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NNRTI HIV

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https://www.readbyqxmd.com/read/28905420/the-hiv-1-p66-homodimeric-rt-exhibits-different-conformations-in-the-binding-competent-and-incompetent-nnrti-site
#1
Naima G Sharaf, Zhaoyong Xi, Rieko Ishima, Angela M Gronenborn
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (RT), NNRTIs, which bind to the p66/p51 heterodimeric RT, also interact with the p66/p66 homodimer, whose structure is unknown. (19) F NMR of a single 4-trifluoromethylphenylalanine (tfmF) residue, incorporated into the NNRTI binding pocket of the p66/p66 homodimer at position 181, was used to investigate NNRTI binding. In the NNRTI-bound homodimer complex, two different (19) F signals are observed, with the resonance frequencies matching those of the NNRTI-bound p66/p51 heterodimer spectra, in which the individual p66- or p51-subunits were labeled with tfmF at positions 181...
September 14, 2017: Proteins
https://www.readbyqxmd.com/read/28903520/hepatic-renal-hematologic-and-inflammatory-markers-in-hiv-infected-children-on-long-term-suppressive-antiretroviral-therapy
#2
Ann J Melvin, Meredith Warshaw, Alexandra Compagnucci, Yacine Saidi, Linda Harrison, Anna Turkova, Gareth Tudor-Williams
Background: Data on long-term toxicity of antiretroviral therapy (ART) in HIV-infected children are sparse. PENPACT-1 was an open-label trial in which HIV-infected children were assigned randomly to receive protease inhibitor (PI)- or nonnucleoside reverse-transcriptase inhibitor (NNRTI)-based ART. Methods: We examined changes in clinical, immunologic, and inflammatory markers from baseline to year 4 in the subset of children in the PENPACT-1 study who experienced viral suppression between week 24 and year 4 of ART...
September 1, 2017: Journal of the Pediatric Infectious Diseases Society
https://www.readbyqxmd.com/read/28870148/accumulation-of-hiv-1-drug-resistance-in-patients-on-a-standard-thymidine-analogue-based-first-line-antiretroviral-therapy-after-virological-failure-implications-for-the-activity-of-next-line-regimens-from-a-longitudinal-study-in-mozambique
#3
Andrea De Luca, Zita Jorge Sidumo, Giacomo Zanelli, Noorjehan Abdul Magid, Richard Luhanga, Davide Brambilla, Giuseppe Liotta, Sandro Mancinelli, Maria Cristina Marazzi, Leonardo Palombi, Susanna Ceffa
BACKGROUND: We describe the accumulation of HIV-1 drug resistance and its effect on the activity of next-line components in patients with virological failure (HIV-1 RNA >1000 copies/mL) after 1 year (t1) of first-line antiretroviral therapy (ART) not switching to second-line drugs for one additional year (t2) in low-middle income countries (LMIC). METHODS AND RESULTS: We selected 48 patients from the DREAM cohort (Maputo, Mozambique); their median pre-ART CD4+ cell count was 165 cells/μl...
September 5, 2017: BMC Infectious Diseases
https://www.readbyqxmd.com/read/28859436/prevalence-of-drug-resistant-minority-variants-in-untreated-hiv-1-infected-individuals-with-and-those-without-transmitted-drug-resistance-detected-by-sanger-sequencing
#4
Dana S Clutter, Shuntai Zhou, Vici Varghese, Soo-Yon Rhee, Benjamin A Pinsky, W Jeffrey Fessel, Daniel B Klein, Ean Spielvogel, Susan P Holmes, Leo B Hurley, Michael J Silverberg, Ronald Swanstrom, Robert W Shafer
Minority variant human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase inhibitor (NNRTI) resistance mutations are associated with an increased risk of virological failure during treatment with NNRTI-containing regimens. To determine whether individuals to whom variants with isolated NNRTI-associated drug resistance were transmitted are at increased risk of virological failure during treatment with a non-NNRTI-containing regimen, we identified minority variant resistance mutations in 33 individuals with isolated NNRTI-associated transmitted drug resistance and 49 matched controls...
August 1, 2017: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/28859311/design-synthesis-and-antiviral-evaluation-of-novel-heteroarylcarbothioamide-derivatives-as-dual-inhibitors-of-hiv-1-reverse-transcriptase-associated-rnase-h-and-rddp-functions
#5
Angela Corona, Valentina Onnis, Alessandro Deplano, Giulia Bianco, Monica Demurtas, Simona Distinto, Yung-Chi Cheng, Stefano Alcaro, Francesca Esposito, Enzo Tramontano
In the continuous effort to identify new HIV-1 inhibitors endowed with innovative mechanisms, the dual inhibition of different viral functions would provide a significant advantage against drug-resistant variants. The HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) is the only viral-encoded enzymatic activity that still lacks an efficient inhibitor. We synthesized a library of 3,5-diamino-N-aryl-1H-pyrazole-4-carbothioamide and 4-amino-5-benzoyl-N-phenyl-2-(substituted-amino)-1H-pyrrole-3-carbothioamide derivatives and tested them against RNase H activity...
August 31, 2017: Pathogens and Disease
https://www.readbyqxmd.com/read/28841912/choice-of-initial-antiretroviral-drugs-and-treatment-outcomes-among-hiv-infected-patients-in-sub-saharan-africa-systematic-review-and-meta-analysis-of-observational-studies
#6
Tadesse Awoke Ayele, Alemayehu Worku, Yigzaw Kebede, Kassahun Alemu, Adetayo Kasim, Ziv Shkedy
BACKGROUND: The effectiveness of antiretroviral therapy (ART) depends on the choice of regimens during initiation. Most evidences from developed countries indicated that there is difference between efavirenz (EFV) and nevirapine (NVP). However, the evidences are limited in resource poor countries particularly in Africa. Thus, this systematic review and meta-analysis was carried out to summarize reported long-term treatment outcomes among people on first line therapy in sub-Saharan Africa...
August 25, 2017: Systematic Reviews
https://www.readbyqxmd.com/read/28832407/prevalence-and-clinical-impacts-of-hiv-1-intersubtype-recombinants-in-uganda-revealed-by-a-near-full-genome-population-and-deep-sequencing-approaches
#7
Guinevere Q Lee, David R Bangsberg, Theresa Mo, Chris Lachowski, Chanson J Brumme, Wendy Zhang, Viviane D Lima, Yap Boum, Bosco Bwana Mwebesa, Conrad Muzoora, Iren Andia, Yona Mbalibulha, Annet Kembabazi, Ryan Carroll, Mark J Siedner, Jessica E Haberer, A Rain Mocello, Simone H Kigozi, Peter W Hunt, Jeffrey N Martin, P Richard Harrigan
OBJECTIVES: To estimate prevalence, examine time trends, and test for clinical correlates and outcomes associated with HIV-1 intersubtype recombination under a full-genome sequencing context in a rural community in Mbarara, Uganda, where HIV-1 subtypes A1 and D co-circulate. METHODS: Near-full-genome HIV-1 Sanger sequence data was collected from plasma samples of 504 treatment-naïve individuals, who then received PI or NNRTI-containing regimens and were monitored for up to 7...
August 21, 2017: AIDS
https://www.readbyqxmd.com/read/28830014/ultradeep-sequencing-of-b-and-non-b-hiv-1-subtypes-viral-diversity-and-drug-resistance-mutations-before-and-after-one-month-of-antiretroviral-therapy-in-naive-patients
#8
Olivier Epaulard, Anne Signori-Schmuck, Sylvie Larrat, Om Kulkarni, Michael G Blum, Katia Fusillier, Myriam Blanc, Pascale Leclercq, Olivier François, Patrice Morand
BACKGROUND: Ultradeep pyrosequencing technologies permit an assessment of the genetic diversity and the presence and frequency of minority variants in a viral population. The effect of these parameters on the outcome of highly active antiretroviral therapy (HAART) in HIV-infected patients is poorly understood. OBJECTIVES: The present study used the pyrosequencing Roche 454 prototype assay to determine whether antiretroviral efficacy is correlated with viral diversity and minority drug resistance mutations in HIV-infected treatment-naive patients and to compare assay performance in B and non-B subtypes...
July 25, 2017: Journal of Clinical Virology: the Official Publication of the Pan American Society for Clinical Virology
https://www.readbyqxmd.com/read/28827354/covalent-inhibitors-for-eradication-of-drug-resistant-hiv-1-reverse-transcriptase-from-design-to-protein-crystallography
#9
Albert H Chan, Won-Gil Lee, Krasimir A Spasov, José A Cisneros, Shalley N Kudalkar, Zaritza O Petrova, Amanda B Buckingham, Karen S Anderson, William L Jorgensen
Development of resistance remains a major challenge for drugs to treat HIV-1 infections, including those targeting the essential viral polymerase, HIV-1 reverse transcriptase (RT). Resistance associated with the Tyr181Cys mutation in HIV-1 RT has been a key roadblock in the discovery of nonnucleoside RT inhibitors (NNRTIs). It is the principal point mutation that arises from treatment of HIV-infected patients with nevirapine, the first-in-class drug still widely used, especially in developing countries. We report covalent inhibitors of Tyr181Cys RT (CRTIs) that can completely knock out activity of the resistant mutant and of the particularly challenging Lys103Asn/Tyr181Cys variant...
August 21, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28812250/miv-150-and-zinc-acetate-combination-provides-potent-and-broad-activity-against-hiv-1
#10
Olga Mizenina, Mayla Hsu, Ninochka Jean-Pierre, Meropi Aravantinou, Keith Levendosky, Gabriela Paglini, Thomas M Zydowsky, Melissa Robbiani, José A Fernández-Romero
We previously showed that the combination of the non-nucleoside reverse transcriptase inhibitor (NNRTI) MIV-150 with zinc acetate (ZA) formulated in a carrageenan (CG; MZC) gel provided macaques significant protection against vaginal simian-human immunodeficiency virus-RT (SHIV-RT) challenge, better than either MIV-150/CG or ZA/CG. The MZC gel was shown to be safe in a phase 1 clinical trial. Herein, we used in vitro approaches to study the antiviral properties of ZA and the MIV-150/ZA combination, compared to other NNRTIs...
August 15, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28799325/comparison-between-next-generation-and-sanger-based-sequencing-for-the-detection-of-transmitted-drug-resistance-mutations-among-recently-infected-hiv-1-patients-in-israel-2000-2014
#11
Roy Moscona, Daniela Ram, Marina Wax, Efrat Bucris, Itzchak Levy, Ella Mendelson, Orna Mor
INTRODUCTION: Transmitted drug-resistance mutations (TDRM) may hamper successful anti-HIV-1 therapy and impact future control of the HIV-1 epidemic. Recently infected, therapy-naïve individuals are best suited for surveillance of such TDRM. In this study, TDRM, detected by next-generation sequencing (NGS) were compared to those identified by Sanger-based population sequencing (SBS) in recently infected HIV-1 patients. METHODS: Historical samples from 80 recently infected HIV-1 patients, diagnosed between 2000 and 2014, were analysed by MiSeq (NGS) and ABI (SBS)...
August 11, 2017: Journal of the International AIDS Society
https://www.readbyqxmd.com/read/28797181/hiv-resistance-with-correlation-to-pmtct-regimen-in-hiv-infected-infants-in-northern-tanzania
#12
Dorothy Elizabeth Dow, Werner Schimana, Balthazar M Nyombi, Blandina T Mmbaga, Aisa M Shayo, John A Bartlett, Charles G Massambu, Emmanuel G Kifaro, Elizabeth L Turner, Todd DeMarco, Fangping Cai, Coleen Cunningham, Ann M Buchanan
Prevention of mother-to-child transmission (PMTCT) guidelines recommend that all HIV-infected pregnant woman receive antiretroviral therapy (Option B) and HIV-infected infants should initiate therapy with a protease inhibitor based regimen; however, implementation of these guidelines has lagged in many resource-limited settings. Tanzania only recently implemented these guidelines with little country specific data to inform whether HIV non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance was present among infected infants under the Option A guidelines...
August 11, 2017: AIDS Research and Human Retroviruses
https://www.readbyqxmd.com/read/28753637/collaborative-update-of-a-rule-based-expert-system-for-hiv-1-genotypic-resistance-test-interpretation
#13
Roger Paredes, Philip L Tzou, Gert van Zyl, Geoff Barrow, Ricardo Camacho, Sergio Carmona, Philip M Grant, Ravindra K Gupta, Raph L Hamers, P Richard Harrigan, Michael R Jordan, Rami Kantor, David A Katzenstein, Daniel R Kuritzkes, Frank Maldarelli, Dan Otelea, Carole L Wallis, Jonathan M Schapiro, Robert W Shafer
INTRODUCTION: HIV-1 genotypic resistance test (GRT) interpretation systems (IS) require updates as new studies on HIV-1 drug resistance are published and as treatment guidelines evolve. METHODS: An expert panel was created to provide recommendations for the update of the Stanford HIV Drug Resistance Database (HIVDB) GRT-IS. The panel was polled on the ARVs to be included in a GRT report, and the drug-resistance interpretations associated with 160 drug-resistance mutation (DRM) pattern-ARV combinations...
2017: PloS One
https://www.readbyqxmd.com/read/28750647/high-level-of-hiv-1-drug-resistance-mutations-in-patients-with-unsuppressed-viral-loads-in-rural-northern-south-africa
#14
Elizabeth M Etta, Lufuno Mavhandu, Cecile Manhaeve, Keanan McGonigle, Patrick Jackson, David Rekosh, Marie-Louise Hammarskjold, Pascal O Bessong, Denis M Tebit
BACKGROUND: Combination antiretroviral therapy (cART) has significantly reduced HIV morbidity and mortality in both developed and developing countries. However, the sustainability of cART may be compromised by the emergence of viral drug resistance mutations (DRM) and the cellular persistence of proviruses carrying these DRM. This is potentially a more serious problem in resource limited settings. METHODS: DRM were evaluated in individuals with unsuppressed viral loads after first or multiple lines of cART at two sites in rural Limpopo, South Africa...
July 27, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28738474/-hiv-1-drug-resistance-transmission-threshold-survey-in-dehong-prefecture-of-yunnan-province-2015
#15
M Chen, J B Wang, H Xing, Y L Ma, J Yang, H C Chen, S T Yao, H B Luo, X Duan, Y K Wang, S Duan, M H Jia
Objective: To study the HIV-1 drug resistance transmission level in HIV infected persons receiving no antiviral therapy in Dehong prefecture of Yunnan province in 2015. Methods: A total of 72 plasma samples were collected from recently reported HIV-infected persons aged 16-25 years in Dehong from January to July 2015 for drug resistance gene detection. Results: Forty eight samples were successfully sequenced and analyzed. Among them, 31.2% (15/48) were from Chinese, and 68.8% (33/48) were from Burmese. Based on pol sequences, HIV genotypes included URF (52...
July 10, 2017: Zhonghua Liu Xing Bing Xue za Zhi, Zhonghua Liuxingbingxue Zazhi
https://www.readbyqxmd.com/read/28732792/drug-resistance-in-b-and-non-b-subtypes-amongst-subjects-recently-diagnosed-as-primary-recent-or-chronic-hiv-infected-over-the-period-2013-2016-impact-on-susceptibility-to-first-line-strategies-including-integrase-strand-transfer-inhibitors
#16
Samantha Andreis, Monica Basso, Renzo Scaggiante, Mario Cruciani, Roberto Ferretto, Vinicio Manfrin, Sandro Panese, Maria Cristina Rossi, Ermenegildo Francavilla, Caterina Boldrin, Mario Alvarez, Federico Dal Bello, Carlo Mengoli, Ombretta Turriziani, Loredana Sarmati, Guido Antonelli, Massimo Andreoni, Giorgio Palù, Saverio Giuseppe Parisi
OBJECTIVES: To characterize the prevalence of transmitted drug resistance mutations (TDRMs) by plasma analysis of 750 patients at the time of HIV diagnosis from January 1, 2013 to November 16, 2016 in the Veneto region (Italy), where all drugs included in the recommended first line therapies were prescribed, included integrase strand transfer inhibitors (InNSTI). METHODS: TDRMs were defined according to the Stanford HIV database algorithm. RESULTS: Subtype B was the most prevalent HIV clade (67...
September 2017: Journal of Global Antimicrobial Resistance
https://www.readbyqxmd.com/read/28722475/ann-qsar-workflow-for-predicting-the-inhibition-of-hiv-1-reverse-transcriptase-by-pyridinone-non-nucleoside-derivatives
#17
Abolfazl Barzegar, Elham Zamani-Gharehchamani, Ali Kadkhodaie-Ilkhchi
AIM: Pyridinone derivatives have high potency against non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant human immunodeficiency virus type-1 strains. Quantitative structure-activity relationship (QSAR) studies on a series of pyridinone derivatives acting as NNRTIs are very important in designing the next generation of NNRTIs. Methodology & results: The QSAR models were developed using linear (single and forward stepwise) and combined nonlinear artificial neural network (ANN) approaches...
July 19, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28715160/meeting-the-who-90-target-antiretroviral-treatment-efficacy-in-poland-is-associated-with-baseline-clinical-patient-characteristics
#18
Milosz Parczewski, Ewa Siwak, Magdalena Leszczyszyn-Pynka, Iwona Cielniak, Ewa Burkacka, Piotr Pulik, Adam Witor, Karolina Muller, Ewelina Zasik, Anna Grzeszczuk, Maria Jankowska, Małgorzata Lemańska, Anita Olczak, Edyta Grąbczewska, Aleksandra Szymczak, Jacek Gąsiorowski, Bartosz Szetela, Monika Bociąga-Jasik, Paweł Skwara, Magdalena Witak-Jędra, Elżbieta Jabłonowska, Kamila Wójcik-Cichy, Juliusz Kamerys, Małgorzata Janczarek, Dagny Krankowska, Tomasz Mikuła, Katarzyna Kozieł, Dariusz Bielec, Justyna Stempkowska, Aleksandra Kocbach, Wiesława Błudzin, Andrzej Horban
INTRODUCTION: Modern combined antiretroviral therapies (cART) allow to effectively suppress HIV-1 viral load, with the 90% virologic success rate, meeting the WHO target in most clinical settings. The aim of this study was to analyse antiretroviral treatment efficacy in Poland and to identify variables associated with virologic suppression. M: ethods Cross-sectional data on 5152 (56.92% of the countrywide treated at the time-point of analysis) patients on cART for more than six months with at least one HIV-RNA measurement in 2016 were collected from 14 Polish centres...
July 17, 2017: Journal of the International AIDS Society
https://www.readbyqxmd.com/read/28696229/mdr1-and-bcrp-transporter-mediated-drug-drug-interaction-between-rilpivirine-and-abacavir-and-effect-on-intestinal-absorption
#19
Josef Reznicek, Martina Ceckova, Zuzana Ptackova, Ondrej Martinec, Lenka Tupova, Lukas Cerveny, Frantisek Staud
Rilpivirine (TMC278) is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI) representing an effective component of combination antiretroviral therapy (cART) in the treatment of HIV-positive patients. Many antiretroviral drugs commonly used in cART are substrates of ATP-binding cassette (ABC) and/or solute carrier (SLC) drug transporters and, therefore, are prone to pharmacokinetic drug-drug interactions (DDIs). The aim of our study was to evaluate rilpivirine interactions with abacavir and lamivudine on selected ABC and SLC transporters in vitro and assess its importance for pharmacokinetics in vivo Using accumulation assays in MDCK cells overexpressing selected ABC or SLC drug transporters, we revealed rilpivirine as a potent inhibitor of MDR1 and BCRP, but not MRP2, OCT1, OCT2, or MATE1...
September 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28692532/cardiovascular-outcomes-among-hiv-infected-veterans-receiving-atazanavir-a-us-national-historical-cohort-study
#20
Joanne Lafleur, Adam P Bress, Lisa Rosenblatt, Jacob Crook, Paul E Sax, Joel Myers, Corey Ritchings
OBJECTIVE: Patients with HIV infection have an increased risk of cardiovascular disease compared with uninfected individuals. Antiretroviral therapy with atazanavir delays progression of atherosclerosis markers; whether this reduces cardiovascular disease event risk compared with other antiretroviral regimens is currently unknown. DESIGN: Population-based, non-interventional, historical cohort study conducted from July 1, 2003, through December 31, 2015. SETTING: Veterans Health Administration (VHA) hospitals and clinics throughout the United States...
July 7, 2017: AIDS
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