Brad Sleebs

7-N-Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc(1) Complex

William Nguyen, Madeline G Dans, Iain Currie, Jon Kyle Awalt, Brodie L Bailey, Chris Lumb, Anna Ngo, Paola Favuzza, Josephine Palandri, Saishyam Ramesh, Jocelyn Penington, Kate E Jarman, Partha Mukherjee, Arnish Chakraborty, Alexander G Maier, Giel G van Dooren, Tony Papenfuss, Sergio Wittlin, Alisje Churchyard, Jake Baum, et al.

Journal article  |  2023  |  ACS INFECTIOUS DISEASES

The development of new antimalarials is required because of the threat of resistance to current antimalarial therapies. To discove..

Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4

Trent D Ashton, Madeline G Dans, Paola Favuzza, Anna Ngo, Adele M Lehane, Xinxin Zhang, Deyun Qiu, Bikash Chandra Maity, Nirupam De, Kyra A Schindler, Tomas Yeo, Heekuk Park, Anne-Catrin Uhlemann, Alisje Churchyard, Jake Baum, David A Fidock, Kate E Jarman, Kym N Lowes, Delphine Baud, Stephen Brand, et al.

Journal article  |  2023  |  JOURNAL OF MEDICINAL CHEMISTRY

There is an urgent need to populate the antimalarial clinical portfolio with new candidates because of resistance against frontlin..

Design and characterization of a heterobifunctional degrader of KEAP1

Hao Chen, Nghi H Nguyen, Charlene M Magtoto, Simon A Cobbold, Grace M Bidgood, Lizeth G Meza Guzman, Lachlan W Richardson, Jason Corbin, Amanda E Au, Bernhard C Lechtenberg, Rebecca Feltham, Kate D Sutherland, Christoph Grohmann, Sandra E Nicholson, Brad E Sleebs

Journal article  |  2023  |  REDOX BIOLOGY

The Kelch-like ECH-associated protein 1 (KEAP1) - nuclear factor erythroid 2-related factor 2 (NRF2) signaling pathway senses reac..

Targeting malaria parasites with novel derivatives of azithromycin

Amy L Burns, Brad E Sleebs, Maria Gancheva, Kimberley T McLean, Ghizal Siddiqui, Henrietta Venter, James G Beeson, Ryan O'Handley, Darren J Creek, Shutao Ma, Sonja Froelich, Christopher D Goodman, Geoffrey McFadden, Danny W Wilson

Journal article  |  2022  |  FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY

INTRODUCTION: The spread of artemisinin resistant Plasmodium falciparum parasites is of global concern and highlights the need to ..

Thermal proteome profiling reveals Haemonchus orphan protein HCO_011565 as a target of the nematocidal small molecule UMW-868

Aya CC Taki, Tao Wang, Nghi NN Nguyen, Ching-Seng Ang, Michael GG Leeming, Shuai Nie, Joseph JJ Byrne, Neil DD Young, Yuanting Zheng, Guangxu Ma, Pasi KK Korhonen, Anson VV Koehler, Nicholas AA Williamson, Andreas Hofmann, Bill CH Chang, Cecile Haeberli, Jennifer Keiser, Abdul Jabbar, Brad EE Sleebs, Robin BB Gasser

Journal article  |  2022  |  FRONTIERS IN PHARMACOLOGY

Parasitic roundworms (nematodes) cause destructive diseases, and immense suffering in humans and other animals around the world. T..

The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria

Manuel de Lera Ruiz, Paola Favuzza, Zhuyan Guo, Lianyun Zhao, Bin Hu, Zhiyu Lei, Dongmei Zhan, Nicholas Murgolo, Christopher W Boyce, Marissa Vavrek, Jennifer Thompson, Anna Ngo, Kate E Jarman, Johnathan Robbins, Justin Boddey, Brad E Sleebs, Kym N Lowes, Alan F Cowman, David B Olsen, John A McCauley

Journal article  |  2022  |  ACS MEDICINAL CHEMISTRY LETTERS

Drug resistance to first-line antimalarials-including artemisinin-is increasing, resulting in a critical need for the discovery of..

Australian chemistry and drug discovery towards the development of antimalarials

Brad E Sleebs

Journal article  |  2022  |  AUSTRALIAN JOURNAL OF CHEMISTRY

Malaria, a disease caused by the Plasmodium parasite, accounts for more than 450 000 deaths annually. The devastating impact of th..

The Medicines for Malaria Venture Malaria Box contains inhibitors of protein secretion in Plasmodium falciparum blood stage parasites

Oliver Looker, Madeline G Dans, Hayley E Bullen, Brad E Sleebs, Brendan S Crabb, Paul R Gilson

Journal article  |  2022  |  TRAFFIC

Plasmodium falciparum parasites which cause malaria, traffic hundreds of proteins into the red blood cells (RBCs) they infect. The..

Substrate Peptidomimetic Inhibitors of P. falciparum Plasmepsin X with Potent Antimalarial Activity

Lachlan W Richardson, Trent D Ashton, Madeline G Dans, Nghi Nguyen, Paola Favuzza, Tony Triglia, Anthony N Hodder, Anna Ngo, Kate E Jarman, Alan F Cowman, Brad E Sleebs

Journal article  |  2022  |  CHEMMEDCHEM

Plasmepsin X (PMX) is an aspartyl protease that processes proteins essential for Plasmodium parasites to invade and egress from ho..

Basis for drug selectivity of plasmepsin IX and X inhibition in Plasmodium falciparum and vivax

Anthony N Hodder, Janni Christensen, Stephen Scally, Tony Triglia, Anna Ngo, Richard W Birkinshaw, Brodie Bailey, Paola Favuzza, Melanie H Dietrich, Wai-Hong Tham, Peter E Czabotar, Kym Lowes, Zhuyan Guo, Nicholas Murgolo, Manuel de Lera Ruiz, John A McCauley, Brad E Sleebs, David Olsen, Alan F Cowman

Journal article  |  2022  |  STRUCTURE

Plasmepsins IX (PMIX) and X (PMX) are essential aspartyl proteases for Plasmodium spp. egress, invasion, and development. WM4 and ..