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Page 1
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.
Palmer WS, Poncet-Montange G, Liu G, Petrocchi A, Reyna N, Subramanian G, Theroff J, Yau A, Kost-Alimova M, Bardenhagen JP, Leo E, Shepard HE, Tieu TN, Shi X, Zhan Y, Zhao S, Barton MC, Draetta G, Toniatti C, Jones P, Geck Do M, Andersen JN. Palmer WS, et al. Among authors: jones p. J Med Chem. 2016 Feb 25;59(4):1440-54. doi: 10.1021/acs.jmedchem.5b00405. Epub 2015 Jul 6. J Med Chem. 2016. PMID: 26061247 Free PMC article.
Identification of potent and selective MTH1 inhibitors.
Petrocchi A, Leo E, Reyna NJ, Hamilton MM, Shi X, Parker CA, Mseeh F, Bardenhagen JP, Leonard P, Cross JB, Huang S, Jiang Y, Cardozo M, Draetta G, Marszalek JR, Toniatti C, Jones P, Lewis RT. Petrocchi A, et al. Among authors: jones p. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1503-1507. doi: 10.1016/j.bmcl.2016.02.026. Epub 2016 Feb 11. Bioorg Med Chem Lett. 2016. PMID: 26898335
In Vivo Functional Platform Targeting Patient-Derived Xenografts Identifies WDR5-Myc Association as a Critical Determinant of Pancreatic Cancer.
Carugo A, Genovese G, Seth S, Nezi L, Rose JL, Bossi D, Cicalese A, Shah PK, Viale A, Pettazzoni PF, Akdemir KC, Bristow CA, Robinson FS, Tepper J, Sanchez N, Gupta S, Estecio MR, Giuliani V, Dellino GI, Riva L, Yao W, Di Francesco ME, Green T, D'Alesio C, Corti D, Kang Y, Jones P, Wang H, Fleming JB, Maitra A, Pelicci PG, Chin L, DePinho RA, Lanfrancone L, Heffernan TP, Draetta GF. Carugo A, et al. Among authors: jones p. Cell Rep. 2016 Jun 28;16(1):133-147. doi: 10.1016/j.celrep.2016.05.063. Epub 2016 Jun 16. Cell Rep. 2016. PMID: 27320920 Free article.
An inhibitor of oxidative phosphorylation exploits cancer vulnerability.
Molina JR, Sun Y, Protopopova M, Gera S, Bandi M, Bristow C, McAfoos T, Morlacchi P, Ackroyd J, Agip AA, Al-Atrash G, Asara J, Bardenhagen J, Carrillo CC, Carroll C, Chang E, Ciurea S, Cross JB, Czako B, Deem A, Daver N, de Groot JF, Dong JW, Feng N, Gao G, Gay J, Do MG, Greer J, Giuliani V, Han J, Han L, Henry VK, Hirst J, Huang S, Jiang Y, Kang Z, Khor T, Konoplev S, Lin YH, Liu G, Lodi A, Lofton T, Ma H, Mahendra M, Matre P, Mullinax R, Peoples M, Petrocchi A, Rodriguez-Canale J, Serreli R, Shi T, Smith M, Tabe Y, Theroff J, Tiziani S, Xu Q, Zhang Q, Muller F, DePinho RA, Toniatti C, Draetta GF, Heffernan TP, Konopleva M, Jones P, Di Francesco ME, Marszalek JR. Molina JR, et al. Among authors: jones p. Nat Med. 2018 Jul;24(7):1036-1046. doi: 10.1038/s41591-018-0052-4. Epub 2018 Jun 11. Nat Med. 2018. PMID: 29892070
Metabolic reprogramming toward oxidative phosphorylation identifies a therapeutic target for mantle cell lymphoma.
Zhang L, Yao Y, Zhang S, Liu Y, Guo H, Ahmed M, Bell T, Zhang H, Han G, Lorence E, Badillo M, Zhou S, Sun Y, Di Francesco ME, Feng N, Haun R, Lan R, Mackintosh SG, Mao X, Song X, Zhang J, Pham LV, Lorenzi PL, Marszalek J, Heffernan T, Draetta G, Jones P, Futreal A, Nomie K, Wang L, Wang M. Zhang L, et al. Among authors: jones p. Sci Transl Med. 2019 May 8;11(491):eaau1167. doi: 10.1126/scitranslmed.aau1167. Sci Transl Med. 2019. PMID: 31068440
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E, Kovacs JJ, Feng N, Gera S, Harris AL, Liu Z, Mullinax RA, Pang J, Parker CA, Spencer ND, Yu SS, Wu Q, Tremblay MR, Mikule K, Wilcoxen K, Heffernan TP, Draetta GF, Jones P. Czako B, et al. Among authors: jones p. J Med Chem. 2020 Sep 10;63(17):9888-9911. doi: 10.1021/acs.jmedchem.0c00936. Epub 2020 Aug 18. J Med Chem. 2020. PMID: 32787110
Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib.
Sun Y, Meyers BA, Czako B, Leonard P, Mseeh F, Harris AL, Wu Q, Johnson S, Parker CA, Cross JB, Di Francesco ME, Bivona BJ, Bristow CA, Burke JP, Carrillo CC, Carroll CL, Chang Q, Feng N, Gao G, Gera S, Giuliani V, Huang JK, Jiang Y, Kang Z, Kovacs JJ, Liu CY, Lopez AM, Ma X, Mandal PK, McAfoos T, Miller MA, Mullinax RA, Peoples M, Ramamoorthy V, Seth S, Spencer ND, Suzuki E, Williams CC, Yu SS, Zuniga AM, Draetta GF, Marszalek JR, Heffernan TP, Kohl NE, Jones P. Sun Y, et al. Among authors: jones p. Cancer Res. 2020 Nov 1;80(21):4840-4853. doi: 10.1158/0008-5472.CAN-20-1634. Epub 2020 Sep 14. Cancer Res. 2020. PMID: 32928921
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.
Soth MJ, Le K, Di Francesco ME, Hamilton MM, Liu G, Burke JP, Carroll CL, Kovacs JJ, Bardenhagen JP, Bristow CA, Cardozo M, Czako B, de Stanchina E, Feng N, Garvey JR, Gay JP, Do MKG, Greer J, Han M, Harris A, Herrera Z, Huang S, Giuliani V, Jiang Y, Johnson SB, Johnson TA, Kang Z, Leonard PG, Liu Z, McAfoos T, Miller M, Morlacchi P, Mullinax RA, Palmer WS, Pang J, Rogers N, Rudin CM, Shepard HE, Spencer ND, Theroff J, Wu Q, Xu A, Yau JA, Draetta G, Toniatti C, Heffernan TP, Jones P. Soth MJ, et al. Among authors: jones p. J Med Chem. 2020 Nov 12;63(21):12957-12977. doi: 10.1021/acs.jmedchem.0c01398. Epub 2020 Oct 29. J Med Chem. 2020. PMID: 33118821 Free PMC article.
Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT. Hamilton MM, et al. Among authors: jones p. J Med Chem. 2021 Aug 12;64(15):11302-11329. doi: 10.1021/acs.jmedchem.1c00679. Epub 2021 Jul 22. J Med Chem. 2021. PMID: 34292726
8,640 results