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Conversion of Bim-BH3 from Activator to Inhibitor of Bak through Structure-Based Design.
Brouwer JM, Lan P, Cowan AD, Bernardini JP, Birkinshaw RW, van Delft MF, Sleebs BE, Robin AY, Wardak A, Tan IK, Reljic B, Lee EF, Fairlie WD, Call MJ, Smith BJ, Dewson G, Lessene G, Colman PM, Czabotar PE. Brouwer JM, et al. Among authors: cowan ad. Mol Cell. 2017 Nov 16;68(4):659-672.e9. doi: 10.1016/j.molcel.2017.11.001. Mol Cell. 2017. PMID: 29149594 Free article.
Conformational switching of the pseudokinase domain promotes human MLKL tetramerization and cell death by necroptosis.
Petrie EJ, Sandow JJ, Jacobsen AV, Smith BJ, Griffin MDW, Lucet IS, Dai W, Young SN, Tanzer MC, Wardak A, Liang LY, Cowan AD, Hildebrand JM, Kersten WJA, Lessene G, Silke J, Czabotar PE, Webb AI, Murphy JM. Petrie EJ, et al. Among authors: cowan ad. Nat Commun. 2018 Jun 21;9(1):2422. doi: 10.1038/s41467-018-04714-7. Nat Commun. 2018. PMID: 29930286 Free PMC article.
Potent Inhibition of Necroptosis by Simultaneously Targeting Multiple Effectors of the Pathway.
Pierotti CL, Tanzer MC, Jacobsen AV, Hildebrand JM, Garnier JM, Sharma P, Lucet IS, Cowan AD, Kersten WJA, Luo MX, Liang LY, Fitzgibbon C, Garnish SE, Hempel A, Nachbur U, Huang DCS, Czabotar PE, Silke J, van Delft MF, Murphy JM, Lessene G. Pierotti CL, et al. Among authors: cowan ad. ACS Chem Biol. 2020 Oct 16;15(10):2702-2713. doi: 10.1021/acschembio.0c00482. Epub 2020 Sep 22. ACS Chem Biol. 2020. PMID: 32902249
BAK core dimers bind lipids and can be bridged by them.
Cowan AD, Smith NA, Sandow JJ, Kapp EA, Rustam YH, Murphy JM, Brouwer JM, Bernardini JP, Roy MJ, Wardak AZ, Tan IK, Webb AI, Gulbis JM, Smith BJ, Reid GE, Dewson G, Colman PM, Czabotar PE. Cowan AD, et al. Nat Struct Mol Biol. 2020 Nov;27(11):1024-1031. doi: 10.1038/s41594-020-0494-5. Epub 2020 Sep 14. Nat Struct Mol Biol. 2020. PMID: 32929280
The Bak core dimer focuses triacylglycerides in the membrane.
Smith NA, Wardak AZ, Cowan AD, Colman PM, Czabotar PE, Smith BJ. Smith NA, et al. Among authors: cowan ad. Biophys J. 2022 Feb 1;121(3):347-360. doi: 10.1016/j.bpj.2021.12.043. Epub 2021 Dec 30. Biophys J. 2022. PMID: 34973947 Free PMC article.
The X-ray crystal structure of full-length human plasminogen.
Law RH, Caradoc-Davies T, Cowieson N, Horvath AJ, Quek AJ, Encarnacao JA, Steer D, Cowan A, Zhang Q, Lu BG, Pike RN, Smith AI, Coughlin PB, Whisstock JC. Law RH, et al. Cell Rep. 2012 Mar 29;1(3):185-90. doi: 10.1016/j.celrep.2012.02.012. Epub 2012 Mar 8. Cell Rep. 2012. PMID: 22832192 Free article.
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.
Imaide S, Riching KM, Makukhin N, Vetma V, Whitworth C, Hughes SJ, Trainor N, Mahan SD, Murphy N, Cowan AD, Chan KH, Craigon C, Testa A, Maniaci C, Urh M, Daniels DL, Ciulli A. Imaide S, et al. Among authors: cowan ad. Nat Chem Biol. 2021 Nov;17(11):1157-1167. doi: 10.1038/s41589-021-00878-4. Epub 2021 Oct 21. Nat Chem Biol. 2021. PMID: 34675414 Free PMC article.
14 results