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Scaleable manufacture of HIV-1 entry inhibitor griffithsin and validation of its safety and efficacy as a topical microbicide component
- B. O’Keefe, F. Vojdani, K. Palmer
- BiologyProceedings of the National Academy of Sciences
- 14 April 2009
A manufacturing breakthrough for griffithsin (GRFT), one of the most potent HIV entry inhibitors, is reported, which has broad-spectrum activity against HIV clades A, B, and C, with utility as a microbicide component for HIV prevention in established epidemics in sub-Saharan Africa, South Asia, China, and the industrialized West.
A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria
The excellent safety profile, blood- and liver-stage activity, and predicted long half-life in humans position DSM265 as a new potential drug combination partner for either single-dose treatment or once-weekly chemoprevention of malaria.
(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium
- M. Jiménez-Díaz, D. Ebert, R. Guy
- Biology, MedicineProceedings of the National Academy of Sciences
- 1 December 2014
The results demonstrate that targeting ATP4 has great potential to deliver useful drugs for malaria eradication and suggest that inhibitors of PfATP4 have highly attractive features for fast-acting antimalarials to be used in the global eradication campaign.
Preclinical Evaluations To Identify Optimal Linezolid Regimens for Tuberculosis Therapy
Findings show that with linezolid monotherapy, a clear tradeoff exists between antibacterial activity and toxicity, and can provide valuable insight for designing optimal dosage regimens for lineZolid that are part of the long combination courses used to treat multidrug-resistant M. tuberculosis.
Micronucleated erythrocyte frequency in peripheral blood of B6C3F1 mice from short‐term, prechronic, and chronic studies of the NTP carcinogenesis bioassay program
- K. Witt, A. Knapton, J. T. Macgregor
- Biology, Environmental ScienceEnvironmental and molecular mutagenesis
The mouse peripheral blood micronucleus (MN) test has been proposed as a useful adjunct to rodent toxicity tests and has been effectively incorporated as a routine part of overall toxicity testing by the NTP.
Measurement of unscheduled DNA synthesis and S‐phase synthesis in rodent hepatocytes following in vivo treatment: Testing of 24 compounds
Results indicate that most of the test compounds do not induce UDS in the liver; however, the significant S‐phase response induced by many of these compounds, especially the halogenated solvents, may be an important mechanism in their hepatocarcinogenicity.
Detection of genotoxic carcinogens in the in vivo-in vitro hepatocyte DNA repair assay.
The in vivo-in vitro hepatocyte DNA repair assay is valuable for the detection and study of a variety of genotoxic carcinogens.
In vivo transgenic mutation assays.
In vivo transgenic mutation assays
Transgenic rodent gene mutation models provide quick and statistically reliable assays for mutations in the DNA from any tissue, and Sequencing data would not normally be required but might provide useful additional information in specific circumstances.
Chromium (VI) at plausible drinking water concentrations is not genotoxic in the in vivo bone marrow micronucleus or liver unscheduled DNA synthesis assays
- J. Mirsalis, C. Hamilton, K. O’Loughlin, D. Paustenbach, B. Kerger, S. Patierno
- BiologyEnvironmental and molecular mutagenesis
This study examines the potential in vivo genotoxicity of Chromium(VI) in drinking water at concentrations ranging from the relevant human exposure level of 1 mg/l to the upper limit of palatability…