molecularbindingmodeofpf232798aclinicalantihivcandidateatchemokinereceptorccr5

	molecularbindingmodeofpf232798aclinicalantihivcandidateatchemokinereceptorccr5
	Ya Zhu 1; Yanlong Zhao 1; Jian Li 1; Hong Liu 1; Qiang Zhao 1; Beili Wu 1; Zhenlin Yang 1
刊名	中国药理学报英文版
	2019
卷号	040 期号:004 页码:563
关键词	CCR5 anti-HIV PF-232798 maraviroc antagonist crystal structure
ISSN号	1671-4083
英文摘要	The chemokine receptor CCR5 is an important anti-HIV (human immunodeficiency virus) drug target owning to its pivotal role in HIV-1 viral entry as a co-receptor. Here, we present a 2.9 A resolution crystal structure of CCR5 bound to PF-232798, a secondgeneration oral CCR5 antagonist currently in phase II clinical trials. PF-232798 and the marketed HIV drug maraviroc share a similar tropane scaffold with different amino (A/)- and carboxyl (Q- substituents. Comparison of the CCR5-PF-232798 structure with the previously determi ned structure of CCR5 in complex with maraviroc reveals d iff ere nt bindi ng modes of the two allosteric an tago nists and subseque nt con formati onal cha nges of the receptor. Our results not only offer in sights into the phe nomenon that PF-232798 has higher affinity and alternative resista nee profile to maraviroc, but also will facilitate the desig n of new an ti-HIV drugs.
语种	英语
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/283573]
专题	中国科学院上海药物研究所
作者单位	1.中国科学院 2.中国科学院大学 3.上海科技大学 4.中国科学院上海药物研究所
推荐引用方式 GB/T 7714	Ya Zhu,Yanlong Zhao,Jian Li,et al. molecularbindingmodeofpf232798aclinicalantihivcandidateatchemokinereceptorccr5[J]. 中国药理学报英文版,2019,040(004):563.
APA	Ya Zhu.,Yanlong Zhao.,Jian Li.,Hong Liu.,Qiang Zhao.,...&Zhenlin Yang.(2019).molecularbindingmodeofpf232798aclinicalantihivcandidateatchemokinereceptorccr5.中国药理学报英文版,040(004),563.
MLA	Ya Zhu,et al."molecularbindingmodeofpf232798aclinicalantihivcandidateatchemokinereceptorccr5".中国药理学报英文版 040.004(2019):563.