Although protease acts at the last step of the virus life cycle, protease inhibitors were discovered shortly after nucleoside reverse transcriptase inhibitors. The era of HIV protease inhibitor drugs began in 1996 with the i...
Although protease acts at the last step of the virus life cycle, protease inhibitors were discovered shortly after nucleoside reverse tranase inhibitors. The era of HIV protease inhibitor drugs began in 1996 with the introduction of saquinavir, indinavir, and ritonavir as the first-generation HIV pr...
The last 5 years have witnessed a transition from peptide-like inhibitors that are generally marginal as drugs because of poor solubility and/or bioavailability, to smaller, nonpeptide, organic molecules with enhanced pharmacokinetic properties. The process of protease inhibitor development has encompassed...
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...
[17] Bhagwat P, Ofotokun I, McComsey GA,et al. Changes in waist circumference in HIV-infectedindividuals initiating a raltegravir or protease inhibitor regimen: efects of sex and race[J]. Open Forum InfectDis, 2018, 5(11):ofy201. ...
[12] Daar E S, DeJesus E, Ruane P, et al. Efficacy and safety of switching to fixed-dose bictegravir, emtricitabine, and tenofovir alafenamide from boosted protease inhibitor-based regimens in virologically suppressed adults with HIV-1: 48 week results of a randomised, open-label, multicentr...
Inhibitor99.87% Lopinavir (ABT-378) 是一种高效、选择性肽模拟HIV-1蛋白酶 (HIV-1protease) 的抑制剂,对野生型和突变型HIV蛋白酶的抑制Kis值为 1.3 到 3.6 pM。Lopinavir 通过阻止HIV-1的成熟而起作用,从而阻断其感染性。Lopinavir 也是SARS-CoV3CLpro的抑制剂,IC50为 14.2 μM。
Contraindicated statin use in people living with HIV have declined between 2007 and 2014 because of less frequent preions for HIV protease inhibitors. 由于HIV蛋白酶抑制剂的处方使用频率较低,在2007年至2014年期间,HIV感染者中禁止使用他汀类药物的情况有所减少。
Purpose: The development of new cancer drugs is slow and costly. HIV protease inhibitors are Food and Drug Administration approved for HIV patients. Because these drugs cause toxicities that can be associated with inhibition of Akt, an emerging target in cancer, we assessed the potential of HIV ...
HIV感染者的寿命随着抗反转录病毒治疗(ART)的普及得到大幅提高,已接近非HIV感染者的寿命,HIV感染逐渐成为了一种慢性疾病,非AIDS定义性疾病已经取代HIV相关性疾病成为HIV感染者的主要死亡原因[1],尤其是包括心血管疾病(CVD)在内的代谢相关疾病,CVD是继肝病后非AIDS