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Page 1
Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.
Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A, Feng Y, Fortin PD, Gould T, Lagu B, Lei H, Lenoir F, Majumdar D, Ochala E, Palermo MG, Pham L, Pu M, Smith T, Stams T, Tomlinson RC, Touré BB, Visser M, Wang RM, Waters NJ, Shao W. Shultz MD, et al. Among authors: tomlinson rc. J Med Chem. 2013 Aug 22;56(16):6495-511. doi: 10.1021/jm400807n. Epub 2013 Aug 13. J Med Chem. 2013. PMID: 23844574
Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA).
Cheung AK, Hurley B, Kerrigan R, Shu L, Chin DN, Shen Y, O'Brien G, Sung MJ, Hou Y, Axford J, Cody E, Sun R, Fazal A, Fridrich C, Sanchez CC, Tomlinson RC, Jain M, Deng L, Hoffmaster K, Song C, Van Hoosear M, Shin Y, Servais R, Towler C, Hild M, Curtis D, Dietrich WF, Hamann LG, Briner K, Chen KS, Kobayashi D, Sivasankaran R, Dales NA. Cheung AK, et al. Among authors: tomlinson rc. J Med Chem. 2018 Dec 27;61(24):11021-11036. doi: 10.1021/acs.jmedchem.8b01291. Epub 2018 Dec 13. J Med Chem. 2018. PMID: 30407821
Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling.
Huang SM, Mishina YM, Liu S, Cheung A, Stegmeier F, Michaud GA, Charlat O, Wiellette E, Zhang Y, Wiessner S, Hild M, Shi X, Wilson CJ, Mickanin C, Myer V, Fazal A, Tomlinson R, Serluca F, Shao W, Cheng H, Shultz M, Rau C, Schirle M, Schlegl J, Ghidelli S, Fawell S, Lu C, Curtis D, Kirschner MW, Lengauer C, Finan PM, Tallarico JA, Bouwmeester T, Porter JA, Bauer A, Cong F. Huang SM, et al. Nature. 2009 Oct 1;461(7264):614-20. doi: 10.1038/nature08356. Epub 2009 Sep 16. Nature. 2009. PMID: 19759537
PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.
Cai X, Xu Y, Cheung AK, Tomlinson RC, Alcázar-Román A, Murphy L, Billich A, Zhang B, Feng Y, Klumpp M, Rondeau JM, Fazal AN, Wilson CJ, Myer V, Joberty G, Bouwmeester T, Labow MA, Finan PM, Porter JA, Ploegh HL, Baird D, De Camilli P, Tallarico JA, Huang Q. Cai X, et al. Among authors: tomlinson rc. Chem Biol. 2013 Jul 25;20(7):912-21. doi: 10.1016/j.chembiol.2013.05.010. Chem Biol. 2013. PMID: 23890009 Free PMC article.
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: tomlinson rc. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
Structure-Based Design of Selective Noncovalent CDK12 Inhibitors.
Johannes JW, Denz CR, Su N, Wu A, Impastato AC, Mlynarski S, Varnes JG, Prince DB, Cidado J, Gao N, Haddrick M, Jones NH, Li S, Li X, Liu Y, Nguyen TB, O'Connell N, Rivers E, Robbins DW, Tomlinson R, Yao T, Zhu X, Ferguson AD, Lamb ML, Manchester JI, Guichard S. Johannes JW, et al. ChemMedChem. 2018 Feb 6;13(3):231-235. doi: 10.1002/cmdc.201700695. Epub 2018 Jan 26. ChemMedChem. 2018. PMID: 29266803
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex.
Hsu JH, Rasmusson T, Robinson J, Pachl F, Read J, Kawatkar S, O' Donovan DH, Bagal S, Code E, Rawlins P, Argyrou A, Tomlinson R, Gao N, Zhu X, Chiarparin E, Jacques K, Shen M, Woods H, Bednarski E, Wilson DM, Drew L, Castaldi MP, Fawell S, Bloecher A. Hsu JH, et al. Cell Chem Biol. 2020 Jan 16;27(1):41-46.e17. doi: 10.1016/j.chembiol.2019.11.004. Epub 2019 Nov 27. Cell Chem Biol. 2020. PMID: 31786184 Free article.
Mechanistic Insights into a CDK9 Inhibitor Via Orthogonal Proteomics Methods.
Hendricks JA, Beaton N, Chernobrovkin A, Miele E, Hamza GM, Ricchiuto P, Tomlinson RC, Friman T, Borenstain C, Barlaam B, Hande S, Lamb ML, De Savi C, Davies R, Main M, Hellner J, Beeler K, Feng Y, Bruderer R, Reiter L, Molina DM, Castaldi MP. Hendricks JA, et al. Among authors: tomlinson rc. ACS Chem Biol. 2022 Jan 21;17(1):54-67. doi: 10.1021/acschembio.1c00488. Epub 2021 Dec 25. ACS Chem Biol. 2022. PMID: 34955012 Free article.
Dependence on the Pyrimidine Biosynthetic Enzyme DHODH Is a Synthetic Lethal Vulnerability in Mutant KRAS-Driven Cancers.
Koundinya M, Sudhalter J, Courjaud A, Lionne B, Touyer G, Bonnet L, Menguy I, Schreiber I, Perrault C, Vougier S, Benhamou B, Zhang B, He T, Gao Q, Gee P, Simard D, Castaldi MP, Tomlinson R, Reiling S, Barrague M, Newcombe R, Cao H, Wang Y, Sun F, Murtie J, Munson M, Yang E, Harper D, Bouaboula M, Pollard J, Grepin C, Garcia-Echeverria C, Cheng H, Adrian F, Winter C, Licht S, Cornella-Taracido I, Arrebola R, Morris A. Koundinya M, et al. Cell Chem Biol. 2018 Jun 21;25(6):705-717.e11. doi: 10.1016/j.chembiol.2018.03.005. Epub 2018 Apr 5. Cell Chem Biol. 2018. PMID: 29628435 Free article.
24 results