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Page 1
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. Among authors: tandeske l. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
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. Among authors: tandeske l. 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: tandeske l. 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
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM. Smith A, et al. Among authors: tandeske l. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2017. PMID: 29107542
A strategy to assess the cellular activity of E3 ligase components against neo-substrates using electrophilic probes.
Pinch BJ, Buckley DL, Gleim S, Brittain SM, Tandeske L, D'Alessandro PL, Hauseman ZJ, Lipps J, Xu L, Harvey EP, Schirle M, Sprague ER, Forrester WC, Dovala D, McGregor LM, Thoma CR. Pinch BJ, et al. Among authors: tandeske l. Cell Chem Biol. 2022 Jan 20;29(1):57-66.e6. doi: 10.1016/j.chembiol.2021.08.007. Epub 2021 Sep 8. Cell Chem Biol. 2022. PMID: 34499862 Free article.
Discovery of Potent Pyrazoline-Based Covalent SARS-CoV-2 Main Protease Inhibitors.
Moon P, Zammit CM, Shao Q, Dovala D, Boike L, Henning NJ, Knapp M, Spradlin JN, Ward CC, Wolleb H, Fuller D, Blake G, Murphy JP, Wang F, Lu Y, Moquin SA, Tandeske L, Hesse MJ, McKenna JM, Tallarico JA, Schirle M, Toste FD, Nomura DK. Moon P, et al. Among authors: tandeske l. Chembiochem. 2023 Jun 1;24(11):e202300116. doi: 10.1002/cbic.202300116. Epub 2023 May 3. Chembiochem. 2023. PMID: 37069799
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