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Key residues in the VDAC2-BAK complex can be targeted to modulate apoptosis.
Yuan Z, van Delft MF, Li MX, Sumardy F, Smith BJ, Huang DCS, Lessene G, Khakam Y, Jin R, He S, Smith NA, Birkinshaw RW, Czabotar PE, Dewson G. Yuan Z, et al. Among authors: czabotar pe. PLoS Biol. 2024 May 2;22(5):e3002617. doi: 10.1371/journal.pbio.3002617. eCollection 2024 May. PLoS Biol. 2024. PMID: 38696533 Free PMC article.
VDAC2 and the BCL-2 family of proteins.
Yuan Z, Dewson G, Czabotar PE, Birkinshaw RW. Yuan Z, et al. Among authors: czabotar pe. Biochem Soc Trans. 2021 Dec 17;49(6):2787-2795. doi: 10.1042/BST20210753. Biochem Soc Trans. 2021. PMID: 34913469 Free PMC article. Review.
Bcl-2 family proteins as therapeutic targets.
Czabotar PE, Lessene G. Czabotar PE, et al. Curr Pharm Des. 2010;16(28):3132-48. doi: 10.2174/138161210793292429. Curr Pharm Des. 2010. PMID: 20687882 Review.
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: czabotar pe. 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.
A small molecule interacts with VDAC2 to block mouse BAK-driven apoptosis.
van Delft MF, Chappaz S, Khakham Y, Bui CT, Debrincat MA, Lowes KN, Brouwer JM, Grohmann C, Sharp PP, Dagley LF, Li L, McArthur K, Luo MX, Chin HS, Fairlie WD, Lee EF, Segal D, Duflocq S, Lessene R, Bernard S, Peilleron L, Nguyen T, Miles C, Wan SS, Lane RM, Wardak A, Lackovic K, Colman PM, Sandow JJ, Webb AI, Czabotar PE, Dewson G, Watson KG, Huang DCS, Lessene G, Kile BT. van Delft MF, et al. Among authors: czabotar pe. Nat Chem Biol. 2019 Nov;15(11):1057-1066. doi: 10.1038/s41589-019-0365-8. Epub 2019 Oct 7. Nat Chem Biol. 2019. PMID: 31591564
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. Among authors: czabotar pe. 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
Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-XL and BCL-2.
Roy MJ, Vom A, Okamoto T, Smith BJ, Birkinshaw RW, Yang H, Abdo H, White CA, Segal D, Huang DCS, Baell JB, Colman PM, Czabotar PE, Lessene G. Roy MJ, et al. Among authors: czabotar pe. J Med Chem. 2021 May 13;64(9):5447-5469. doi: 10.1021/acs.jmedchem.0c01771. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904752
Dynamic reconfiguration of pro-apoptotic BAK on membranes.
Sandow JJ, Tan IK, Huang AS, Masaldan S, Bernardini JP, Wardak AZ, Birkinshaw RW, Ninnis RL, Liu Z, Dalseno D, Lio D, Infusini G, Czabotar PE, Webb AI, Dewson G. Sandow JJ, et al. Among authors: czabotar pe. EMBO J. 2021 Oct 18;40(20):e107237. doi: 10.15252/embj.2020107237. Epub 2021 Sep 15. EMBO J. 2021. PMID: 34523147 Free PMC article.
111 results