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bumped 激酶抑制剂作为治疗顶复门寄生虫病的药物:经验教训。

Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned.

机构信息

Department of Medicine, Division of Allergy and Infectious Diseases, Center for Emerging and Reemerging Infectious Diseases (CERID), University of Washington, Seattle, WA 98109, USA.

Department of Biochemistry, University of Washington, Seattle, WA 98195, USA.

出版信息

Int J Parasitol. 2020 May;50(5):413-422. doi: 10.1016/j.ijpara.2020.01.006. Epub 2020 Mar 26.

Abstract

Bumped Kinase Inhibitors, targeting Calcium-dependent Protein Kinase 1 in apicomplexan parasites with a glycine gatekeeper, are promising new therapeutics for apicomplexan diseases. Here we will review advances, as well as challenges and lessons learned regarding efficacy, safety, and pharmacology that have shaped our selection of pre-clinical candidates.

摘要

Bumped 激酶抑制剂靶向顶复门原虫中的钙依赖性蛋白激酶 1,其甘氨酸门控结构使其成为顶复门原虫疾病的有前途的新型治疗药物。在此,我们将回顾在疗效、安全性和药理学方面的进展、挑战和经验教训,这些因素影响了我们对临床前候选药物的选择。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5cc9/8565993/e0ff16ec939c/nihms-1750674-f0001.jpg

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