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Page 1
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: totoritis r. J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26355916
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.
Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L. Charnley AK, et al. Among authors: totoritis r. Bioorg Med Chem. 2015 Nov 1;23(21):7000-6. doi: 10.1016/j.bmc.2015.09.038. Epub 2015 Sep 25. Bioorg Med Chem. 2015. PMID: 26455654
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: totoritis rd. 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
The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase.
Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus R Jr, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB, Desai BM, Swift B, Capriotti CA, Berger SB, Mahajan MK, Reilly MA, Rivera EJ, Sun HH, Nagilla R, Beal AM, Finger JN, Cook MN, King BW, Ouellette MT, Totoritis RD, Pierdomenico M, Negroni A, Stronati L, Cucchiara S, Ziółkowski B, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Casillas LN. Haile PA, et al. Among authors: totoritis rd. J Med Chem. 2016 May 26;59(10):4867-80. doi: 10.1021/acs.jmedchem.6b00211. Epub 2016 May 4. J Med Chem. 2016. PMID: 27109867
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.
Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW. Harris PA, et al. Among authors: totoritis rd. J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2. J Med Chem. 2019. PMID: 31013427
Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity.
Concha NO, Smallwood A, Bonnette W, Totoritis R, Zhang G, Federowicz K, Yang J, Qi H, Chen S, Campobasso N, Choudhry AE, Shuster LE, Evans KA, Ralph J, Sweitzer S, Heerding DA, Buser CA, Su DS, DeYoung MP. Concha NO, et al. Among authors: totoritis r. Mol Pharmacol. 2015 Dec;88(6):1011-23. doi: 10.1124/mol.115.100917. Epub 2015 Oct 5. Mol Pharmacol. 2015. PMID: 26438213
Evaluation of an antibody-free ADP detection assay: ADP-Glo.
Li H, Totoritis RD, Lor LA, Schwartz B, Caprioli P, Jurewicz AJ, Zhang G. Li H, et al. Assay Drug Dev Technol. 2009 Dec;7(6):598-605. doi: 10.1089/adt.2009.0221. Assay Drug Dev Technol. 2009. PMID: 20059376
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: totoritis r. Chembiochem. 2021 Feb 2;22(3):516-522. doi: 10.1002/cbic.202000298. Epub 2020 Nov 16. Chembiochem. 2021. PMID: 32974990
17 results