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Page 1
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Among authors: campobasso n. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.
Medina JR, Blackledge CW, Heerding DA, Campobasso N, Ward P, Briand J, Wright L, Axten JM. Medina JR, et al. Among authors: campobasso n. ACS Med Chem Lett. 2010 Jul 22;1(8):439-42. doi: 10.1021/ml100136n. eCollection 2010 Nov 11. ACS Med Chem Lett. 2010. PMID: 24900229 Free PMC article.
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.
Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI. Lin H, et al. Among authors: campobasso n. ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10. ACS Med Chem Lett. 2015. PMID: 26985301 Free PMC article.
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP, Scherzer D, Shu A, Bobko MA, Chadderton AR, Dumble M, Gardiner CM, Gilbert S, Liu Q, Rabindran SK, Sudakin V, Xiang H, Brady PG, Campobasso N, Ward P, Axten JM. Medina JR, et al. Among authors: campobasso n. J Med Chem. 2011 Mar 24;54(6):1871-95. doi: 10.1021/jm101527u. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341675
Characterization of Apo-Form Selective Inhibition of Indoleamine 2,3-Dioxygenase*.
Ortiz-Meoz RF, Wang L, Matico R, Rutkowska-Klute A, De la Rosa M, Bedard S, Midgett R, Strohmer K, Thomson D, Zhang C, Mebrahtu M, Guss J, Totoritis R, Consler T, Campobasso N, Taylor D, Lewis T, Weaver K, Muelbaier M, Seal J, Dunham R, Kazmierski W, Favre D, Bergamini G, Shewchuk L, Rendina A, Zhang G. Ortiz-Meoz RF, et al. Among authors: campobasso n. Chembiochem. 2021 Feb 2;22(3):516-522. doi: 10.1002/cbic.202000298. Epub 2020 Nov 16. Chembiochem. 2021. PMID: 32974990
Understanding the origins of time-dependent inhibition by polypeptide deformylase inhibitors.
Totoritis R, Duraiswami C, Taylor AN, Kerrigan JJ, Campobasso N, Smith KJ, Ward P, King BW, Murrayz-Thompson M, Jones AD, Van Aller GS, Aubart KM, Zalacain M, Thrall SH, Meek TD, Schwartz B. Totoritis R, et al. Among authors: campobasso n. Biochemistry. 2011 Aug 9;50(31):6642-54. doi: 10.1021/bi200655g. Biochemistry. 2011. PMID: 21711014
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ. Harris PA, et al. Among authors: campobasso n. J Med Chem. 2016 Mar 10;59(5):2163-78. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23. J Med Chem. 2016. PMID: 26854747
Structure-guided optimization of small molecule c-Abl activators.
Hong X, Cao P, Washio Y, Simpson G, Campobasso N, Yang J, Borthwick J, Burton G, Chabanet J, Bertrand S, Evans H, Young RJ, Qu J, Li H, Cottom J, Ward P, Zhang H, Ho T, Qin D, Christensen S, Head MS. Hong X, et al. Among authors: campobasso n. J Comput Aided Mol Des. 2014 Feb;28(2):75-87. doi: 10.1007/s10822-014-9731-5. Epub 2014 Feb 27. J Comput Aided Mol Des. 2014. PMID: 24573412 Free PMC article.
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Zuercher WJ, et al. Among authors: campobasso n. J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p. J Med Chem. 2010. PMID: 20345102
51 results