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Page 1
Inhibition of NOTCH signaling by gamma secretase inhibitor engages the RB pathway and elicits cell cycle exit in T-cell acute lymphoblastic leukemia cells.
Rao SS, O'Neil J, Liberator CD, Hardwick JS, Dai X, Zhang T, Tyminski E, Yuan J, Kohl NE, Richon VM, Van der Ploeg LH, Carroll PM, Draetta GF, Look AT, Strack PR, Winter CG. Rao SS, et al. Among authors: draetta gf. Cancer Res. 2009 Apr 1;69(7):3060-8. doi: 10.1158/0008-5472.CAN-08-4295. Epub 2009 Mar 24. Cancer Res. 2009. PMID: 19318552
Down-regulation of the Notch pathway mediated by a gamma-secretase inhibitor induces anti-tumour effects in mouse models of T-cell leukaemia.
Tammam J, Ware C, Efferson C, O'Neil J, Rao S, Qu X, Gorenstein J, Angagaw M, Kim H, Kenific C, Kunii K, Leach KJ, Nikov G, Zhao J, Dai X, Hardwick J, Scott M, Winter C, Bristow L, Elbi C, Reilly JF, Look T, Draetta G, Van der Ploeg L, Kohl NE, Strack PR, Majumder PK. Tammam J, et al. Among authors: draetta g. Br J Pharmacol. 2009 Nov;158(5):1183-95. doi: 10.1111/j.1476-5381.2009.00389.x. Epub 2009 Sep 23. Br J Pharmacol. 2009. PMID: 19775282 Free PMC article.
Downregulation of Notch pathway by a gamma-secretase inhibitor attenuates AKT/mammalian target of rapamycin signaling and glucose uptake in an ERBB2 transgenic breast cancer model.
Efferson CL, Winkelmann CT, Ware C, Sullivan T, Giampaoli S, Tammam J, Patel S, Mesiti G, Reilly JF, Gibson RE, Buser C, Yeatman T, Coppola D, Winter C, Clark EA, Draetta GF, Strack PR, Majumder PK. Efferson CL, et al. Among authors: draetta gf. Cancer Res. 2010 Mar 15;70(6):2476-84. doi: 10.1158/0008-5472.CAN-09-3114. Epub 2010 Mar 2. Cancer Res. 2010. PMID: 20197467
PDK1 attenuation fails to prevent tumor formation in PTEN-deficient transgenic mouse models.
Ellwood-Yen K, Keilhack H, Kunii K, Dolinski B, Connor Y, Hu K, Nagashima K, O'Hare E, Erkul Y, Di Bacco A, Gargano D, Shomer NH, Angagaw M, Leccese E, Andrade P, Hurd M, Shin MK, Vogt TF, Northrup A, Bobkova EV, Kasibhatla S, Bronson RT, Scott ML, Draetta G, Richon V, Kohl N, Blume-Jensen P, Andersen JN, Kraus M. Ellwood-Yen K, et al. Among authors: draetta g. Cancer Res. 2011 Apr 15;71(8):3052-65. doi: 10.1158/0008-5472.CAN-10-2282. Cancer Res. 2011. PMID: 21493594
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: draetta g. 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
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: draetta gf. 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
Met activation in non-small cell lung cancer is associated with de novo resistance to EGFR inhibitors and the development of brain metastasis.
Benedettini E, Sholl LM, Peyton M, Reilly J, Ware C, Davis L, Vena N, Bailey D, Yeap BY, Fiorentino M, Ligon AH, Pan BS, Richon V, Minna JD, Gazdar AF, Draetta G, Bosari S, Chirieac LR, Lutterbach B, Loda M. Benedettini E, et al. Among authors: draetta g. Am J Pathol. 2010 Jul;177(1):415-23. doi: 10.2353/ajpath.2010.090863. Epub 2010 May 20. Am J Pathol. 2010. PMID: 20489150 Free PMC article.
The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies.
Vangamudi B, Paul TA, Shah PK, Kost-Alimova M, Nottebaum L, Shi X, Zhan Y, Leo E, Mahadeshwar HS, Protopopov A, Futreal A, Tieu TN, Peoples M, Heffernan TP, Marszalek JR, Toniatti C, Petrocchi A, Verhelle D, Owen DR, Draetta G, Jones P, Palmer WS, Sharma S, Andersen JN. Vangamudi B, et al. Among authors: draetta g. Cancer Res. 2015 Sep 15;75(18):3865-3878. doi: 10.1158/0008-5472.CAN-14-3798. Epub 2015 Jul 2. Cancer Res. 2015. PMID: 26139243 Free PMC article.
171 results