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Human African trypanosomiasis: pharmacological re‐engagement with a neglected disease
- M. Barrett, D. Boykin, R. Brun, R. Tidwell
- BiologyBritish Journal of Pharmacology
- 1 December 2007
The challenges of chemotherapy for human African trypanosomiasis (HAT) are discussed, and the few drugs registered for use against the disease are unsatisfactory for a number of reasons.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
- M. Hammerschlag, C. Dykstra, D. Vandewiele
- Computer ScienceAntimicrobial Agents and Chemotherapy
- 1 January 2007
Because the abstract will be published separately by abstracting services, it must be complete and understandable without reference to the text.
New Treatment Option for Second-Stage African Sleeping Sickness: In Vitro and In Vivo Efficacy of Aza Analogs of DB289
- T. Wenzler, D. Boykin, M. Ismail, J. Hall, R. Tidwell, R. Brun
- BiologyAntimicrobial Agents and Chemotherapy
- 20 July 2009
DB868 with oral and DB829 with parenteral application are potential candidates for further development of a second-stage African sleeping sickness drug.
Accumulation and Intracellular Distribution of Antitrypanosomal Diamidine Compounds DB75 and DB820 in African Trypanosomes
It is shown that DB75 and DB820 rapidly accumulate and strongly concentrate within trypanosomes, with intracellular concentrations over 15,000-fold higher than mouse plasma concentrations.
CYP4F Enzymes Are the Major Enzymes in Human Liver Microsomes That Catalyze the O-Demethylation of the Antiparasitic Prodrug DB289 [2,5-Bis(4-amidinophenyl)furan-bis-O-methylamidoxime]
- Michael Zhuo Wang, Janelle Y Saulter, J. Hall
- Biology, ChemistryDrug Metabolism And Disposition
- 1 December 2006
An in vitro metabolism study to characterize enzymes in human liver microsomes (HLMs) that catalyze the initial O-demethylation of DB289 confirmed that M1 formation is catalyzed by P450 enzymes, and indicated that members of the CYP4F subfamily biotransform not only endogenous compounds but also xenobiotics.
Antileishmanial Activities of Several Classes of Aromatic Dications
- J. Brendle, Abram Outlaw, K. Werbovetz
- Chemistry, BiologyAntimicrobial Agents and Chemotherapy
- 1 March 2002
The structure-activity relationships demonstrate the potent antileishmanial activity of several aromatic dications and provide valuable information for the future design and synthesis of more potent antiparasitic agents.
A gel‐free MS‐based quantitative proteomic approach accurately measures cytochrome P450 protein concentrations in human liver microsomes
- Michael Zhuo Wang, J. Wu, J. Hall
- BiologyProteomics
- 1 October 2008
This work has developed a gel‐free MS‐based protein quantification strategy to quantify CYP3A enzymes in human liver microsomes (HLM), which should facilitate P450 characterization during drug development, especially when specific substrates and/or antibodies are unavailable.
Mechanisms Underlying Differences in Systemic Exposure of Structurally Similar Active Metabolites: Comparison of Two Preclinical Hepatic Models
- Grace Zhixia Yan, K. Brouwer, M. Paine
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 May 2011
Selection of in vitro models that accurately characterize metabolite systemic and hepatobiliary exposure remains a challenge in drug development. In the present study, mechanisms underlying…
Transport of Dicationic Drugs Pentamidine and Furamidine by Human Organic Cation Transporters
- X. Ming, Wujian Ju, Huali Wu, R. Tidwell, J. Hall, D. Thakker
- Biology, ChemistryDrug Metabolism And Disposition
- 1 February 2009
This is the first finding that dicationic drugs, such as pentamidine and furamidine, are substrates for hOCT1, which may play important roles in the disposition of aromatic diamidines in humans, as well as resultant drug-drug interactions and toxicity involving diamidine drugs.
Novel Arylimidamides for Treatment of Visceral Leishmaniasis
- Michael Zhuo Wang, Xiaohua Zhu, K. Werbovetz
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 5 April 2010
It is demonstrated that arylimidamides are a promising class of molecules that possess good antileishmanial activity and desirable pharmacokinetics and should be considered for further preclinical development as an oral treatment for VL.
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