撞击激酶抑制剂1294可治疗已有的弓形虫感染。
Bumped kinase inhibitor 1294 treats established Toxoplasma gondii infection.
作者信息
Doggett J Stone, Ojo Kayode K, Fan Erkang, Maly Dustin J, Van Voorhis Wesley C
机构信息
VA Medical Center, Portland, Oregon, USA Division of Infectious Diseases, Oregon Health & Science University, Portland, Oregon, USA
Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA.
出版信息
Antimicrob Agents Chemother. 2014 Jun;58(6):3547-9. doi: 10.1128/AAC.01823-13. Epub 2014 Mar 31.
Abstract
Toxoplasma gondii is a unicellular parasite that causes severe brain and eye disease. Current drugs for T. gondii are limited by toxicity. Bumped kinase inhibitors (BKIs) selectively inhibit calcium-dependent protein kinases of the apicomplexan pathogens T. gondii, cryptosporidia, and plasmodia. A lead anti-Toxoplasma BKI, 1294, has been developed to be metabolically stable and orally bioavailable. Herein, we demonstrate the oral efficacy of 1294 against toxoplasmosis in vivo.
摘要
刚地弓形虫是一种单细胞寄生虫，可引发严重的脑部和眼部疾病。目前用于治疗刚地弓形虫的药物存在毒性限制。碰撞激酶抑制剂（BKIs）可选择性抑制顶复门病原体刚地弓形虫、隐孢子虫和疟原虫的钙依赖性蛋白激酶。一种先导抗弓形虫BKIs，即1294，已被开发出来，具有代谢稳定性和口服生物利用度。在此，我们展示了1294在体内抗弓形虫病的口服疗效。
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