006. PMID: 16524729
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Kym PR, Iyengar R, Souers AJ, Lynch JK, Judd AS, Gao J, Freeman J, Mulhern M, Zhao G, Vasudevan A, Wodka D, Blackburn C, Brown J, Che JL, Cullis C, Lai SJ, LaMarche MJ, Marsilje T, Roses J, Sells T, Geddes B, Govek E, Patane M, Fry D, Dayton BD, Brodjian S, Falls D, Brune M, Bush E, Shapiro R, Knourek-Segel V, Fey T, McDowell C, Reinhart GA, Preusser LC, Marsh K, Hernandez L, Sham HL, Collins CA. Kym PR, et al. Among authors: cullis c. J Med Chem. 2005 Sep 22;48(19):5888-91. doi: 10.1021/jm050598r. J Med Chem. 2005. PMID: 16161992
Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4.
Blackburn C, Guan B, Brown J, Cullis C, Condon SM, Jenkins TJ, Peluso S, Ye Y, Gimeno RE, Punreddy S, Sun Y, Wu H, Hubbard B, Kaushik V, Tummino P, Sanchetti P, Yu Sun D, Daniels T, Tozzo E, Balani SK, Raman P. Blackburn C, et al. Among authors: cullis c. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3504-9. doi: 10.1016/j.bmcl.2006.03.102. Epub 2006 Apr 27. Bioorg Med Chem Lett. 2006. PMID: 16644217
66 results