Cargando…

A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants

BACKGROUND: The recently approved anti-AIDS drug rilpivirine (TMC278, Edurant) is a nonnucleoside inhibitor (NNRTI) that binds to reverse transcriptase (RT) and allosterically blocks the chemical step of DNA synthesis. In contrast to earlier NNRTIs, rilpivirine retains potency against well-character...

Descripción completa

Detalles Bibliográficos
Autores principales:	Johnson, Barry C, Pauly, Gary T, Rai, Ganesha, Patel, Disha, Bauman, Joseph D, Baker, Heather L, Das, Kalyan, Schneider, Joel P, Maloney, David J, Arnold, Eddy, Thomas, Craig J, Hughes, Stephen H
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	BioMed Central 2012
Materias:	Research
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3549755/ https://www.ncbi.nlm.nih.gov/pubmed/23217210 http://dx.doi.org/10.1186/1742-4690-9-99

Ejemplares similares

Rilpivirine analogs potently inhibit drug-resistant HIV-1 mutants
por: Smith, Steven J., et al.
Publicado: (2016)

Snapshot of the equilibrium dynamics of a drug bound to HIV-1 reverse transcriptase
por: Kuroda, Daniel G., et al.
Publicado: (2013)

HIV-1 reverse transcriptase complex with DNA and nevirapine reveals nonnucleoside inhibition mechanism
por: Das, Kalyan, et al.
Publicado: (2012)

Effect of intrinsic and extrinsic factors on the pharmacokinetics of TMC278 in antiretroviral-naïve, HIV-1-infected patients in ECHO and THRIVE
por: Crauwels, HM, et al.
Publicado: (2010)

Cryo-EM structures of wild-type and E138K/M184I mutant HIV-1 RT/DNA complexed with inhibitors doravirine and rilpivirine
por: Singh, Abhimanyu K., et al.
Publicado: (2022)

Efficacy and safety of TMC278 in treatment-naïve, HIV-1-infected patients with HBV/HCV co-infection enrolled in the phase III ECHO and THRIVE trials
por: Nelson, M, et al.
Publicado: (2010)

Crystal engineering of HIV-1 reverse transcriptase for structure-based drug design
por: Bauman, Joseph D., et al.
Publicado: (2008)

Crystal Structure of a Retroviral Polyprotein: Prototype Foamy Virus Protease-Reverse Transcriptase (PR-RT)
por: Harrison, Jerry Joe E. K., et al.
Publicado: (2021)

Pooled week 48 safety and efficacy results from the ECHO and THRIVE phase III trials comparing TMC278 vs EFV in treatment-naïve, HIV-1-infected patients
por: Cohen, C, et al.
Publicado: (2010)

PSUN278 Factitious hypoglycemia, diagnostic delay due to insulin assay failure to detect insulin analogues.
por: Harned, Leighton Kahle, et al.
Publicado: (2022)

Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus
por: Wei, Lei, et al.
Publicado: (2017)

Phenyl Substituted 4-Hydroxypyridazin-3(2H)-ones and 5-Hydroxypyrimidin-4(3H)-ones: Inhibitors of Influenza A Endonuclease
por: Sagong, Hye Yeon, et al.
Publicado: (2014)

Safety of rilpivirine plus nucleoside reverse-transcriptase inhibitors in HIV-infected Taiwanese with a higher prevalence of hepatitis virus infection
por: Wu, Pei-Ying, et al.
Publicado: (2014)

Biochemical mechanism of clinical resistance to rilpivirine
por: Singh, Kamalendra, et al.
Publicado: (2012)

CIB2 interacts with TMC1 and TMC2 and is essential for mechanotransduction in auditory hair cells
por: Giese, Arnaud P. J., et al.
Publicado: (2017)

Integrative structural biology studies of HIV-1 reverse transcriptase binding to a high-affinity DNA aptamer
por: Tuske, Steve, et al.
Publicado: (2020)

TMC and EVER genes belong to a larger novel family, the TMC gene family encoding transmembrane proteins
por: Keresztes, Gabor, et al.
Publicado: (2003)

GABA signaling triggered by TMC-1/Tmc delays neuronal aging by inhibiting the PKC pathway in C. elegans
por: Wu, Jieyu, et al.
Publicado: (2022)

The role of rilpivirine in Southern Africa
por: Moorhouse, Michelle A., et al.
Publicado: (2019)

Impact of rilpivirine cross-resistance on long-acting cabotegravir-rilpivirine in low and middle-income countries
por: Steegen, Kim, et al.
Publicado: (2023)

Health Tract, No. 278: Health Hodge Podge
Publicado: (1867)

Transgenic Tmc2 expression preserves inner ear hair cells and vestibular function in mice lacking Tmc1
por: Asai, Yukako, et al.
Publicado: (2018)

Identification and Splicing Characterization of Novel TMC6 and TMC8 Variants Associated With Epidermodysplasia Verruciformis in Three Chinese Families
por: Wang, Rongrong, et al.
Publicado: (2021)

Conference on Drivers for Inertial Confinement Fusion : TMC
por: Collective
Publicado: (1992)

TMC threshold as function of beam-beam interaction
por: Cornelis, K
Publicado: (1993)

Is TMC1 the Hair Cell Mechanotransducer Channel?
por: Fettiplace, Robert
Publicado: (2016)

Ankyrin Is An Intracellular Tether for TMC Mechanotransduction Channels
por: Tang, Yi-Quan, et al.
Publicado: (2020)

Ankyrin Is An Intracellular Tether for TMC Mechanotransduction Channels
por: Tang, Yi-Quan, et al.
Publicado: (2020)

Mitochondrial toxicities of nucleoside analogue reverse transcriptase inhibitors in AIDS cases
por: Marfatia, Yogesh S., et al.
Publicado: (2014)

PLGA, PLGA-TMC and TMC-TPP Nanoparticles Differentially Modulate the Outcome of Nasal Vaccination by Inducing Tolerance or Enhancing Humoral Immunity
por: Keijzer, Chantal, et al.
Publicado: (2011)

Zebrafish-Based Discovery of Antiseizure Compounds from the North Sea: Isoquinoline Alkaloids TMC-120A and TMC-120B
por: Copmans, Daniëlle, et al.
Publicado: (2019)

The development of an effective synthetic route of rilpivirine
por: Zhang, Tao, et al.
Publicado: (2021)

Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV
por: Himmel, Daniel M., et al.
Publicado: (2020)

Single and Dual Vector Gene Therapy with AAV9-PHP.B Rescues Hearing in Tmc1 Mutant Mice
por: Wu, Jason, et al.
Publicado: (2021)

Room-Temperature, Copper-Free Sonogashira Reactions Facilitated by Air-Stable, Monoligated Precatalyst [DTBNpP] Pd(crotyl)Cl
por: Pohida, Katherine, et al.
Publicado: (2018)

Drug Resistance in Non-B Subtype HIV-1: Impact of HIV-1 Reverse Transcriptase Inhibitors
por: Singh, Kamalendra, et al.
Publicado: (2014)

Calculation of TMC threshold in the presence of beam-beam force
por: Li, G, et al.
Publicado: (1994)

Structures of the TMC-1 complex illuminate mechanosensory transduction
por: Jeong, Hanbin, et al.
Publicado: (2022)

Functional consequences of Genetics variant in TMC1 and TMC2 within a United Arab Emirates family with Pre-lingual hearing loss
por: Al Mutery, Abdullah, et al.
Publicado: (2023)

Dolutegravir/rilpivirine for the treatment of HIV-1 infection
por: Dowers, Ellen, et al.
Publicado: (2018)

Cannot write session to /tmp/vufind_sessions/sess_pu0l9q20o6ecf66876isi73c6c