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Page 1
Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.
Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z. Papillon JPN, et al. Among authors: vattay a. J Med Chem. 2018 Nov 21;61(22):10155-10172. doi: 10.1021/acs.jmedchem.8b01318. Epub 2018 Oct 31. J Med Chem. 2018. PMID: 30339381
1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.
Miller-Moslin K, Peukert S, Jain RK, McEwan MA, Karki R, Llamas L, Yusuff N, He F, Li Y, Sun Y, Dai M, Perez L, Michael W, Sheng T, Lei H, Zhang R, Williams J, Bourret A, Ramamurthy A, Yuan J, Guo R, Matsumoto M, Vattay A, Maniara W, Amaral A, Dorsch M, Kelleher JF 3rd. Miller-Moslin K, et al. Among authors: vattay a. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
The Discovery of SWI/SNF Chromatin Remodeling Activity as a Novel and Targetable Dependency in Uveal Melanoma.
Rago F, Elliott G, Li A, Sprouffske K, Kerr G, Desplat A, Abramowski D, Chen JT, Farsidjani A, Xiang KX, Bushold G, Feng Y, Shirley MD, Bric A, Vattay A, Möbitz H, Nakajima K, Adair CD, Mathieu S, Ntaganda R, Smith T, Papillon JPN, Kauffmann A, Ruddy DA, Bhang HC, Castelletti D, Jagani Z. Rago F, et al. Among authors: vattay a. Mol Cancer Ther. 2020 Oct;19(10):2186-2195. doi: 10.1158/1535-7163.MCT-19-1013. Epub 2020 Aug 3. Mol Cancer Ther. 2020. PMID: 32747420
Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma.
Visser M, Papillon JPN, Luzzio M, LaMarche MJ, Fan J, Michael W, Wang D, Zhang A, Straub C, Mathieu S, Kato M, Palermo M, Chen C, Ramsey T, Joud C, Barrett R, Vattay A, Guo R, Bric A, Chung F, Liang G, Romanowski MJ, Lam J, Thohan S, Atassi F, Wylie A, Cooke VG. Visser M, et al. Among authors: vattay a. J Med Chem. 2024 Jan 25;67(2):1447-1459. doi: 10.1021/acs.jmedchem.3c02002. Epub 2024 Jan 10. J Med Chem. 2024. PMID: 38198520
Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist.
Pan S, Wu X, Jiang J, Gao W, Wan Y, Cheng D, Han D, Liu J, Englund NP, Wang Y, Peukert S, Miller-Moslin K, Yuan J, Guo R, Matsumoto M, Vattay A, Jiang Y, Tsao J, Sun F, Pferdekamper AC, Dodd S, Tuntland T, Maniara W, Kelleher JF 3rd, Yao YM, Warmuth M, Williams J, Dorsch M. Pan S, et al. Among authors: vattay a. ACS Med Chem Lett. 2010 Mar 16;1(3):130-4. doi: 10.1021/ml1000307. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900187 Free PMC article.
Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma.
Buonamici S, Williams J, Morrissey M, Wang A, Guo R, Vattay A, Hsiao K, Yuan J, Green J, Ospina B, Yu Q, Ostrom L, Fordjour P, Anderson DL, Monahan JE, Kelleher JF, Peukert S, Pan S, Wu X, Maira SM, García-Echeverría C, Briggs KJ, Watkins DN, Yao YM, Lengauer C, Warmuth M, Sellers WR, Dorsch M. Buonamici S, et al. Among authors: vattay a. Sci Transl Med. 2010 Sep 29;2(51):51ra70. doi: 10.1126/scitranslmed.3001599. Sci Transl Med. 2010. PMID: 20881279 Free PMC article.
Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened.
Peukert S, He F, Dai M, Zhang R, Sun Y, Miller-Moslin K, McEwan M, Lagu B, Wang K, Yusuff N, Bourret A, Ramamurthy A, Maniara W, Amaral A, Vattay A, Wang A, Guo R, Yuan J, Green J, Williams J, Buonamici S, Kelleher JF 3rd, Dorsch M. Peukert S, et al. Among authors: vattay a. ChemMedChem. 2013 Aug;8(8):1261-5. doi: 10.1002/cmdc.201300217. Epub 2013 Jul 2. ChemMedChem. 2013. PMID: 23821351 No abstract available.