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  • Timothy M Chapman, Simon A. Osborne, +9 authors Anthony A. Holder
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2013 (First Publication: 1 May 2013)
  • A series of imidazopyridazines which are potent inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) was identified from a high-throughput screen against the isolatedContinue Reading
  • Timothy M Chapman, Simon A. Osborne, +8 authors Anthony A. Holder
  • Medicine, Chemistry
  • Journal of medicinal chemistry
  • 2014 (First Publication: 24 April 2014)
  • A structure-guided design approach using a homology model of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) was used to improve the potency of a series of imidazopyridazineContinue Reading
  • Judith L. Green, Robert W Moon, +14 authors Anthony A. Holder
  • Medicine, Biology
  • Antimicrobial agents and chemotherapy
  • 2015 (First Publication: 1 March 2016)
  • Imidazopyridazine compounds are potent, ATP-competitive inhibitors of calcium-dependent protein kinase 1 (CDPK1) and of Plasmodium falciparum parasite growth in vitro. Here, we show that theseContinue Reading
  • Shishir M. Pant, Amanda Mukonoweshuro, +8 authors Juha Klefström
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • 2018 (First Publication: 24 May 2018)
  • Hepsin is a membrane-anchored serine protease whose role in hepatocyte growth factor (HGF) signaling and epithelial integrity makes it a target of therapeutic interest in carcinogenesis andContinue Reading
  • Timothy M Chapman, Nathalie Bouloc, +7 authors David P. Whalley
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 2012 (First Publication: 1 May 2012)
  • A high-throughput screen against PknB, an essential serine-threonine protein kinase present in Mycobacterium tuberculosis (M. tuberculosis), allowed the identification of an aminoquinazolineContinue Reading
  • Keith H. Ansell, Hayley M. Jones, +14 authors Anthony A. Holder
  • Medicine, Biology
  • Antimicrobial agents and chemotherapy
  • 2014 (First Publication: 1 October 2014)
  • PfCDPK1 is a Plasmodium falciparum calcium-dependent protein kinase, which has been identified as a potential target for novel antimalarial chemotherapeutics. In order to further investigate the roleContinue Reading