Brad Sleebs-Publications

Brad Sleebs-Publications

Researcher: 

Selected publications

  1. Wong W, Bai XC, Sleebs BE, Triglia T, Brown A, Thompson JK, Jackson KE, Hanssen E, Marapana DS, Fernandez IS, Ralph SA, Cowman AF, Scheres SHW, Baum J. Mefloquine targets the Plasmodium falciparum 80S ribosome to inhibit protein synthesis. Nat. Microbiol. 2017 2: 17031. PMID: 28288098
  2. Gilson PR, Tan C, Jarman KE, Lowes KN, Curtis JM, Nguyen W, Di Rago AE, Bullen HE, Prinz B, Duffy S, Baell JB, Hutton CA, Jousset Subroux H, Crabb BS, Avery VM, Cowman AF, Sleebs BE. Optimization of 2-anilino 4-amino substituted quinazolines into potent antimalarial agents with oral in vivo activity. J. Med. Chem. 2017 60(3): 1171-1188. PMID: 28080063 
  3. Nguyen W, Hodder AN, de Lezongard RB, Czabotar PE, Jarman KE, O'Neill MT, Thompson JK, Jousset Sabroux H, Cowman AF, Boddey JA, Sleebs BE. Enhanced antimalarial activity of plasmepsin V inhibitors by modification of the P2 position of PEXEL peptidomimetics. Eur. J. Med. Chem. 2018 15: 182-198. PMID: 29800827
  4. Gazdik M, Jarman KE, O'Neill MT, Hodder AN, Lowes KN, Jousset Sabroux H, Cowman AF, Boddey JA, Sleebs BE. Exploration of the P3 region of PEXEL peptidomimetics leads to a potent inhibitor of the Plasmodium protease, plasmepsin V. Bioorg. Med. Chem. 2016 24(9): 1993-2010. PMID: 27021426
  5. Coffey MJ, Sleebs BE, Uboldi AD, Garnham A, Franco M, Marino ND, Panas MW, Ferguson DJ, Enciso M, O'Neill MT, Lopaticki S, Stewart RJ, Dewson G, Smyth GK, Smith BJ, Masters SL, Boothroyd JC, Boddey JA, Tonkin CJ. An aspartyl protease defines a novel pathway for export of Toxoplasma proteins into the host cell. Elife. 2015 18;4. e10809. PMID: 26576949
  6. Hodder AN, Sleebs BE, Czabotar PE, Gazdik M, Xu Y, O'Neill MT, Lopaticki S, Nebl T, Triglia T, Smith BJ, Lowes K, Boddey JA, Cowman AF. Structural basis for plasmepsin V inhibition that blocks export of malaria proteins to human erythrocytes. Nat. Struct. Mol. Biol. 2015 22(8): 590-6. PMID: 26214367
  7. Sleebs BE, Gazdik M, O'Neill MT, Rajasekaran P, Lopaticki S, Lackovic K, Lowes K, Smith BJ, Cowman AF, Boddey JA. Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.  J. Med. Chem. 2014 57(18): 7644-62. PMID: 25167370
  8. Sleebs BE, Lopaticki S, Marapana DS, O'Neill MT, Rajasekaran P, Gazdik M, Günther S, Whitehead LW, Lowes KN, Barfod L, Hviid L, Shaw PJ, Hodder AN, Smith BJ, Cowman AF, Boddey JA. Inhibition of plasmepsin V activity demonstrates its essential role in protein export, PfEMP1 display, and survival of malaria parasites.  PLoS Biol. 2014 12(7): e1001897. PMID: 24983235
  9. Lessene G, Czabotar PE, Sleebs BE, Zobel K, Lowes KN, Adams JM, Baell JB, Colman PM, Deshayes K, Fairbrother WJ, Flygare JA, Gibbons P, Kersten WJ, Kulasegaram S, Moss RM, Parisot JP, Smith BJ, Street IP, Yang H, Huang DC, Watson KG. Structure-guided design of a selective BCL-X(L) inhibitor. Nat. Chem. Biol. 2013 9(6): 390-7. PMID: 23603658
  10. Sleebs BE, Kersten WJ, Kulasegaram S, Nikolakopoulos G, Hatzis E, Moss RM, Parisot JP, Yang H, Czabotar PE, Fairlie WD, Lee EF, Adams JM, Chen L, van Delft MF, Lowes KN, Wei A, Huang DC, Colman PM, Street IP, Baell JB, Watson K, Lessene G. Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL. J. Med. Chem. 2013 56(13): 5514-40. PMID: 23767404

 

Further publications