抗艾滋病药物洛匹那韦/利托那韦可激活苦味受体。

IF 2.8 4区 心理学 Q1 BEHAVIORAL SCIENCES Chemical Senses Pub Date : 2023-01-01 DOI:10.1093/chemse/bjad035
Shurui Chen, Xinyi Zhou, Yongcheng Lu, Keman Xu, Jiao Wen, Meng Cui
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引用次数: 0

摘要

洛匹那韦和利托那韦(LPV/r)是世界卫生组织推荐的主要抗人类免疫缺陷病毒(HIV)药物,用于治疗3岁及以上感染HIV的儿童。这些药物通常以液体制剂的形式提供,以帮助无法吞咽药片的儿童给药。然而,与这些药物相关的强烈苦味可能是依从性的重大障碍,尤其是在幼儿中,并可能危及治疗的有效性。研究表明,适口性差会影响艾滋病毒感染儿童的存活率。因此,开发更适合儿童的蛋白酶抑制剂配方,特别是那些味道更好的配方,对感染艾滋病毒的儿童至关重要。洛匹那韦和利托那韦激活苦味受体TAS2Rs的分子机制尚不清楚。在这项研究中,我们利用钙动员试验来表征洛匹那韦和利托那韦对苦味受体的激活。我们发现洛匹那韦激活TAS2R1和TAS2R13,而利托那韦激活塔斯2R1、塔斯2R8、塔斯2R13和塔斯2R14。开发安全靶向这些受体的苦味阻断剂,对于消除这些抗HIV药物令人不快的苦味是非常可取的。
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Anti-HIV drugs lopinavir/ritonavir activate bitter taste receptors.

Lopinavir and ritonavir (LPV/r) are the primary anti-human immunodeficiency virus (HIV) drugs recommended by the World Health Organization for treating children aged 3 years and above who are infected with the HIV. These drugs are typically available in liquid formulations to aid in dosing for children who cannot swallow tablets. However, the strong bitter taste associated with these medications can be a significant obstacle to adherence, particularly in young children, and can jeopardize the effectiveness of the treatment. Studies have shown that poor palatability can affect the survival rate of HIV-infected children. Therefore, developing more child-friendly protease inhibitor formulations, particularly those with improved taste, is critical for children with HIV. The molecular mechanism by which lopinavir and ritonavir activate bitter taste receptors, TAS2Rs, is not yet clear. In this study, we utilized a calcium mobilization assay to characterize the activation of bitter taste receptors by lopinavir and ritonavir. We discovered that lopinavir activates TAS2R1 and TAS2R13, while ritonavir activates TAS2R1, TAS2R8, TAS2R13, and TAS2R14. The development of bitter taste blockers that target these receptors with a safe profile would be highly desirable in eliminating the unpleasant bitter taste of these anti-HIV drugs.

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来源期刊
Chemical Senses
Chemical Senses 医学-行为科学
CiteScore
8.60
自引率
2.90%
发文量
25
审稿时长
1 months
期刊介绍: Chemical Senses publishes original research and review papers on all aspects of chemoreception in both humans and animals. An important part of the journal''s coverage is devoted to techniques and the development and application of new methods for investigating chemoreception and chemosensory structures.
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