Kym Lowes

Property activity refinement of 2-anilino 4-amino substituted quinazolines as antimalarials with fast acting asexual parasite activity.

Trent D Ashton, Anna Ngo, Paola Favuzza, Hayley E Bullen, Maria R Gancheva, Ornella Romeo, Molly Parkyn Schneider, Nghi Nguyen, Ryan WJ Steel, Sandra Duffy, Kym N Lowes, Helene Jousset Sabroux, Vicky M Avery, Justin A Boddey, Danny W Wilson, Alan F Cowman, Paul R Gilson, Brad E Sleebs

Journal article  |  2021  |  Bioorg Chem

Malaria is a devastating disease caused by Plasmodium parasites. Emerging resistance against current antimalarial therapeutics has..

Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity

Brodie L Bailey, William Nguyen, Anna Ngo, Christopher D Goodman, Maria R Gancheva, Paola Favuzza, Laura M Sanz, Francisco-Javier Gamo, Kym N Lowes, Geoffrey I McFadden, Danny W Wilson, Benoit Laleu, Stephen Brand, Paul F Jackson, Alan F Cowman, Brad E Sleebs

Journal article  |  2021  |  BIOORGANIC CHEMISTRY

Malaria is a devastating parasitic disease caused by parasites from the genus Plasmodium. Therapeutic resistance has been reported..

Optimization of Benzothiazole and Thiazole Hydrazones as Inhibitors of Schistosome BCL-2

William Nguyen, Erinna F Lee, Marco Evangelista, Mihwa Lee, Tiffany J Harris, Peter M Colman, Nicholas A Smith, Luke B Williams, Kate E Jarman, Kym N Lowes, Cecile Haeberli, Jennifer Keiser, Brian J Smith, W Douglas Fairlie, Brad E Sleebs

Journal article  |  2021  |  ACS INFECTIOUS DISEASES

Limited therapeutic options are available for the treatment of human schistosomiasis caused by the parasitic Schistosoma flatworm...

Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

William Nguyen, Madeline G Dans, Anna Ngo, Maria R Gancheva, Ornella Romeo, Sandra Duffy, Tania F de Koning-Ward, Kym N Lowes, Helene Jousset Sabroux, Vicky M Avery, Danny W Wilson, Paul R Gilson, Brad E Sleebs

Journal article  |  2021  |  EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The emerging resistance to combination therapies comprised of artemisinin derivatives has driven a need to identify new antimalari..

Mechanism and inhibition of the papain-like protease, PLpro, of SARS-CoV-2

Theresa Klemm, Gregor Ebert, Dale J Calleja, Cody C Allison, Lachlan W Richardson, Jonathan P Bernardini, Bernadine GC Lu, Nathan W Kuchel, Christoph Grohmann, Yuri Shibata, Zhong Yan Gan, James P Cooney, Marcel Doerflinger, Amanda E Au, Timothy R Blackmore, Gerbrand J van der Heden van Noort, Paul P Geurink, Huib Ovaa, Janet Newman, Alan Riboldi-Tunnicliffe, et al.

Journal article  |  2020  |  EMBO JOURNAL

The SARS-CoV-2 coronavirus encodes an essential papain-like protease domain as part of its non-structural protein (nsp)-3, namely ..

A small molecule interacts with VDAC2 to block mouse BAK-driven apoptosis

Mark F van Delft, Stephane Chappaz, Yelena Khakham, T Bui Chinh, Marlyse A Debrincat, Kym N Lowes, Jason M Brouwer, Christoph Grohmann, Phillip P Sharp, Laura F Dagley, Lucy Li, Kate McArthur, Meng-Xiao Luo, Hui San Chin, W Douglas Fairlie, Erinna F Lee, David Segal, Stephane Duflocq, Romina Lessene, Sabrina Bernard, et al.

Journal article  |  2019  |  NATURE CHEMICAL BIOLOGY

Activating the intrinsic apoptosis pathway with small molecules is now a clinically validated approach to cancer therapy. In contr..

Viral MLKL Homologs Subvert Necroptotic Cell Death by Sequestering Cellular RIPK3

Emma J Petrie, Jarrod J Sandow, Wil IL Lehmann, Lung-Yu Liang, Diane Coursier, Samuel N Young, Wilhelmus JA Kersten, Cheree Fitzgibbon, Andre L Samson, Annette V Jacobsen, Kym N Lowes, Amanda E Au, Helene Jousset Sabroux, Najoua Lalaoui, Andrew I Webb, Guillaume Lessene, Gerard Manning, Isabelle S Lucet, James M Murphy

Journal article  |  2019  |  CELL REPORTS

Necroptotic cell death has been implicated in many human pathologies and is thought to have evolved as an innate immunity mechanis..

Colorectal Cancer Cell Line Proteomes Are Representative of Primary Tumors and Predict Drug Sensitivity

Jing Wang, Dmitri Mouradov, Xiaojing Wang, Robert N Jorissen, Matthew C Chambers, Lisa J Zimmerman, Suhas Vasaikar, Christopher G Love, Shan Li, Kym Lowes, Karl-Johan Leuchowius, Helene Jousset, Janet Weinstock, Christopher Yau, John Mariadason, Zhiao Shi, Yuguan Ban, Xi Chen, Robert JC Coffey, Robbert JC Slebos, et al.

Journal article  |  2017  |  GASTROENTEROLOGY

BACKGROUND AND AIMS: Proteomics holds promise for individualizing cancer treatment. We analyzed to what extent the proteomic lands..

Optimization of 2-Anilino 4-Amino Substituted Quinazolines into Potent Antimalarial Agents with Oral in Vivo Activity

Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Subroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs

Journal article  |  2017  |  JOURNAL OF MEDICINAL CHEMISTRY

Novel antimalarial therapeutics that target multiple stages of the parasite lifecycle are urgently required to tackle the emerging..

Exploration of the P-3 region of PEXEL peptidomimetics leads to a potent inhibitor of the Plasmodium protease, plasmepsin V

Michelle Gazdik, Kate E Jarman, Matthew T O'Neill, Anthony N Hodder, Kym N Lowes, Helene Jousset Sabroux, Alan F Cowman, Justin A Boddey, Brad E Sleebs

Journal article  |  2016  |  BIOORGANIC & MEDICINAL CHEMISTRY

The use of arginine isosteres is a known strategy to overcome poor membrane permeability commonly associated with peptides or pept..