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Page 1
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. Among authors: notte gt. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Smith-Maxwell C, Dhalla AK, Rajamani S, Stafford B, Tang J, Mollova N, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: notte gt. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206. doi: 10.1016/j.bmcl.2016.03.101. Epub 2016 Mar 30. Bioorg Med Chem Lett. 2016. PMID: 27080178
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
Farand J, Mai N, Chandrasekhar J, Newby ZE, Van Veldhuizen J, Loyer-Drew J, Venkataramani C, Guerrero J, Kwok A, Li N, Zherebina Y, Wilbert S, Zablocki J, Phillips G, Watkins WJ, Mourey R, Notte GT. Farand J, et al. Among authors: notte gt. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5926-5930. doi: 10.1016/j.bmcl.2016.10.092. Epub 2016 Nov 2. Bioorg Med Chem Lett. 2016. PMID: 27876318
ASK1 contributes to fibrosis and dysfunction in models of kidney disease.
Liles JT, Corkey BK, Notte GT, Budas GR, Lansdon EB, Hinojosa-Kirschenbaum F, Badal SS, Lee M, Schultz BE, Wise S, Pendem S, Graupe M, Castonguay L, Koch KA, Wong MH, Papalia GA, French DM, Sullivan T, Huntzicker EG, Ma FY, Nikolic-Paterson DJ, Altuhaifi T, Yang H, Fogo AB, Breckenridge DG. Liles JT, et al. Among authors: notte gt. J Clin Invest. 2018 Oct 1;128(10):4485-4500. doi: 10.1172/JCI99768. Epub 2018 Jul 19. J Clin Invest. 2018. PMID: 30024858 Free PMC article.
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Farand J, Kropf JE, Blomgren P, Xu J, Schmitt AC, Newby ZE, Wang T, Murakami E, Barauskas O, Sudhamsu J, Feng JY, Niedziela-Majka A, Schultz BE, Schwartz K, Viatchenko-Karpinski S, Kornyeyev D, Kashishian A, Fan P, Chen X, Lansdon EB, Ports MO, Currie KS, Watkins WJ, Notte GT. Farand J, et al. Among authors: notte gt. ACS Med Chem Lett. 2019 Nov 19;11(3):358-364. doi: 10.1021/acsmedchemlett.9b00420. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184970 Free PMC article.
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