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Page 1
Tumor Intrinsic Efficacy by SHP2 and RTK Inhibitors in KRAS-Mutant Cancers.
Hao HX, Wang H, Liu C, Kovats S, Velazquez R, Lu H, Pant B, Shirley M, Meyer MJ, Pu M, Lim J, Fleming M, Alexander L, Farsidjani A, LaMarche MJ, Moody S, Silver SJ, Caponigro G, Stuart DD, Abrams TJ, Hammerman PS, Williams J, Engelman JA, Goldoni S, Mohseni M. Hao HX, et al. Among authors: stuart dd. Mol Cancer Ther. 2019 Dec;18(12):2368-2380. doi: 10.1158/1535-7163.MCT-19-0170. Epub 2019 Aug 22. Mol Cancer Ther. 2019. PMID: 31439712
Inhibition of prenylated KRAS in a lipid environment.
Jansen JM, Wartchow C, Jahnke W, Fong S, Tsang T, Pfister K, Zavorotinskaya T, Bussiere D, Cheng JM, Crawford K, Dai Y, Dove J, Fang E, Feng Y, Florent JM, Fuller J, Gossert AD, Hekmat-Nejad M, Henry C, Klopp J, Lenahan WP, Lingel A, Ma S, Meyer A, Mishina Y, Narberes J, Pardee G, Ramurthy S, Rieffel S, Stuart D, Subramanian S, Tandeske L, Widger S, Widmer A, Winterhalter A, Zaror I, Hardy S. Jansen JM, et al. PLoS One. 2017 Apr 6;12(4):e0174706. doi: 10.1371/journal.pone.0174706. eCollection 2017. PLoS One. 2017. PMID: 28384226 Free PMC article.
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S. Nishiguchi GA, et al. Among authors: stuart dd. J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8. J Med Chem. 2017. PMID: 28557458
Phase I Dose-Escalation and -Expansion Study of the BRAF Inhibitor Encorafenib (LGX818) in Metastatic BRAF-Mutant Melanoma.
Delord JP, Robert C, Nyakas M, McArthur GA, Kudchakar R, Mahipal A, Yamada Y, Sullivan R, Arance A, Kefford RF, Carlino MS, Hidalgo M, Gomez-Roca C, Michel D, Seroutou A, Aslanis V, Caponigro G, Stuart DD, Moutouh-de Parseval L, Demuth T, Dummer R. Delord JP, et al. Among authors: stuart dd. Clin Cancer Res. 2017 Sep 15;23(18):5339-5348. doi: 10.1158/1078-0432.CCR-16-2923. Epub 2017 Jun 13. Clin Cancer Res. 2017. PMID: 28611198 Free article. Clinical Trial.
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
Shao W, Mishina YM, Feng Y, Caponigro G, Cooke VG, Rivera S, Wang Y, Shen F, Korn JM, Mathews Griner LA, Nishiguchi G, Rico A, Tellew J, Haling JR, Aversa R, Polyakov V, Zang R, Hekmat-Nejad M, Amiri P, Singh M, Keen N, Dillon MP, Lees E, Ramurthy S, Sellers WR, Stuart DD. Shao W, et al. Among authors: stuart dd. Cancer Res. 2018 Mar 15;78(6):1537-1548. doi: 10.1158/0008-5472.CAN-17-2033. Epub 2018 Jan 17. Cancer Res. 2018. PMID: 29343524
Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties.
Gao Y, Chang MT, McKay D, Na N, Zhou B, Yaeger R, Torres NM, Muniz K, Drosten M, Barbacid M, Caponigro G, Stuart D, Moebitz H, Solit DB, Abdel-Wahab O, Taylor BS, Yao Z, Rosen N. Gao Y, et al. Cancer Discov. 2018 May;8(5):648-661. doi: 10.1158/2159-8290.CD-17-1452. Epub 2018 Feb 26. Cancer Discov. 2018. PMID: 29483135 Free PMC article.
Hyperactivation of MAPK Signaling Is Deleterious to RAS/RAF-mutant Melanoma.
Leung GP, Feng T, Sigoillot FD, Geyer FC, Shirley MD, Ruddy DA, Rakiec DP, Freeman AK, Engelman JA, Jaskelioff M, Stuart DD. Leung GP, et al. Among authors: stuart dd. Mol Cancer Res. 2019 Jan;17(1):199-211. doi: 10.1158/1541-7786.MCR-18-0327. Epub 2018 Sep 10. Mol Cancer Res. 2019. PMID: 30201825
55 results