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Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond
TLDR
The results reveal the immense potential for translating the dispersed expertise in biological assays involving human pathogens into drug discovery starting points, by providing open access to new families of molecules, and emphasize how a small additional investment made to help acquire and distribute compounds, and sharing the data, can catalyze drug discovery for dozens of different indications. Expand
Characterisation of sterol biosynthesis and validation of 14α-demethylase as a drug target in Acanthamoeba
TLDR
It is demonstrated that the major sterol of Acanthamoeba castellanii is ergosterol and novel putative precursors and intermediate sterols in its production are identified and provided a putative framework for their further study. Expand
Bis-Benzimidazole Hits against Naegleria fowleri Discovered with New High-Throughput Screens
TLDR
The mono- and diamidino derivatives offer potential for lead optimization to develop new drugs to treat central nervous system infections with N. fowleri. Expand
Exploitation of Mangrove Endophytic Fungi for Infectious Disease Drug Discovery
TLDR
A screening program to assess the potential of mangrove-derived endophytic fungi as a source of new antibiotics found that more than 60% of active extracts were revealed to be selective to a single target, validating the technique of using small molecules to dysregulate secondary metabolite production pathways. Expand
Phenotypic Screens Reveal Posaconazole as a Rapidly Acting Amebicidal Combination Partner for Treatment of Primary Amoebic Meningoencephalitis
TLDR
Posaconazole was found to inhibit amoeba growth within the first 12 hours of exposure, which was faster than any currently used drug, and could replace fluconazole in the treatment of PAM. Expand
Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae
TLDR
The results of these studies demonstrate the utility of phenotypic screens for discovery of new drugs for pathogenic free-living amoebae, including Acanthamoeba for the first time and validate new targets for structure-based drug design. Expand
Structural and functional studies of histidine biosynthesis in Acanthamoeba spp. demonstrates a novel molecular arrangement and target for antimicrobials
TLDR
It is demonstrated that Acanthamoeba is a histidine autotroph, but with the ability to scavenge preformed histidine, and the potential therapeutic utility of targeting this with antimicrobials is explored. Expand
Keikipukalides, Furanocembrane Diterpenes from the Antarctic Deep Sea Octocoral Plumarella delicatissima
TLDR
Five new furanocembranoid diterpenes, keikipukalides A–E (1–5), the known diterpene pukalide aldehyde, and the known norditerpenoid ineleganolide (7) were isolated from the coral. Expand
Discovery of anti-amoebic inhibitors from screening the MMV Pandemic Response Box on Balamuthia mandrillaris, Naegleria fowleri and Acanthamoeba castellanii
TLDR
These structures serve as a starting point for medicinal chemistry studies and demonstrate the utility of phenotypic screening for drug discovery to treat diseases caused by free-living amoebae. Expand
Conservation of Ancient Genetic Pathways for Intracellular Persistence Among Animal Pathogenic Bordetellae
TLDR
Analysis of the survival of B. bronchiseptica shows that the ability to persist inside macrophage-like RAW 264.7 cells is shared among nearly all Bordetella species, suggesting that resisting phagocytes may be an ancient mechanism that precedes speciation in the genus and may have facilitated the adaptation of Bordetlla species from environmental bacteria to mammalian respiratory pathogens. Expand
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