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Page 1
A Novel Mitochondrial Inhibitor Blocks MAPK Pathway and Overcomes MAPK Inhibitor Resistance in Melanoma.
Vashisht Gopal YN, Gammon S, Prasad R, Knighton B, Pisaneschi F, Roszik J, Feng N, Johnson S, Pramanik S, Sudderth J, Sui D, Hudgens C, Fischer GM, Deng W, Reuben A, Peng W, Wang J, McQuade JL, Tetzlaff MT, Di Francesco ME, Marszalek J, Piwnica-Worms D, DeBerardinis RJ, Davies MA. Vashisht Gopal YN, et al. Among authors: di francesco me. Clin Cancer Res. 2019 Nov 1;25(21):6429-6442. doi: 10.1158/1078-0432.CCR-19-0836. Epub 2019 Aug 22. Clin Cancer Res. 2019. PMID: 31439581 Free PMC article.
SF2312 is a natural phosphonate inhibitor of enolase.
Leonard PG, Satani N, Maxwell D, Lin YH, Hammoudi N, Peng Z, Pisaneschi F, Link TM, Lee GR 4th, Sun D, Prasad BAB, Di Francesco ME, Czako B, Asara JM, Wang YA, Bornmann W, DePinho RA, Muller FL. Leonard PG, et al. Among authors: di francesco me. Nat Chem Biol. 2016 Dec;12(12):1053-1058. doi: 10.1038/nchembio.2195. Epub 2016 Oct 10. Nat Chem Biol. 2016. PMID: 27723749 Free PMC 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: di francesco me. 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: di francesco me. Sci Transl Med. 2019 May 8;11(491):eaau1167. doi: 10.1126/scitranslmed.aau1167. Sci Transl Med. 2019. PMID: 31068440
Mechanism-Specific Pharmacodynamics of a Novel Complex-I Inhibitor Quantified by Imaging Reversal of Consumptive Hypoxia with [18F]FAZA PET In Vivo.
Gammon ST, Pisaneschi F, Bandi ML, Smith MG, Sun Y, Rao Y, Muller F, Wong F, De Groot J, Ackroyd J, Mawlawi O, Davies MA, Gopal YNV, Di Francesco ME, Marszalek JR, Dewhirst M, Piwnica-Worms D. Gammon ST, et al. Among authors: di francesco me. Cells. 2019 Nov 21;8(12):1487. doi: 10.3390/cells8121487. Cells. 2019. PMID: 31766580 Free PMC article.
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: di francesco me. 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: di francesco me. 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 6-[(3S,4S)-4-Amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a Potent and Orally Bioavailable SHP2 Inhibitor.
Czako B, Sun Y, McAfoos T, Cross JB, Leonard PG, Burke JP, Carroll CL, Feng N, Harris AL, Jiang Y, Kang Z, Kovacs JJ, Mandal P, Meyers BA, Mseeh F, Parker CA, Yu SS, Williams CC, Wu Q, Di Francesco ME, Draetta G, Heffernan T, Marszalek JR, Kohl NE, Jones P. Czako B, et al. Among authors: di francesco me. J Med Chem. 2021 Oct 28;64(20):15141-15169. doi: 10.1021/acs.jmedchem.1c01132. Epub 2021 Oct 13. J Med Chem. 2021. PMID: 34643390
29 results