Viruses, Vol. 15, Pages 490: HIV Drug Resistance in Adults Initiating or Reinitiating Antiretroviral Therapy in Uruguay & mdash;Results of a Nationally Representative Survey, 2018 & ndash;2019
Viruses, Vol. 15, Pages 490: HIV Drug Resistance in Adults Initiating or Reinitiating Antiretroviral Therapy in Uruguay—Results of a Nationally Representative Survey, 2018–2019
Viruses doi: 10.3390/v15020490
Authors:
Rosa Flieller
Susana Cabrera
Dora Ruchansky
Amalia Girón-Callejas
María Brasesco
Daniel Pérez
Héctor Chiparelli
Claudia García-Morales
Daniela Tapia-Trejo
Jessica Monreal-Flores
Giovanni Ravasi
Michael R. Jordan
Santiago Ávila-Ríos
The first nationally representative cross-sectional HIV drug resistance (HIVDR) survey was conducted in Uruguay in 2018&am...
Source: Viruses - February 10, 2023 Category: Virology Authors: Rosa Flieller Susana Cabrera Dora Ruchansky Amalia Gir ón-Callejas Mar ía Brasesco Daniel P érez H éctor Chiparelli Claudia Garc ía-Morales Daniela Tapia-Trejo Jessica Monreal-Flores Giovanni Ravasi Michael R. Jordan Santiago Ávila-Ríos Tags: Article Source Type: research
Evaluation of Darunavir-derived HIV-1 protease inhibitors incorporating P2' amide-derivatives: Synthesis, biological evaluation and structural studies
We report here the synthesis and biological evaluation of darunavir derived HIV-1 protease inhibitors and their functional effect on enzyme inhibition and antiviral activity in MT-2 cell lines. The P2' 4-amino functionality was modified to make a number of amide derivatives to interact with residues in the S2' subsite of the HIV-1 protease active site. Several compounds exhibited picomolar enzyme inhibitory and low nanomolar antiviral activity. The X-ray crystal structure of the chloroacetate derivative bound to HIV-1 protease was determined. Interestingly, the active chloroacetate group converted to the acetate functional...
Source: Bioorganic and Medicinal Chemistry Letters - February 4, 2023 Category: Chemistry Authors: Arun K Ghosh Dana Shahabi Maya Kipfmiller Ajay K Ghosh Megan Johnson Yuan-Fang Wang Johnson Agniswamy Masayuki Amano Irene T Weber Hiroaki Mitsuya Source Type: research
Evaluation of COVID-19 protease and HIV inhibitors interactions
In this study, we performed a molecular docking of anti-HIV drugs to refine HIV protease inhibitors and nucleotide analogues to target COVID-19. The evaluation was based on docking scores calculated by AutoDock Vina and top binding poses were analyzed. Our results suggested that lopinavir, darunavir, atazanavir, remdesivir, and tipranavir have the best binding affinity for the 3-chymotrypsin-like protease of COVID-19. The comparison of the binding sites of three drugs, namely, darunavir, atazanavir and remdesivir, showed an overlap region of the protein pocket. Our study showed a strong affinity between lopinavir, darunavi...
Source: Acta Pharmaceutica - January 18, 2023 Category: Drugs & Pharmacology Authors: Linh Tran Dao Ngoc Hien Tam Heba Elhadad Nguyen Minh Hien Nguyen Tien Huy Source Type: research
Evaluation of COVID-19 protease and HIV inhibitors interactions
In this study, we performed a molecular docking of anti-HIV drugs to refine HIV protease inhibitors and nucleotide analogues to target COVID-19. The evaluation was based on docking scores calculated by AutoDock Vina and top binding poses were analyzed. Our results suggested that lopinavir, darunavir, atazanavir, remdesivir, and tipranavir have the best binding affinity for the 3-chymotrypsin-like protease of COVID-19. The comparison of the binding sites of three drugs, namely, darunavir, atazanavir and remdesivir, showed an overlap region of the protein pocket. Our study showed a strong affinity between lopinavir, darunavi...
Source: Acta Pharmaceutica - January 18, 2023 Category: Drugs & Pharmacology Authors: Linh Tran Dao Ngoc Hien Tam Heba Elhadad Nguyen Minh Hien Nguyen Tien Huy Source Type: research
Evaluation of COVID-19 protease and HIV inhibitors interactions
In this study, we performed a molecular docking of anti-HIV drugs to refine HIV protease inhibitors and nucleotide analogues to target COVID-19. The evaluation was based on docking scores calculated by AutoDock Vina and top binding poses were analyzed. Our results suggested that lopinavir, darunavir, atazanavir, remdesivir, and tipranavir have the best binding affinity for the 3-chymotrypsin-like protease of COVID-19. The comparison of the binding sites of three drugs, namely, darunavir, atazanavir and remdesivir, showed an overlap region of the protein pocket. Our study showed a strong affinity between lopinavir, darunavi...
Source: Acta Pharmaceutica - January 18, 2023 Category: Drugs & Pharmacology Authors: Linh Tran Dao Ngoc Hien Tam Heba Elhadad Nguyen Minh Hien Nguyen Tien Huy Source Type: research
Evaluation of COVID-19 protease and HIV inhibitors interactions
In this study, we performed a molecular docking of anti-HIV drugs to refine HIV protease inhibitors and nucleotide analogues to target COVID-19. The evaluation was based on docking scores calculated by AutoDock Vina and top binding poses were analyzed. Our results suggested that lopinavir, darunavir, atazanavir, remdesivir, and tipranavir have the best binding affinity for the 3-chymotrypsin-like protease of COVID-19. The comparison of the binding sites of three drugs, namely, darunavir, atazanavir and remdesivir, showed an overlap region of the protein pocket. Our study showed a strong affinity between lopinavir, darunavi...
Source: Acta Pharmaceutica - January 18, 2023 Category: Drugs & Pharmacology Authors: Linh Tran Dao Ngoc Hien Tam Heba Elhadad Nguyen Minh Hien Nguyen Tien Huy Source Type: research
Evaluation of COVID-19 protease and HIV inhibitors interactions
In this study, we performed a molecular docking of anti-HIV drugs to refine HIV protease inhibitors and nucleotide analogues to target COVID-19. The evaluation was based on docking scores calculated by AutoDock Vina and top binding poses were analyzed. Our results suggested that lopinavir, darunavir, atazanavir, remdesivir, and tipranavir have the best binding affinity for the 3-chymotrypsin-like protease of COVID-19. The comparison of the binding sites of three drugs, namely, darunavir, atazanavir and remdesivir, showed an overlap region of the protein pocket. Our study showed a strong affinity between lopinavir, darunavi...
Source: Acta Pharmaceutica - January 18, 2023 Category: Drugs & Pharmacology Authors: Linh Tran Dao Ngoc Hien Tam Heba Elhadad Nguyen Minh Hien Nguyen Tien Huy Source Type: research
Viruses, Vol. 15, Pages 213: Multi-Targeting Approach in Selection of Potential Molecule for COVID-19 Treatment
dra Nayak
The coronavirus disease (COVID-19) is a pandemic that started in the City of Wuhan, Hubei Province, China, caused by the spread of coronavirus (SARS-CoV-2). Drug discovery teams around the globe are in a race to develop a medicine for its management. It takes time for a novel molecule to enter the market, and the ideal way is to exploit the already approved drugs and repurpose them therapeutically. We have attempted to screen selected molecules with an affinity towards multiple protein targets in COVID-19 using the Schrödinger suit for in silico predictions. The proteins selected were angiotensin...
Source: Viruses - January 12, 2023 Category: Virology Authors: Varalakshmi Velagacherla Akhil Suresh Chetan Hasmukh Mehta Usha Y. Nayak Yogendra Nayak Tags: Article Source Type: research
Low incidence of advanced neurological burden but high incidence of age-related conditions that are dementia risk factors in aging people living with HIV: a data-linkage 10-year follow-up study
AbstractAlthough increasing research is focusing on age-related comorbidities (ARC) among people living with HIV (PLHIV), no studies have concomitantly assessed non-HIV age-related neurological disorders (e.g., Alzheimer ’s dementia). A total of 254 PLHIV and 69 HIV-negative controls completed baseline medical history and cognitive testing. ARC data were collected from medical records over the subsequent 9-10 years and included all types of strokes, all types of dementia, mild cognitive impairment, Parkinson's dis ease, motor neuron disease (grouped into a non-HIV age-related neurological category), cardiovascular diseas...
Source: Journal of NeuroVirology - December 12, 2022 Category: Neurology Source Type: research
Understanding drug resistance patterns across different classes of antiretrovirals used in HIV-1-infected treatment-Na & #239;ve and experienced patients in Mumbai, India
Conclusion: An increased incidence of HLR was observed for NNRTI as compared to NRTI while PIs and integrase strand transfer inhibitors (INSTIs) demonstrated no HLR in either group of patients. When selecting a regimen for Tn patients consisting of NRTIs + NNRTIs genotypic DR test is essential. While with PIs or INSTIs its optional. Among Te patients, DR testing is recommended for all classes of drugs. (Source: Indian Journal of Sexually Transmitted Diseases)
Source: Indian Journal of Sexually Transmitted Diseases - November 17, 2022 Category: Infectious Diseases Authors: Raj Gurubuxrai Harjani Asha Krishnaraj Iyer Ankita Chaurasia Source Type: research
HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway
Antiviral Res. 2022 Nov 10:105463. doi: 10.1016/j.antiviral.2022.105463. Online ahead of print.ABSTRACTHIV-associated neurocognitive disorder (HAND) is prevalent in people living with HIV, despite the use of antiretroviral therapy (ART). Although several risk factors have been proposed to be related to HAND, substantial effort has been made to explore the neurotoxic effects of ART on HAND. HIV protease inhibitor (PI), an essential component of ART, has neurotoxicity in vivo and in vitro, which can contribute to the development of HAND. However, the pathogenesis of PI-associated neurotoxicity remains unclear. Here, we explo...
Source: Antiviral Research - November 13, 2022 Category: Virology Authors: Xue Chen Wei Ding Xiao Cui Jiaqi Wei Yang Zhang Xin Zhang Tong Zhang Yulin Zhang Source Type: research
HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway
Antiviral Res. 2022 Nov 10:105463. doi: 10.1016/j.antiviral.2022.105463. Online ahead of print.ABSTRACTHIV-associated neurocognitive disorder (HAND) is prevalent in people living with HIV, despite the use of antiretroviral therapy (ART). Although several risk factors have been proposed to be related to HAND, substantial effort has been made to explore the neurotoxic effects of ART on HAND. HIV protease inhibitor (PI), an essential component of ART, has neurotoxicity in vivo and in vitro, which can contribute to the development of HAND. However, the pathogenesis of PI-associated neurotoxicity remains unclear. Here, we explo...
Source: Antiviral Research - November 13, 2022 Category: Virology Authors: Xue Chen Wei Ding Xiao Cui Jiaqi Wei Yang Zhang Xin Zhang Tong Zhang Yulin Zhang Source Type: research
HIV protease inhibitor attenuated astrocyte autophagy involvement in inflammation via p38 MAPK pathway
Antiviral Res. 2022 Nov 10:105463. doi: 10.1016/j.antiviral.2022.105463. Online ahead of print.ABSTRACTHIV-associated neurocognitive disorder (HAND) is prevalent in people living with HIV, despite the use of antiretroviral therapy (ART). Although several risk factors have been proposed to be related to HAND, substantial effort has been made to explore the neurotoxic effects of ART on HAND. HIV protease inhibitor (PI), an essential component of ART, has neurotoxicity in vivo and in vitro, which can contribute to the development of HAND. However, the pathogenesis of PI-associated neurotoxicity remains unclear. Here, we explo...
Source: Antiviral Research - November 13, 2022 Category: Virology Authors: Xue Chen Wei Ding Xiao Cui Jiaqi Wei Yang Zhang Xin Zhang Tong Zhang Yulin Zhang Source Type: research
