Alan Cowman

7-N-Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc1 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 Infect Dis

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  |  J Med Chem

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

RH5.1-CyRPA-Ripr antigen combination vaccine shows little improvement over RH5.1 in a preclinical setting

Julie Healer, Jennifer KK Thompson, Karen LL Mackwell, Cecille DD Browne, Benjamin AA Seager, Anna Ngo, Kym NN Lowes, Sarah EE Silk, David Pulido, Lloyd DW King, Jayne MM Christen, Amy RR Noe, Vinayaka Kotraiah, Paul JJ Masendycz, Rajkannan Rajagopalan, Leanne Lucas, Marianne MM Stanford, Lorraine Soisson, Carter Diggs, Robin Miller, et al.

Journal article  |  2022  |  FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY

BACKGROUND: RH5 is the leading vaccine candidate for the Plasmodium falciparum blood stage and has shown impact on parasite growth..

PCRCR complex is essential for invasion of human erythrocytes by Plasmodium falciparum

Stephen W Scally, Tony Triglia, Cindy Evelyn, Benjamin A Seager, Michal Pasternak, Pailene S Lim, Julie Healer, Niall D Geoghegan, Amy Adair, Wai-Hong Tham, Laura F Dagley, Kelly L Rogers, Alan F Cowman

Journal article  |  2022  |  NATURE MICROBIOLOGY

The most severe form of malaria is caused by Plasmodium falciparum. These parasites invade human erythrocytes, and an essential st..

Nanobodies against Pfs230 block Plasmodium falciparum transmission

Melanie H Dietrich, Mikha Gabriela, Kitsanapong Reaksudsan, Matthew WA Dixon, Li-Jin Chan, Amy Adair, Stephanie Trickey, Matthew TO 'Neill, Li Lynn Tan, Sash Lopaticki, Julie Healer, Sravya Keremane, Alan F Cowman, Wai-Hong Tham

Journal article  |  2022  |  BIOCHEMICAL JOURNAL

Transmission blocking interventions can stop malaria parasite transmission from mosquito to human by inhibiting parasite infection..

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..

Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

Martin A Lowe, Alvaro Cardenas, Jean-Pierre Valentin, Zhaoning Zhu, Jan Abendroth, Jose L Castro, Reiner Class, Annie Delaunois, Renaud Fleurance, Helga Gerets, Vitalina Gryshkova, Lloyd King, Donald D Lorimer, Malcolm MacCoss, Julian H Rowley, Marie-Luce Rosseels, Leandro Royer, Richard D Taylor, Melanie Wong, Oliver Zaccheo, et al.

Journal article  |  2022  |  JOURNAL OF MEDICINAL CHEMISTRY

Plasmepsin X (PMX) is an essential aspartyl protease controlling malaria parasite egress and invasion of erythrocytes, development..

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 ..

The Plasmodium falciparum parasitophorous vacuole protein P113 interacts with the parasite protein export machinery and maintains normal vacuole architecture

Hayley E Bullen, Paul R Sanders, Madeline G Dans, Thorey K Jonsdottir, David T Riglar, Oliver Looker, Catherine S Palmer, Betty Kouskousis, Sarah C Charnaud, Tony Triglia, Mikha Gabriela, Molly Parkyn Schneider, Jo-Anne Chan, Tania F de Koning-Ward, Jake Baum, James W Kazura, James G Beeson, Alan F Cowman, Paul R Gilson, Brendan S Crabb

Journal article  |  2022  |  MOLECULAR MICROBIOLOGY

Infection with Plasmodium falciparum parasites results in approximately 627,000 deaths from malaria annually. Key to the parasite'..