Results 71 to 80 of about 399,014 (392)

Comparative Molecular Field Analysis (CoMFA) for Thiotetrazole Alkynylacetanilides, a Non-Nucleoside Inhibitor of HIV-1 Double Mutant K103N/Y181C Reverse Transcriptase

E-Journal of Chemistry, 2009
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are allosteric inhibitors of the HIV-1 reverse transcriptase. HIV-1 resistance to nucleoside RT inhibitors such as AZT can arise through mutations in the coding region of RT.
Sivan Sree Kanth, Kotla Sai Abhishake, Manga Vijjulatha   +2 more
doaj   +1 more source

Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase

Journal of Enzyme Inhibition and Medicinal Chemistry, 2016
A series of 3-3-{2-[2-3-methyl-4-phenyl-2,3-dihydro-1,3-thiazol-2-ylidene]hydrazin-1-ylidene-2,3-dihydro-1H-indol-2-one derivatives has been designed and synthesized to study their activity on both HIV-1 (Human Immunodeficiency Virus type 1) RT (Reverse ...
R. Meleddu, S. Distinto, A. Corona, E. Tramontano, Giulia Bianco, C. Melis, F. Cottiglia, E. Maccioni   +7 more
semanticscholar   +1 more source

Evolutionary interplay between viruses and R‐loops

FEBS Letters, EarlyView.
Viruses interact with specialized nucleic acid structures called R‐loops to influence host transcription, epigenetic states, latency, and immune evasion. This Perspective examines the roles of R‐loops in viral replication, integration, and silencing, and how viruses co‐opt or avoid these structures.
Zsolt Karányi, Zita Képes, Zoltán Szabó, Eszter Csoma, Lóránt Székvölgyi   +4 more
wiley   +1 more source

Allosteric HIV-1 integrase inhibitors lead to premature degradation of the viral RNA genome and integrase in target cells [PDF]

, 2017
Recent evidence indicates that inhibition of HIV-1 integrase (IN) binding to the viral RNA genome by allosteric integrase inhibitors (ALLINIs) or through mutations within IN yields aberrant particles in which the viral ribonucleoprotein complexes (vRNPs)
Elliott, Jennifer, Errando, Manel, Koneru, Pratibha C, Kutluay, Sebla B, Kvaratskhelia, Mamuka, Lawson, Dana Q, Madison, Michaela K, Ozanturk, Ayse Naz, Townsend, Dana   +8 more
core   +2 more sources

Inhibition of acyl‐CoA synthetase long‐chain isozymes decreases multiple myeloma cell proliferation and causes mitochondrial dysfunction

Molecular Oncology, EarlyView.
Triacsin C inhibition of the acyl‐CoA synthetase long chain (ACSL) family decreases multiple myeloma cell survival, proliferation, mitochondrial respiration, and membrane potential. Made with Biorender.com. Multiple myeloma (MM) is an incurable cancer of plasma cells with a 5‐year survival rate of 59%.
Connor S. Murphy, Heather Fairfield, Victoria E. DeMambro, Samaa Fadel, Carlos A. Gartner, Michelle Karam, Christian Potts, Princess Rodriguez, Ya‐Wei Qiang, Habib Hamidi, Xiangnan Guan, Calvin P. H. Vary, Michaela R. Reagan   +12 more
wiley   +1 more source

MET variants with activating N‐lobe mutations identified in hereditary papillary renal cell carcinomas still require ligand stimulation

Molecular Oncology, EarlyView.
MET variants in the N‐lobe of the kinase domain, found in hereditary papillary renal cell carcinoma, require ligand stimulation to promote cell transformation, in contrast to other RTK variants. This suggests that HGF expression in the microenvironment is important for tumor growth in such patients. Their sensitivity to MET inhibitors opens the way for
Célia Guérin, Audrey Vinchent, Marie Fernandes, Isabelle Damour, Agathe Laratte, Rémi Tellier, Gabriella O. Estevam, Jean‐Pascal Meneboo, Céline Villenet, Clotilde Descarpentries, James S. Fraser, Martin Figeac, Alexis B. Cortot, Etienne Rouleau, David Tulasne   +14 more
wiley   +1 more source

Biochemical characterization of a multi-drug resistant HIV-1 subtype AG reverse transcriptase: antagonism of AZT discrimination and excision pathways and sensitivity to RNase H inhibitors [PDF]

, 2016
We analyzed a multi-drug resistant (MR) HIV-1 re- verse transcriptase (RT), subcloned from a patient- derived subtype CRF02 AG, harboring 45 amino acid exchanges, amongst them four thymidine analog mutations (TAMs) relevant for high-level AZT (azi-
Bodem, Jochen, Buchholz, Bernd, Corona, Angela, Di Santo, Roberto, Jordan, Mareike, Maccioni, Elias, Schneider, Anna, Spã¶ring, Imke, Tramontano, Enzo, Wã¶hrl, Birgitta M.   +9 more
core   +1 more source

Targeting the MDM2‐MDM4 interaction interface reveals an otherwise therapeutically active wild‐type p53 in colorectal cancer

Molecular Oncology, EarlyView.
This study investigates an alternative approach to reactivating the oncosuppressor p53 in cancer. A short peptide targeting the association of the two p53 inhibitors, MDM2 and MDM4, induces an otherwise therapeutically active p53 with unique features that promote cell death and potentially reduce toxicity towards proliferating nontumor cells.
Sonia Valentini, Giada Mele, Marika Attili, Maria Rita Assenza, Fulvio Saccoccia, Francesca Sardina, Cinzia Rinaldo, Roberto Massari, Nicola Tirelli, Alfredo Pontecorvi, Fabiola Moretti   +10 more
wiley   +1 more source

The role of drug resistance in poor viral suppression in rural South Africa: findings from a population-based study. [PDF]

, 2020
BACKGROUND:Understanding factors driving virological failure, including the contribution of HIV drug resistance mutations (DRM), is critical to ensuring HIV treatment remains effective.
Barnhart, Scott, Gilmore, Hailey J, Grignon, Jessica S, Hunt, Gillian, Liegler, Teri, Lippman, Sheri A, Mooney, Alyssa C, Prach, Lisa M, Puren, Adrian, Truong, Hong-Ha M   +9 more
core  

Weight gain among treatment-naïve persons with HIV starting integrase inhibitors compared to non-nucleoside reverse transcriptase inhibitors or protease inhibitors in a large observational cohort in the United States and Canada. [PDF]

, 2020
IntroductionWeight gain following antiretroviral therapy (ART) initiation is common, potentially predisposing some persons with HIV (PWH) to cardio-metabolic disease.
Altoff, Keri N, Bourgi, Kassem, Crane, Heidi, Gange, Stephen J, Gill, John, Horberg, Michael A, Jenkins, Cathy A, Kirk, Gregory, Koethe, John R, Lake, Jordan, Li, Jun, Lima, Viviane D, Margolick, Joseph, Mathews, William C, Moore, Richard D, North American AIDS Cohort Collaboration on Research and Design (NA-ACCORD), Palella, Frank, Rabkin, Charles S, Rebeiro, Peter F, Silverberg, Michael, Sterling, Timothy R, Thorne, Jennifer, Willig, Amanda, Wong, Cherise   +23 more
core   +1 more source