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Nelfinavir

Nelfinavir is a protease inhibitor used in the treatment of HIV infection.
It is often used in combination with other antiretroviral agents to suppress viral replication and improve clinical outcomes.
Nelfinavir works by binding to the HIV protease enzyme, inhibiting its activity and preventing the maturation of new viral particles.
Research into optimizing Nelfinavir protocols can be enhanced through the use of PubCompare.ai, which helps users locate relevant literature, preprints, and patents, and leverages AI-driven comparisons to identify the best protocols and products.
This can boost reproducibility and accuracy in Nelfinavit research, leading to more effective therapies for those living with HIV.

Most cited protocols related to «Nelfinavir»

Neurodevelopmental Outcomes of Early vs Deferred ART in HIV-Infected Children

Cited 9 times

Our primary objective was to determine neurodevelopmental outcomes at week 144 in early vs. deferred ART children. The secondary objective was to compare these outcomes between the HIV-infected children in PREDICT and their HIV-uninfected peers. We assessed a range of behavioral and cognitive abilities which are at risk for HIV-associated impairment using standardized tests that were in use in Thailand and Cambodia and which have good validity and reliability in their original form.. Neuropsychological tests that required attention, tapping memory, psychomotor speed, and processing speed were selected for administration in this study as these cognitive domains are frequently impaired among HIV-infected individuals. Further, measures that tap these cognitive constructs are relatively brief to administer and score and they minimize language responses. Finally, the selected neuropsychological measures allowed straightforward translation of instructions as well as appropriate methods to ensure data fidelity through staff training and efficient monitoring of accuracy in test administration and scoring. HIV-infected children underwent age-appropriate psychomotor and behavioral assessments every 6 months and cognitive tests annually. The Cambodian sites performed only the psychomotor and behavioral measures; the Intelligence and Memory tests were not administered. The cognitive tests were either the Thai-version of the Wechsler Intelligence Scale for Children (WISC)-III (age 6 to 17 years) or the Wechsler Preschool and Primary Scale of Intelligence (WPPSI)-III (age 2 to 7.25 years), and the Stanford Binet II memory test (Beads/Sentences for age 3.5 to 17 years; Digits/Objects for age 6 to 17 years). The psychomotor assessments were Beery Visual Motor Integration (VMI) (age 2 to 17 years), Purdue Pegboard (age 5 to 17 years) and Children’s Color Trails (age 8 to 17 years). Thai versions of WISC-III, WPPSI-III and Stanford Binet II memory tests were available and widely used in Thailand, and have been validated by the Thai Psychologist Society. The assessments were completed by psychologists at all Thai sites. For the fine motor tests (Berry VMI, Purdue Pegboard and Color Trails), the English instructions were translated into Thai and Khmer by bi-lingual translators. Trained nurses were certified to administer these tests by experienced Thai and US neuropsychologists after correctly performing and scoring a minimum of 10 subjects per test. External quality assurance review by a US neuropsychologist was performed several times over the course of the study. The Child Behavior Checklist (CBCL) was completed by primary caregivers to assess behavioral problems at all sites (age 2 to 17 years), using the preschool (18 months to less than 6 years) and school-aged (age 6–18 years) forms. The English version of CBCL was translated into Thai and Khmer, and then back translated into English to ensure accurate translation. Between 2010–2011, the HIV-uninfected controls (155 born to HIV-infected mothers (“exposed”) and 164 born to HIV-uninfected mothers (“unexposed”) underwent a one-time neurodevelopmental assessment using the same tests. HIV-uninfected/exposed children were recruited from siblings of HIV-infected children and from children delivered to HIV-infected mothers at the study sites. HIV-uninfected/unexposed children were recruited from well-child clinics in the same hospitals. In the HIV-infected children, first-line ART consisted of zidovudine, lamivudine and nevirapine. A protease inhibitor (lopinavir/ritonavir or nelfinavir) was substituted for nevirapine in children with prior exposure to nevirapine as part of PMTCT (nelfinavir was not used after September 2007).¹⁶ The protocol received approval from the Thai and Cambodian National, and local Institutional Review Boards.

Puthanakit T., Ananworanich J., Vonthanak S., Kosalaraksa P., Hansudewechakul R., van der Lugt J., Kerr S.J., Kanjanavanit S., Ngampiyaskul C., Wongsawat J., Luesomboon W., Vibol U., Pruksakaew K., Suwarnlerk T., Apornpong T., Ratanadilok K., Paul R., Mofenson L.M., Fox L., Valcour V., Brouwers P, & Ruxrungtham K. (2013). Cognitive Function and Neurodevelopmental Outcomes in HIV-Infected Children Older than 1 Year of Age Randomized to Early Versus Deferred Antiretroviral Therapy: The PREDICT Neurodevelopmental Study. The Pediatric infectious disease journal, 32(5), 501-508.

Publication 2013

Attention Beer Berries Cambodians Child Child, Preschool Childbirth Cognition Cognitive Testing Ethics Committees, Research Fingers Lamivudine lopinavir-ritonavir drug combination Memory Mothers Nelfinavir Neuropsychological Tests Nevirapine Nurses Problem Behavior Protease Inhibitors Sibling Stanford-Binet Test Thai TNFSF10 protein, human Tongue Zidovudine

Proficiency Testing of Antiretroviral Drugs

Cited 8 times

Every six months the CPQA PT program offered prepared plasma samples containing pre-specified concentrations (unknown to CPLs) of up to 21 ARV analytes: abacavir (ABC), amprenavir (APV), atazanavir (ATV), darunavir (DRV), didanosine (DDI), efavirenz (EFV), emtricitabine (FTC), etravirine (ETR), indinavir (IDV), lamivudine (3TC), lopinavir (LPV), maraviroc (MVC), nelfinavir (NFV), nevirapine (NVP), raltegravir (RGV), ritonavir (RTV), saquinavir (SQV), stavudine (D4T), tenofovir (TFV), tipranavir (TPV), zidovudine (ZDV). In each round and for each ARV, 5 concentrations, spanning an expected therapeutic range of each ARV, as well as occasional concentrations below or above, were provided. Samples are prepared by an outside subcontractor and tested by the CPQA lab prior to distribution. PT samples were stored at −70 ± 15°C and then shipped on dry ice to participating laboratories with detailed instructions. Upon arrival, each laboratory confirmed sample integrity and indicated planned reporting of specific analytes. Results were reported either through an online Laboratory Data Management System (LDMS) or via a template which was then uploaded into the LDMS database. At the end of the submission period, a completeness evaluation was performed to confirm that all planned results were received; discrepancies were queried for resolution. To summarize the proficiency of individual labs, a pre-specified scoring algorithm was applied to the RCs (see next paragraph). The scoring algorithm reflects US Clinical Laboratory Improvement Act (CLIA) PT regulations[13 (link)]. After review and approval by the CPQA advisory board chair, a final report was sent to the participating laboratories (with laboratories de-identified) and key leadership (laboratories identified per network leader).
An individual RC is deemed Acceptable provided a concentration is present where expected, and the concentration is within 20% of the final target (FT)[14 (link)]. (If a concentration is reported as below the lower limit of quantification (BLQ), and the run lower limit was below 80%*FT, the concentration was labeled Unacceptable.) For a given prepared sample, if the number of labs reporting for that sample is large enough, the variability between CPLs is small enough (≤15%) and the percent deviation of the group mean (GM, determined after removal of outliers, if any)from the weighed-in value (WIV) is >5%, the FT is set to the GM. Otherwise, FT is set to the WIV. At the analyte level, a CPL’sperformance is deemed Satisfactory for the round provided at least 80% of RCs are Acceptable. If the CPL score is <80% for an analyte, the CPL submits a corrective action plan to reestablish accuracy; a root cause is requested. Finally, in accordance with CLIA rules, a lab is classified as successful for an analyte provided the round-specific score was Satisfactory in at least 2 of the last 3 rounds (including the current).

DiFrancesco R., Rosenkranz S.L., Taylor C.R., Pande P.G., Siminski S.M., Jenny R.W, & Morse G.D. (2013). Clinical Pharmacology Quality Assurance (CPQA) Program: Models for Longitudinal Analysis of Antiretroviral (ARV) Proficiency Testing for International Laboratories. Therapeutic drug monitoring, 35(5), 631-642.

Publication 2013

abacavir amprenavir Atazanavir Clinical Laboratory Services Darunavir Dry Ice efavirenz etravirine Indinavir Lopinavir Maraviroc Nelfinavir Nevirapine Plant Roots Plasma Raltegravir Ritonavir Saquinavir Tenofovir Therapeutics tipranavir Zidovudine

Cell Viability Assay with MTT

Cited 6 times

Cell viability was tested by MTT assay (Sigma, St. Louis, MO, USA). Briefly, cells were seeded in 96-well plates (4 × 10³ cells/well) and were treated the following day for 48 h with erlotinib, nelfinavir or nitroxoline as single agents, or with combinations of the drugs at various concentrations as indicated. Then, the MTT solution was added to each well and incubated at 37 °C for at least 3 h, until a purple precipitate was visible. In order to dissolve formazan crystals, the culture medium was replaced with dimethyl sulfoxide (DMSO, Euroclone). Absorbance of each well was quantified at 540 and 690 nm, using a Synergy H1 microplate reader (BioTek Instruments Inc., Winooski, VT, USA).

Veschi S., De Lellis L., Florio R., Lanuti P., Massucci A., Tinari N., De Tursi M., di Sebastiano P., Marchisio M., Natoli C, & Cama A. (2018). Effects of repurposed drug candidates nitroxoline and nelfinavir as single agents or in combination with erlotinib in pancreatic cancer cells. Journal of Experimental & Clinical Cancer Research : CR, 37, 236.

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Publication 2018

Biological Assay Cells Cell Survival Culture Media Drug Combinations Erlotinib Formazans Nelfinavir nitroxoline Sulfoxide, Dimethyl

Clonogenic Survival Assay for Radiosensitization

Cited 6 times

Cells were trypsinized to create single cell suspensions, seeded into T-25 flasks at defined densities, and incubated overnight to ensure log phase of growth. The next day, two hours pre-irradiation, cells were fed with fresh media supplemented with either lapatinib (5 μM), U0126 (5 μM), or LY294002 (10 μM). Cells treated with nelfinavir (1 or 5 μM) received 2 or 26 h of pre-treatment prior to irradiation. Control cells were maintained in media containing a corresponding concentration of vehicle (DMSO or ethanol) alone. Cells were irradiated with single doses of 1, 3, 5, or 7 Gy using a Mark I ¹³⁷Cs irradiator (JL Shepherd, San Fernando, CA) delivering a dose rate of 158 cGy/min. Two hours post-irradiation, all drugs were removed and the cells re-fed with fresh media. After 10 to 15 days, surviving colonies were fixed with a solution of methanol and acetic acid (3:1 v/v) and stained with 1% crystal violet. Colonies containing more than 50 cells were counted and survival curves were generated.
The surviving fraction was calculated from the number of colonies formed in the irradiated dishes compared with the number formed in the unirradiated control, where plating efficiency is defined as the percentage of cells plated that form colonies in unirradiated dishes, and surviving fraction = number of colonies formed/(number of cells plated × plating efficiency). Statistical comparisons were done using GraphPad Prism according to the two-tailed nonparametric Mann-Whitney test. The clonogenic survival curve for each condition was fitted to a linear-quadratic model (Y=e^{−[A * X + B * X²]}) using GraphPad Prism according to a least squares fit, weighted to minimize the relative distances squared, and compared using the extra sum-of-squares F test. Each point represents the mean surviving fraction calculated from three independent experiments done in triplicate for each treatment condition; error bars represent the standard deviation. The mean inactivation dose was calculated according to the method of Fertil (21 (link)) and the cell survival enhancement ratio (ER) was calculated as the ratio of the mean inactivation dose under control conditions divided by the mean inactivation dose after drug exposure as described by Morgan (22 (link)). A value significantly greater than 1 indicates radiosensitization. For the drug dose response comparison, two-way ANOVA followed by Bonferroni posttests was performed using GraphPad Prism.

Kimple R.J., Vaseva A.V., Cox A.D., Baerman K.M., Calvo B.F., Tepper J.E., Shields J.M, & Sartor C.I. (2010). Radiosensitization of EGFR/HER2 positive pancreatic cancer is mediated by inhibition of Akt independent of Ras mutational status. Clinical cancer research : an official journal of the American Association for Cancer Research, 16(3), 912.

Publication 2009

Acetic Acid Cells Cell Survival Ethanol Hyperostosis, Diffuse Idiopathic Skeletal Lapatinib LY 294002 Methanol Nelfinavir neuro-oncological ventral antigen 2, human Pharmaceutical Preparations prisma Sulfoxide, Dimethyl U 0126 Violet, Gentian

Modeling of HIV-1 Protease Inhibitor Complexes

Cited 5 times

The simulation systems of the HIV-1 PR-inhibitor complexes were prepared using the crystal structures from PDB (Nelfinavir: 1OHR; Amprenavir: 1HPV). The protein complexes were solvated in rectangular TIP3P⁴⁴ water box using the tleap program of AMBER 10.⁴⁵ The solute atoms were separated from nearest walls of the water box by at least 12 Å. Sodium chloride counterions were added to make the solution charge neutral. The simulation systems of the solvated inhibitors were prepared in a similar way. The solvated enzyme–inhibitor boxes contain about 34000 atoms. The solvated inhibitor systems contain about 4200 atoms.
The Amber ff99SB parameter set^{46 (link)} was used to model the protein in aqueous solutions. The force field parameters of the ligand were obtained using the Antechamber program^{47 (link)} of AMBER 10. The AM1-BCC method⁴⁸ was used to assign the atomic charges for the ligands. In the present study, all the MD simulations were performed using the GROMACS program version 4.04.⁴⁹ The AMBER 10 generated parameters/topology files were converted to the GROMACS format using a Perl script developed by Pande’s group.⁵⁰ Electrostatic interactions were computed using the particle-mesh Ewald (PME) method,⁵¹ with a real space cutoff of 11 Å and a grid spacing of 1.0 Å. A switching function between 9 Å and 10 Å was used for van der Waals interactions. SHAKE⁵² was used to constrain bond lengths involving hydrogen atoms. A stochastic Langevin dynamics integrator with a friction constant of 0.4 ps⁻¹ and a time step of 2 fs was used to integrate the equations of motion and to provide constant temperature control. The following protocol has been used to minimize and equilibrate the solvated system: the solvent alone was first minimized for 500 steps using steepest descent method followed by 500 steps of conjugated gradient method. Following the minimization steps, the system was equilibrated at the target temperature for 200 ps. The equilibration was performed in the NPT ensemble using Berendsen’s weak coupling method for constant pressure control. Finally, the equilibrated system was simulated in the production MD in the NVT ensemble.
To obtain well equilibrated initial configurations for the decoupling simulations, the solvated enzyme–inhibitor complex and the solvated ligand were equilibrated for 10 and 5 ns, respectively. For ligand–protein decoupling calculation, 11 ns simulation was performed on the solvated enzyme–inhibitor complex at each λ value. The first halves of the trajectory were treated as equilibration and the rest of trajectory were used in the thermodynamic integration. For ligand-water decoupling, 1.2 ns simulation was carried out on the solvated ligands at each λ; the data collected in the last 1 ns were used in the calculation. A total of >3 μs free energy simulation data were collected in the current work. The plots of Hamiltonian derivative 〈∂U/∂λ〉_λ obtained from the decoupling simulations were shown in the Supporting Information (SI).

Deng N.J., Zhang P., Cieplak P, & Lai L. (2011). Elucidating the Energetics of Entropically Driven Protein–Ligand Association: Calculations of Absolute Binding Free Energy and Entropy. The journal of physical chemistry. B, 115(41), 11902-11910.

Publication 2011

A-A-1 antibiotic Amber amprenavir Debility Electrostatics Enzyme Inhibitors Friction HIV-1 Hydrogen inhibitors Ligands Multienzyme Complexes Nelfinavir Pressure Proteins Sodium Chloride Solvents STEEP1 protein, human

Most recents protocols related to «Nelfinavir»

Rat Hippocampal Neuron Cultures

Hippocampi were dissected from embryonic day (E) 16 to E18 rat embryos obtained from pregnant Sprague-Dawley dams (Envigo). All animal procedures were approved by the Institutional Animal Care and Use Committee (IACUC) at Columbia University. Cell dissociation was performed using TripLE Express. Neurons (50,000 to 60,000 per microfluidic chamber) were plated on poly-d-lysine (0.1 mg ml⁻¹; MilliporeSigma)– and laminin (2 μg ml⁻¹; Bio-Techne)–coated substrates and grown in Neurobasal supplemented with 10% fetal bovine serum, 2 mM l-glutamine, 1 mM sodium pyruvate, and antibiotics (50 U ml⁻¹ penicillin-streptomycin). Tripartite microfluidic chambers were produced with Dow Corning Sylgard 184 Silicone Encapsulant Clear Kit (10:1 mix ratio; Ellsworth Adhesives) cured at ~70°C for at least 4 hours following published protocols (19 (link)). Chamber design incorporated two sets of 200-μm-long microgroove barriers to exclude the crossing of cell bodies and dendrites. After 24 hours, the medium was changed to Neurobasal containing 1× B27 and 2 mM l-glutamine. Subsequent medium changes (half volumes) were performed at day in vitro 4 (DIV4) and thereafter every 3 to 5 days. To prevent glial cell proliferation, medium changes included 5-flurodeoxyuridine and uridine (final concentration: 10 mM; MilliporeSigma) after DIV4. Neuronal cultures were grown in a 37°C, 5% CO₂ humidified atmosphere until DIV12 to DIV14. Whenever stated, axonal or cell body compartments were treated with 30 μM ciliobrevin A (R&D Systems), 100 nM emetine (MilliporeSigma), or 10/15 μM nelfinavir (MilliporeSigma). Dovitinib (Selleck Chemicals) was bath-applied at 40 nM 30 min before Aβ₄₂ stimulation. Unless otherwise specified, reagents were purchased from Thermo Fisher Scientific.

Gouveia Roque C., Chung K.M., McCurdy E.P., Jagannathan R., Randolph L.K., Herline-Killian K., Baleriola J, & Hengst U. (2023). CREB3L2-ATF4 heterodimerization defines a transcriptional hub of Alzheimer’s disease gene expression linked to neuropathology. Science Advances, 9(9), eadd2671.

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Publication 2023

Animals Antibiotics Atmosphere Axon Bath Cell Body Cell Proliferation Cells Dendrites dovitinib Embryo Emetine Fetal Bovine Serum Glutamine Institutional Animal Care and Use Committees Laminin Lysine Nelfinavir Neuroglia Neurons OAS1 protein, human Penicillins Poly A Pyruvate Seahorses Silicones Sodium Streptomycin Uridine

HIV-1 Viral Protein Detection in CD8-Depleted PBMCs

CD8-depleted PBMC’s were prepared using magnetic bead EasyStep human CD8 positive selection kits II (Cat 17853 StemCell Technologies) before being infected with HIV-1_BAL (NIH HIV Reagent Program) using a predetermined TCID50 as previously described. A total of 40x10⁶ cells were used per condition in the presence of 50 μM QVD-OPH, 40 nM Nelfinavir, or DMSO. Media was changed and fresh compounds added accordingly on Day 3. On Day 6, infected cells were harvested, washed in 1x PBS, and lysed in SDS-free Pierce IP lysis buffer (Cat 87787 ThermoFisher). Aliquots of heterogenous, whole-cell lysates were taken for loading controls. HIV gag proteins were precipitated out using the Dynabeads Protein G immunoprecipitation kit (Cat 10007D ThermoFisher) labeled with unconjugated KC57 coulter clone (IgG1 FH190) antibody (Beckman Coulter) before undergoing SDS-PAGE in 10–20% Novex Wedge-Well tris-glycine gels (Cat XP04200BOX ThermoFisher). Proteins were transferred to 0.45μM nitrocellulose membranes using the iBlot2 dry blotting system (ThermoFisher) before being probed with primary rabbit anti-p55/p24/p17 polyclonal antibody (Cat ab63917 Abcam) or IgG2b mouse anti-human β-actin monoclonal clone BA3R antibody (Cat MA5-15739 ThermoFisher) at 1:2,000 in 2% BSA PBS-T (1x PBS/0.1% Tween20) for 1 hour. Membranes were washed in PBS-T for 5 mins before being labeled with secondary goat IgG polyclonal anti-rabbit Fc-HRP (Cat 31463 ThermoFisher) or goat IgG (H+L) SuperClonal recombinant polyclonal anti-mouse-HRP antibody (Cat A28177 ThermoFisher) at 1:2,000 dilution for 1 hour. Membranes were washed in PBS-T before being developed using SuperSignal West Dura Extended Substrate Kit (Cat 34076 ThermoFisher) and analyzed using the FluorChem M imaging platform (ProteinSimple).

Segura J., Ireland J., Zou Z., Roth G., Buchwald J., Shen T.J., Fischer E., Moir S., Chun T.W, & Sun P.D. (2023). HIV-1 release requires Nef-induced caspase activation. PLOS ONE, 18(2), e0281087.

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Publication 2023

Actins anti-IgG Antibodies, Anti-Idiotypic Buffers Cells Clone Cells Dura Mater G-substrate Gels Gene Products, gag Genetic Heterogeneity Glycine Goat Homo sapiens IgG1 IgG2B Immunoglobulins Immunoprecipitation Mus Nelfinavir Nitrocellulose Proteins quinoline-val-asp(OMe)-CH2-OPH Rabbits SDS-PAGE Stem Cells Sulfoxide, Dimethyl Technique, Dilution Tissue, Membrane Tromethamine Tween 20

Antiretroviral Exposure During Pregnancy

Pregnant women were considered exposed to antiretroviral combination if they started antiretroviral treatment before or during pregnancy, and continued at least until delivery. Antiretroviral combination was defined by at least three drugs: namely two nucleoside reverse transcriptase inhibitors (NRTI) associated with a PI (lopinavir/ritonavir, atazanavir/ritonavir, darunavir/ritonavir, fosamprenavir, saquinavir and nelfinavir) or a NNRTI (efavirenz or nevirapine). We categorised the exposure into three different periods: pre-conception, early pregnancy (first trimester) and late pregnancy (second and third trimester).

Saint-Lary L., Benevent J., Damase-Michel C., Vayssière C., Leroy V, & Sommet A. (2023). Adverse perinatal outcomes associated with prenatal exposure to protease-inhibitor-based versus non-nucleoside reverse transcriptase inhibitor-based antiretroviral combinations in pregnant women with HIV infection: a systematic review and meta-analysis. BMC Pregnancy and Childbirth, 23, 80.

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Publication 2023

atazanavir, ritonavir drug combination Conception Darunavir efavirenz fosamprenavir lopinavir-ritonavir drug combination Nelfinavir Nevirapine Nucleosides Obstetric Delivery Pharmaceutical Preparations Pregnancy Pregnant Women Reverse Transcriptase Inhibitors Ritonavir Saquinavir

Interpreting HIV-1 Drug Resistance

The sequences were submitted to the Stanford University HIV Resistance Database (http://hivdb.stanford.edu/) to describe and interpret HIV-1 TDR. TDR level was classified according to the Stanford Penalty Score as high (60), intermediate (30–59), or low (15–29) to the following drugs: PI, Protease inhibitor; NRTI, Nucleoside reverse transcriptase inhibitor; NNRTI, Non-nucleoside reverse transcriptase inhibitor; INSTI, Integrase strand transfer inhibitors; NFV: Nelfinavir; ABC: Abacavir; AZT: Zidovudine; D4T: Stavudine; DDI: Didanosine; FTC: Emtricitabine; 3TC, Lamivudine; TDF: Tenofovir; DOR: Doravirine; EFV: Efavirenz; ETR: Etravirine; RPV: Rilpivirine. Drug resistance mutations were analyzed using the CRP tool (http://cpr.stanford.edu/cpr.cgi).

Hong H., Tang C., Liu Y., Jiang H., Fang T, & Xu G. (2023). HIV-1 drug resistance and genetic transmission network among newly diagnosed people living with HIV/AIDS in Ningbo, China between 2018 and 2021. Virology Journal, 20, 233.

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Publication 2023

abacavir Didanosine doravirine efavirenz Emtricitabine etravirine HIV-1 Integrase Inhibitors Lamivudine Mutation Nelfinavir Nucleosides Pharmaceutical Preparations Protease Inhibitors Resistance, Drug Reverse Transcriptase Inhibitors Rilpivirine Stavudine Tenofovir Zidovudine

Multidrug-Resistant HIV-1 Variants Selection

MT-4 cells were grown in RPMI 1640 culture medium, while TZM-b1 cells [The National Institutes of Health (NIH) HIV Reagent Program] and 293T cells were propagated in Dulbecco’s modified Eagle’s medium. These media were supplemented with 10% fetal calf serum (Gemini Bio-Products) plus antibiotic-antimycotic (Anti-Anti; Gibco).
A highly PI/NRTI-resistant HIV-1 variant (HIV_DRV^R_P51, referred as HIV_P51 in the present report) had previously been selected in vitro with DRV using a mixture of eight multidrug-
resistant HIV-1 clinical isolates as a starting viral population (21 (link)). HIV_P51 that includes multiple virus species represents a
quasi-species HIV isolate (table S1). HIV^WT_SQV-5μM,
HIV^WT_IDV-5μM, HIV^WT_NFV-5μM, HIV^WT_RTV-5μM, HIV^WT_APV-5μM, HIV^WT_LPV-5μM, and HIV^WT_ATV-5μM were selected with SQV, indinavir (IDV), nelfinavir (NFV), RTV, amprenavir (APV), and atazanavir
(ATV), respectively, using wild-type HIV-1_NL4-3
(rHIV^WT) (21 (link), 27 (link)). HIV^V32I_DRV-1μM, HIV^I54M_DRV-1μM, and HIV^I84V_DRV-1μM were obtained by selecting with DRV using rHIV^WTs carrying V32I, I54M, or I84V in protease (29 ). HIV^11MIX_TPV-15μM was selected with tipranavir (TPV) using a mixture of 11 multidrug resistant HIV-1 clinical isolates as a starting viral population (28 (link)). Eight recombinant infectious HIV-1 clones (rHIV^{CL1-PR/CL1-RT},
rHIV^{CL1-PR/CL1-RT/CL1-IN}, rHIV^{CL2-PR/CL1-RT}, rHIV^{CL2-PR/CL2-RT/CL2-IN}, rHIV^{CL3-PR/CL3-RT}, rHIV^{CL3-PR/CL3-RT/CL3-IN}, rHIV^{CL7-PR/CL7-RT}, and rHIV^{CL7-PR/CL7-RT/CL7-IN}) were generated by replacing PR-, RT-, and/or IN-encoding genes of HIV-1_NL4-3–based plasmid (pHIV_NL4-3) with corresponding genes of clinical HIV-1 strains isolated from four representative patients (HIV^CL1, HIV^CL2, HIV^CL3, and HIV^CL7), who were highly experienced with multiple classes of antiretroviral agents including INSTI(s) and had developed high multitudes of drug resistance over 10 to 25 years of antiretroviral therapy. Clinical profiles of the four patients and drug resistance–associated amino acid substitutions detected in their clinical isolates are illustrated in table S3. The study (NCT01976715) was approved by the Institutional Review Board of the National Cancer Institute. All participants provided written informed consent.
GRL-142 was designed and synthesized as previously described (20 (link)). Abacavir, lamivudine, efavirenz, SQV, IDV, NFV, RTV, APV, ATV, and DRV were purchased from Sigma-Aldrich. Tenofovir was purchased from BioVision. Doravirine, cabotegravir, bictegravir, TPV, and BI224436 were purchased from MedChemExpress. RAL, elvitegravir, and DTG were purchased from Tronto Research Chemicals. Emtricitabine and RPV were obtained from the NIH AIDS Reagent Program.

Aoki M., Aoki-Ogata H., Bulut H., Hayashi H., Takamune N., Kishimoto N., Tanaka H., Higashi-Kuwata N., Hattori S.I., Das D., Venkateswara Rao K., Iwama K., Davis D.A., Hasegawa K., Murayama K., Yarchoan R., Ghosh A.K., Pau A.K., Machida S., Misumi S, & Mitsuya H. (2023). GRL-142 binds to and impairs HIV-1 integrase nuclear localization signal and potently suppresses highly INSTI-resistant HIV-1 variants. Science Advances, 9(28), eadg2955.

Publication 2023

abacavir Acquired Immunodeficiency Syndrome Amino Acid Substitution amprenavir Anti-Retroviral Agents Antibiotics Atazanavir bictegravir cabotegravir Cells Clone Cells doravirine Eagle efavirenz elvitegravir Emtricitabine Ethics Committees, Research Fetal Bovine Serum Genes HEK293 Cells HIV-1 Indinavir Infection Lamivudine Nelfinavir Patient Representatives Patients Peptide Hydrolases Plasmids Quasispecies Resistance, Drug Strains Tenofovir Therapeutics tipranavir Virus

Top products related to «Nelfinavir»

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Lopinavir by Merck Group

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Bovine serum albumin (bsa) by Merck Group

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1 10 phenanthroline by Merck Group

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Indinavir by Merck Group

Sourced in United States, Germany

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Nelfinavir by Selleck Chemicals

Sourced in Germany, China

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Zidovudine by Merck Group

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Atazanavir by Bristol-Myers Squibb

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Fetal bovine serum (fbs) by Thermo Fisher Scientific

Sourced in United States, China, United Kingdom, Germany, Australia, Japan, Canada, Italy, France, Switzerland, New Zealand, Brazil, Belgium, India, Spain, Israel, Austria, Poland, Ireland, Sweden, Macao, Netherlands, Denmark, Cameroon, Singapore, Portugal, Argentina, Holy See (Vatican City State), Morocco, Uruguay, Mexico, Thailand, Sao Tome and Principe, Hungary, Panama, Hong Kong, Norway, United Arab Emirates, Czechia, Russian Federation, Chile, Moldova, Republic of, Gabon, Palestine, State of, Saudi Arabia, Senegal

Fetal Bovine Serum (FBS) is a cell culture supplement derived from the blood of bovine fetuses. FBS provides a source of proteins, growth factors, and other components that support the growth and maintenance of various cell types in in vitro cell culture applications.

Ritonavir by Merck Group

Sourced in United States, Germany

Ritonavir is a pharmaceutical product developed by Merck Group. It is a protease inhibitor used in the treatment of HIV infection. The core function of Ritonavir is to prevent the human immunodeficiency virus (HIV) from multiplying in the body by inhibiting the activity of the HIV protease enzyme.

What is Nelfinavir and how does it work?

What are some common usage challenges with Nelfinavir?

One key challenge with Nelfinavir is that it can have significant drug-drug interactions, particularly with certain cholesterol-lowering medications and antifungal drugs. Patients and clinicians need to be vigilant about monitoring for potential interactions and adjusting dosages accordingly. Additionally, Nelfinavir can sometimes cause gastrointestinal side effects like diarrhea, which may impact adherence and effectiveness.

Are there different variations or types of Nelfinavir?

While there is primarily one formulation of Nelfinavir, there can be some variations in how it is administered. For example, Nelfinavir is typically taken as a oral powder or tablet, but there are also liquid formulations available for patients who have difficulty swallowing pills. The specific dosage and frequency can also vary based on the individual patient's needs and the other antiretroviral medications they are taking.

In what specific applications is Nelfinavir used?

Nelfinavir is primarily used as part of antiretroviral therapy (ART) regimens for the treatment of HIV infection. It is often combined with other protease inhibitors or nucleoside reverse transcriptase inhibitors (NRTIs) to provide a more potent and durable suppression of viral replication. Nelfinavir may also be used off-label for certain other viral infections, but its primary clinical use is in the management of HIV disease.

How can PubCompare.ai assist with optimizing Nelfinavir research and use?

PubCompare.ai can help optimize Nelfinavir research and use in several ways. First, it allows researchers to more efficiently screen the literature on Nelfinavir protocols, studies, and products. The platform's AI-driven analysis can also pinpoint critical insights, helping researchers identify the most effective Nelfinavir protocols for their specific research goals. By highlighting key differences in protocol effectiveness, PubCompare.ai enables users to choose the best options to maximize reproducibility and accuracy in their Nelfinavir studies. Tis can ultimately lead to more effective therapies for those living with HIV.

More about "Nelfinavir"

Nelfinavir, a crucial HIV protease inhibitor, has been widely used in combination with other antiretroviral agents to effectively suppress viral replication and improve clinical outcomes for individuals living with HIV/AIDS.
This potent medication works by binding to the HIV protease enzyme, inhibiting its activity and preventing the maturation of new viral particles.
To optimize Nelfinavir research and development, scientists can leverage the power of PubCompare.ai, an innovative tool that helps users locate and analyze relevant literature, preprints, and patents.
This AI-driven platform enables researchers to identify the best protocols and products, enhancing reproducibility and accuracy in Nelfinavir studies.
This, in turn, can lead to the development of more effective therapies for those battling the HIV virus.
Beyond Nelfinavir, other key antiretroviral agents like Lopinavir, Indinavir, Atazanavir, and Ritonavir have also been extensively studied and utilized in the treatment of HIV.
Additionally, compounds such as Bovine serum albumin (BSA) and 1,10-phenanthroline have been explored for their potential roles in HIV research and drug development.
The combination of these various components, along with the optimization techniques facilitated by PubCompare.ai, can contribute to a more comprehensive understanding of Nelfinavit and its application in the fight against HIV/AIDS.