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Catalytic in vivo protein knockdown by small-molecule PROTACs.
Bondeson DP, Mares A, Smith IE, Ko E, Campos S, Miah AH, Mulholland KE, Routly N, Buckley DL, Gustafson JL, Zinn N, Grandi P, Shimamura S, Bergamini G, Faelth-Savitski M, Bantscheff M, Cox C, Gordon DA, Willard RR, Flanagan JJ, Casillas LN, Votta BJ, den Besten W, Famm K, Kruidenier L, Carter PS, Harling JD, Churcher I, Crews CM. Bondeson DP, et al. Among authors: churcher i. Nat Chem Biol. 2015 Aug;11(8):611-7. doi: 10.1038/nchembio.1858. Epub 2015 Jun 10. Nat Chem Biol. 2015. PMID: 26075522 Free PMC article.
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2.
Mares A, Miah AH, Smith IED, Rackham M, Thawani AR, Cryan J, Haile PA, Votta BJ, Beal AM, Capriotti C, Reilly MA, Fisher DT, Zinn N, Bantscheff M, MacDonald TT, Vossenkamper A, Dace P, Churcher I, Benowitz AB, Watt G, Denyer J, Scott-Stevens P, Harling JD. Mares A, et al. Among authors: churcher i. Commun Biol. 2020 Mar 20;3(1):140. doi: 10.1038/s42003-020-0868-6. Commun Biol. 2020. PMID: 32198438 Free PMC article.
Optimization of a Series of RIPK2 PROTACs.
Miah AH, Smith IED, Rackham M, Mares A, Thawani AR, Nagilla R, Haile PA, Votta BJ, Gordon LJ, Watt G, Denyer J, Fisher DT, Dace P, Giffen P, Goncalves A, Churcher I, Scott-Stevens P, Harling JD. Miah AH, et al. Among authors: churcher i. J Med Chem. 2021 Sep 9;64(17):12978-13003. doi: 10.1021/acs.jmedchem.1c01118. Epub 2021 Aug 25. J Med Chem. 2021. PMID: 34432979
Structural Insights into PROTAC-Mediated Degradation of Bcl-xL.
Chung CW, Dai H, Fernandez E, Tinworth CP, Churcher I, Cryan J, Denyer J, Harling JD, Konopacka A, Queisser MA, Tame CJ, Watt G, Jiang F, Qian D, Benowitz AB. Chung CW, et al. Among authors: churcher i. ACS Chem Biol. 2020 Sep 18;15(9):2316-2323. doi: 10.1021/acschembio.0c00266. Epub 2020 Aug 13. ACS Chem Biol. 2020. PMID: 32697072
Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.
Bassi ZI, Fillmore MC, Miah AH, Chapman TD, Maller C, Roberts EJ, Davis LC, Lewis DE, Galwey NW, Waddington KE, Parravicini V, Macmillan-Jones AL, Gongora C, Humphreys PG, Churcher I, Prinjha RK, Tough DF. Bassi ZI, et al. Among authors: churcher i. ACS Chem Biol. 2018 Oct 19;13(10):2862-2867. doi: 10.1021/acschembio.8b00705. Epub 2018 Sep 18. ACS Chem Biol. 2018. PMID: 30200762
Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.
Borthwick JA, Ancellin N, Bertrand SM, Bingham RP, Carter PS, Chung CW, Churcher I, Dodic N, Fournier C, Francis PL, Hobbs A, Jamieson C, Pickett SD, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Young RJ. Borthwick JA, et al. Among authors: churcher i. J Med Chem. 2016 Mar 24;59(6):2452-67. doi: 10.1021/acs.jmedchem.5b01607. Epub 2016 Mar 16. J Med Chem. 2016. PMID: 26938474 Free article.
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.
Bertrand SM, Ancellin N, Beaufils B, Bingham RP, Borthwick JA, Boullay AB, Boursier E, Carter PS, Chung CW, Churcher I, Dodic N, Fouchet MH, Fournier C, Francis PL, Gummer LA, Herry K, Hobbs A, Hobbs CI, Homes P, Jamieson C, Nicodeme E, Pickett SD, Reid IH, Simpson GL, Sloan LA, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Valko K, Washio Y, Young RJ. Bertrand SM, et al. Among authors: churcher i. J Med Chem. 2015 Sep 24;58(18):7140-63. doi: 10.1021/acs.jmedchem.5b00313. Epub 2015 Jul 2. J Med Chem. 2015. PMID: 26090771
33 results