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Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond
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.
Characterisation of sterol biosynthesis and validation of 14α-demethylase as a drug target in Acanthamoeba
- S. Thomson, C. Rice, Tong Zhang, R. Edrada-Ebel, F. Henriquez, C. Roberts
- BiologyScientific Reports
- 15 August 2017
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.
Phenotypic Screens Reveal Posaconazole as a Rapidly Acting Amebicidal Combination Partner for Treatment of Primary Amoebic Meningoencephalitis
- B. Colon, C. Rice, R. Guy, D. Kyle
- Biology, MedicineThe Journal of infectious diseases
- 24 October 2018
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.
Bis-Benzimidazole Hits against Naegleria fowleri Discovered with New High-Throughput Screens
- C. Rice, B. Colon, M. Alp, H. Göker, D. Boykin, D. Kyle
- BiologyAntimicrobial Agents and Chemotherapy
- 20 January 2015
The mono- and diamidino derivatives offer potential for lead optimization to develop new drugs to treat central nervous system infections with N. fowleri.
Keikipukalides, Furanocembrane Diterpenes from the Antarctic Deep Sea Octocoral Plumarella delicatissima
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.
Discovery of repurposing drug candidates for the treatment of diseases caused by pathogenic free-living amoebae
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.
Exploitation of Mangrove Endophytic Fungi for Infectious Disease Drug Discovery
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.
Discovery of Anti-Amoebic Inhibitors from Screening the MMV Pandemic Response Box on Balamuthia mandrillaris, Naegleria fowleri, and Acanthamoeba castellanii
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.
Structural and functional studies of histidine biosynthesis in Acanthamoeba spp. demonstrates a novel molecular arrangement and target for antimicrobials
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.
Synthesis, Cytotoxicity and Genotoxicity of 10-Aza-9-oxakalkitoxin, An N,N,O-Trisubstituted Hydroxylamine Analog, or Hydroxalog, of a Marine Natural Product.
- Sandeep Dhanju, K. Upadhyaya, D. Crich
- Biology, ChemistryJournal of the American Chemical Society
- 4 May 2020
10-aza-9-oxakalkitoxin is an N,N,O-trisubstituted hydroxylamine-based analog, or hydroxalog, of the cytotoxic marine natural product kalkit toxin in which the -NMe-O- moiety replaces a -CHMe-CH2- unit in the backbone of the natural product.