Poster Presentation 9th General Meeting of the International Proteolysis Society 2015

Developing potent uPA/NHE1 inhibitors with high selectivity over related TLSPs from the clinical drug amiloride (#105)

Benjamin J Buckley 1 2 , Nathanial L Harris 1 2 , Longguang Jiang 3 , Mingdong Huang 3 , Michael Kelso 2 4 , Marie Ranson 1 2
  1. School of Biological Sciences, University of Wollongong, Wollongong, NSW, Australia
  2. Cancer Drug Discovery Group, Illawarra Health and Medical Research Institute, Wollongong, NSW, Australia
  3. State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Fuzhou, Fujian, China
  4. School of Chemistry, University of Wollongong, Wollongong, NSW, Australia
Publish consent withheld
  1. Webb, B.A., M. Chimenti, M.P. Jacobson, and D.L. Barber, Dysregulated pH: a perfect storm for cancer progression. Nat Rev Cancer, 2011. 11: p. 671-677.
  2. Amith, S.R., Wilkinson, J.M., Baksh, S. and Fliegel, L, The Na+/H+ exchanger (NHE1) as a novel co-adjuvant target in paclitaxel therapy of triple-negative breast cancer cells. Oncotarget, 2015. 6: p.1262-1275.
  3. Matthews, H., M. Ranson, and M.J. Kelso, Anti-tumour/metastasis effects of the potassium-sparing diuretic amiloride: an orally active anti-cancer drug waiting for its call-of-duty? Int J Cancer, 2011. 129: p. 2051-2061.
  4. Matthews, H., M. Ranson, J.D.A. Tyndall, and M.J. Kelso, Synthesis and preliminary evaluation of amiloride analogs as inhibitors of the urokinase-type plasminogen activator (uPA). Bioorg Med Chem Lett, 2011. 21: p. 6760-6766.