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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: huang dcs. 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 enables BAX to mediate apoptosis and limit tumor development.
Chin HS, Li MX, Tan IKL, Ninnis RL, Reljic B, Scicluna K, Dagley LF, Sandow JJ, Kelly GL, Samson AL, Chappaz S, Khaw SL, Chang C, Morokoff A, Brinkmann K, Webb A, Hockings C, Hall CM, Kueh AJ, Ryan MT, Kluck RM, Bouillet P, Herold MJ, Gray DHD, Huang DCS, van Delft MF, Dewson G. Chin HS, et al. Among authors: huang dcs. Nat Commun. 2018 Nov 26;9(1):4976. doi: 10.1038/s41467-018-07309-4. Nat Commun. 2018. PMID: 30478310 Free PMC 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: huang dcs. 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
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: huang dcs. 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
Structural insights into the degradation of Mcl-1 induced by BH3 domains.
Czabotar PE, Lee EF, van Delft MF, Day CL, Smith BJ, Huang DC, Fairlie WD, Hinds MG, Colman PM. Czabotar PE, et al. Proc Natl Acad Sci U S A. 2007 Apr 10;104(15):6217-22. doi: 10.1073/pnas.0701297104. Epub 2007 Mar 27. Proc Natl Acad Sci U S A. 2007. PMID: 17389404 Free PMC article.
217 results