目前,批准用于治疗 AIDS 的抗病毒药物主要有黏附抑制剂(attachment inhibitors,AIs)、逆转录酶抑制剂(reverse transcriptase inhibitors,RTIs)、蛋白酶抑制剂(protease inhibitors,PIs)、整合酶抑制剂(integrase inhibitors,INs)、融合抑制...
Kim D. JandaPeter WirschingUS5827827 * 1996年6月20日 1998年10月27日 The Scripps Research Institute HIV-1 protease inhibitors
Atazanvirand fosamprenavir are two recently approved HIV-1 protease inhibitors.Atazanavir,( BMS-232632)2-5: is a type of antiretroviral agent called a protease inhibitor (PI). It blocks protease, a protein that HIV needs to make more copies of it. It is indicated in combination with other ...
2. WHO. HIV fact sheet[EB/OL].https://www.who.int/zh/news-room/fact-sheets/detail/hiv-aids2019; 3. Research progress in the development of HIV-1 protease inhibitors( 2015 - 2019),2020.
Accordingly, specific, exogenous inhibition of the HIV-1 protease is thought to be a viable approach for the development of novel therapeutics for the treatment of AIDS. Indeed, this hypothesis has been validated in virally-infected cell culture with synthetic inhibitors of HIV-1 protease. This ...
Identification of Novel HIV 1- Protease Inhibitors: Application of Ligand and Structure Based Pharmacophore Mapping and Virtual Screening. PLoS One. 2012;7(11): 关于浦华 深圳浦华系统技术有限公司专注于能源化工和生命科学领域信息化的开拓与创新。浦华作为达索系统(Dassault Systèmes)的合作伙伴,基于达索系统...
随着全面抗病毒治疗(ART)范围的逐步扩大,艾滋病病毒(HIV)耐药也逐渐地出现,而且呈现地区不平衡的特点,这直接导致了ART失败率增高以及地区间治疗较大的差异。HIV在宿主体内复制过程中离不开反转录酶(reverse transcriptase),蛋白酶(protease)和整合酶(integrase)。
G. A convergent synthesis of novel confor- mationally restricted HIV-1 protease inhibitors. Tetrahedron Lett. 1994, 35, 5153-5156.Kim, B. M.; Guare, J. P.; Hanifin, C. M.; Arfordbickerstaff, D. J.; Vacca, J. P.; Ball, R. G. A convergent synthesis novel conformationally ...
HIV-1 protease inhibitors. A review for clinicians. The clinical care of people infected with human immunodeficiency virus (HIV) has been substantially affected by the introduction of HIV-specific protease i... S,G,Deeks,... - 《Jama the Journal of the American Medical Association》 被引量:...
theG86mutationschangetheflapregion’sconformationandslightlypushedawayfromtheactivesiteloopregionandhenceweakenthebindingaffinities.Theobtainedresultsinthisstudyshouldbehelpfulforstudyingthebindingmechanismbetweenreceptorandligandanddesigningpotentinhibitorscombatingdiseases.KeyWords:HIV-1protease,inhibitor,moleculedynamic...