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

Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned.
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碰撞激酶抑制剂作为Apicomplexan寄生虫疾病的疗法:经验教训。

DOI:
10.1016/j.ijpara.2020.01.006
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发表时间:
2020-05
影响因子:
4
通讯作者:
Van Voorhis WC
Van Voorhis WC
中科院分区:
医学2区
文献类型:
--
作者:
Choi R;Hulverson MA;Huang W;Vidadala RSR;Whitman GR;Barrett LK;Schaefer DA;Betzer DP;Riggs MW;Doggett JS;Hemphill A;Ortega-Mora LM;McCloskey MC;Arnold SLM;Hackman RC;Marsh KC;Lynch JJ;Freiberg GM;Leroy BE;Kempf DJ;Choy RKM;de Hostos EL;Maly DJ;Fan E;Ojo KK;Van Voorhis WC

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碰撞激酶抑制剂 (BKI) 通过甘氨酸看门人靶向顶复门寄生虫中的钙依赖性蛋白激酶 1 (CDPK1),是治疗顶复门疾病的有前途的新疗法。在这里,我们将回顾在功效、安全性和药理学方面的进展、挑战和经验教训,这些影响了我们对临床前候选药物的选择。
Bumped Kinase Inhibitors (BKIs), targeting Calcium-dependent Protein Kinase 1 (CDPK1) 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.
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