INTHERES, Université de Toulouse, INRAE, ENVT, Toulouse, France.
INTHERES, Université de Toulouse, INRAE, ENVT, Toulouse, France.
Trends Parasitol. 2024 Oct;40(10):896-913. doi: 10.1016/j.pt.2024.07.008. Epub 2024 Aug 20.
P-glycoprotein (PGP) is a pivotal transmembrane transporter governing the cellular flux of diverse substances shielding mammals from toxics. It can thwart the effectiveness of medicines such as ivermectin (IVM) and other macrocyclic lactone (ML) anthelmintics, undermining therapeutic efforts. We analyze the role of PGPs in limiting the toxicity of these drugs in hosts, and their potential contribution to anthelmintic resistance in nematodes. Targeting nematode PGPs to increase drug sensitivity to MLs seems interesting, but is hampered by the lack of selective inhibitors. The nuclear hormone receptor (NHR)-8 should be seriously considered as a target because it upregulates multiple PGPs involved in anthelmintic resistance and it is specific to nematodes. This would advance our understanding of host-pathogen dynamics and foster innovative therapeutic strategies.
P-糖蛋白(PGP)是一种重要的跨膜转运蛋白,负责调节多种物质在细胞内的流动,使哺乳动物免受毒物的侵害。它可以降低伊维菌素(IVM)和其他大环内酯类驱虫药等药物的疗效,从而破坏治疗效果。我们分析了 PGPs 在限制这些药物在宿主中的毒性以及它们对线虫驱虫剂耐药性的潜在贡献。靶向线虫 PGPs 以提高对 MLs 的药物敏感性似乎很有意义,但受到缺乏选择性抑制剂的阻碍。核激素受体(NHR)-8 应该被认真考虑作为一个靶点,因为它上调了多种与驱虫剂耐药性相关的 PGPs,而且它是线虫特异性的。这将有助于我们理解宿主-病原体的相互作用,并促进创新的治疗策略。