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Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39.
Bassilana F, Carlson A, DaSilva JA, Grosshans B, Vidal S, Beck V, Wilmeringwetter B, Llamas LA, Showalter TB, Rigollier P, Bourret A, Ramamurthy A, Wu X, Harbinski F, Plonsky S, Lee L, Ruffner H, Grandi P, Schirle M, Jenkins J, Sailer AW, Bouwmeester T, Porter JA, Myer V, Finan PM, Tallarico JA, Kelleher JF 3rd, Seuwen K, Jain RK, Luchansky SJ. Bassilana F, et al. Among authors: kelleher jf 3rd. Nat Chem Biol. 2014 May;10(5):343-9. doi: 10.1038/nchembio.1481. Epub 2014 Mar 16. Nat Chem Biol. 2014. PMID: 24633354
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: kelleher jf 3rd. J Med Chem. 2009 Jul 9;52(13):3954-68. doi: 10.1021/jm900309j. J Med Chem. 2009. PMID: 19469545
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: kelleher jf 3rd. ChemMedChem. 2013 Aug;8(8):1261-5. doi: 10.1002/cmdc.201300217. Epub 2013 Jul 2. ChemMedChem. 2013. PMID: 23821351 No abstract available.
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: kelleher jf 3rd. 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: kelleher jf. Sci Transl Med. 2010 Sep 29;2(51):51ra70. doi: 10.1126/scitranslmed.3001599. Sci Transl Med. 2010. PMID: 20881279 Free PMC article.
Loss of the tumor suppressor Snf5 leads to aberrant activation of the Hedgehog-Gli pathway.
Jagani Z, Mora-Blanco EL, Sansam CG, McKenna ES, Wilson B, Chen D, Klekota J, Tamayo P, Nguyen PT, Tolstorukov M, Park PJ, Cho YJ, Hsiao K, Buonamici S, Pomeroy SL, Mesirov JP, Ruffner H, Bouwmeester T, Luchansky SJ, Murtie J, Kelleher JF, Warmuth M, Sellers WR, Roberts CW, Dorsch M. Jagani Z, et al. Among authors: kelleher jf. Nat Med. 2010 Dec;16(12):1429-33. doi: 10.1038/nm.2251. Epub 2010 Nov 14. Nat Med. 2010. PMID: 21076395 Free PMC article.
65 results