| Literature DB >> 27018127 |
Bryan C Jensen1, Nick Booster1, Rama Subba Rao Vidadala2, Dustin J Maly3, Marilyn Parsons4.
Abstract
Human African trypanosomiasis a fatal disease for which no vaccines exist and treatment regimens are difficult. Here, we evaluate a Trypanosoma brucei protein kinase, AEK1, as a potential drug target. Conditional knockouts confirmed AEK1 essentiality in bloodstream forms. For chemical validation, we overcame the lack of AEK1 inhibitors by creating parasites expressing a single, functional analog-sensitive AEK1 allele. Analog treatment of mice infected with this strain delayed parasitemia and death, with one-third of animals showing no parasitemia. These studies validate AEK1 as a drug target and highlight the need for further understanding of its function.Entities:
Keywords: AGC kinase; Analog-sensitive; Drug target; In vivo; Protein kinase; Trypanosome
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Year: 2016 PMID: 27018127 PMCID: PMC4925258 DOI: 10.1016/j.ijpara.2016.03.001
Source DB: PubMed Journal: Int J Parasitol ISSN: 0020-7519 Impact factor: 3.981