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Down-regulation of mitochondrial thymidine kinase 2 and deoxyguanosine kinase by didanosine: implication for mitochondrial toxicities of anti-HIV nucleoside analogs.
Sun R, Eriksson S, and Wang L
Biochemical and Biophysical Research Communications, 450(2), 1021-1026 (2014)
Pär Matsson et al.
Journal of medicinal chemistry, 48(2), 604-613 (2005-01-22)
The influence of different drug transport routes in intestinal drug permeability screening assays was studied. Three experimental models were compared: the small-intestine-like 2/4/A1 cell model, which has a leaky paracellular pathway, the Caco-2 cell model, which has a tighter paracellular
Muriel Lalanne et al.
Bioorganic & medicinal chemistry letters, 17(8), 2237-2240 (2007-02-06)
Novel glycerolipidic prodrugs of didanosine and didanosine monophosphate designed to by-pass the hepatic first pass metabolism were synthesized and tested for their cytotoxicity and anti-HIV-1 activity. Formulation as liposomes of dipalmitoylphosphatidylcholine was elaborated. A simple quantitative HPLC-UV method was developed
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential
J Darbyshire et al.
The Cochrane database of systematic reviews, (2)(2), CD002038-CD002038 (2000-05-05)
Zidovudine (AZT) monotherapy was the first antiretroviral drug to be tested widely. The next two drugs to be developed were didanosine (ddI) and zalcitabine (ddC). To assess the effects of zidovudine (AZT), zidovudine plus didanosine (ddI) and zidovudine plus zalcitabine
D Bradshaw et al.
Antimicrobial agents and chemotherapy, 51(12), 4489-4491 (2007-09-19)
We describe an unusual pathway of human immunodeficiency virus type 1 reverse transcriptase resistance during therapy with tenofovir-emtricitabine, characterized initially by the mutations K70E and M184V and later by K70G and M184V, with the two mutations coexisting on the same
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
Alberto Diez-Torrubia et al.
ChemMedChem, 7(4), 618-628 (2012-02-07)
We previously described a novel prodrug approach in which a di- or tetrapeptide moiety is linked to a wide variety of amine-containing drugs through an amide bond, which is specifically cleaved by dipeptidyl peptidase IV (DPPIV/CD26) activity. Herein we report
E Randall Lanier et al.
Antimicrobial agents and chemotherapy, 54(7), 2901-2909 (2010-05-05)
CMX157 is a lipid (1-0-hexadecyloxypropyl) conjugate of the acyclic nucleotide analog tenofovir (TFV) with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. CMX157 was consistently >300-fold more active than tenofovir against multiple viruses in
Gurudutta Pattnaik et al.
Journal of microencapsulation, 29(7), 666-676 (2012-05-02)
Human immunodeficiency viruses (HIV) hide themselves in macrophages at the early stage of infection. Delivering drug in a sustained manner from polymeric nanoparticles in those cells could control the disease effectively. The study was intended to develop poly(d,l-lactic-co-glycolic acid)-based nanoparticles
Jan Balzarini et al.
European journal of medicinal chemistry, 44(1), 303-311 (2008-04-19)
A series of novel thiazolidin-4-ones bearing a lipophilic adamantyl substituent at position 2 or 3 were synthesized. A majority of them showed a modest anti-HIV-1 activity, whereas 2-adamantan-1-yl-3-(4,6-dimethylpyrimidin-2-yl)-thiazolidin-4-one (8) was endowed with a remarkable antiviral potency (EC(50)=0.67 microM). The new
R Nahid Samiei et al.
European review for medical and pharmacological sciences, 24(3), 1454-1459 (2020-02-26)
The current study was designed to investigate the effects of some nucleoside reverse transcriptase inhibitors (NRTIs) on HSV-1 infection. Initially, the SwissTargetPrediction server was used to predict the interactions between HSV-1 thymidine kinase and acyclovir, stavudine, zidovudine, didanosine, and entecavir.
Rosario Palacios et al.
Expert review of anti-infective therapy, 4(6), 965-971 (2006-12-22)
There are currently several suitable and different antiretroviral regimens to start highly active antiretroviral therapy (HAART), and many clinicians and patients prefer once-daily therapy. The efficacy and potency of efavirenz (EFV) has been established in many clinical trials and cohort
Marco Bongiovanni et al.
Current medicinal chemistry, 13(23), 2789-2793 (2006-11-01)
Nucleoside reverse transcriptase inhibitors (NRTI) are essential components of highly active antiretroviral treatment (HAART). Although several combinations can be used as NRTI backbones, not all are associated with good virological and/or immunological results. In particular, some NRTI combinations should be
Ramiro Javier Romo González et al.
Acta gastroenterologica Latinoamericana, 41(4), 320-323 (2012-02-02)
Nodular regenerative hyperplasia of the liver is a rare condition. We describe here the case of a patient with HIV who presented with a clinical syndrome of portal hypertension. After multiple evaluations the diagnosis was recognized by the histology. The
Nicolas Sluis-Cremer et al.
Antimicrobial agents and chemotherapy, 53(9), 3715-3719 (2009-07-15)
Although the approved nucleoside reverse transcriptase (RT) inhibitors (NRTI) are integral components of therapy for human immunodeficiency virus type 1 (HIV-1) infection, they can have significant limitations, including the selection of NRTI-resistant HIV-1 and cellular toxicity. Accordingly, there is a
William R Birmingham et al.
Nature chemical biology, 10(5), 392-399 (2014-03-25)
Concatenation of engineered biocatalysts into multistep pathways markedly increases their utility, but the development of generalizable assembly methods remains a major challenge. Herein we evaluate 'bioretrosynthesis', which is an application of the retrograde evolution hypothesis, for biosynthetic pathway construction. To
Fanconi syndrome and nephrogenic diabetes insipidus associated with didanosine therapy in HIV infection: a case report and literature review.
Géraldine D'Ythurbide et al.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association, 22(12), 3656-3659 (2007-10-02)
Richard M Hoglund et al.
British journal of clinical pharmacology, 79(4), 636-649 (2014-10-10)
Drug-drug interactions between antimalarial and antiretroviral drugs may influence antimalarial treatment outcomes. The aim of this study was to investigate the potential drug-drug interactions between the antimalarial drugs, lumefantrine, artemether and their respective metabolites desbutyl-lumefantrine and dihydroartemisinin, and the HIV
Tenofovir and didanosine: a dangerous liaison.
Laura Waters et al.
The AIDS reader, 15(8), 403-406 (2005-08-23)
J J McGowan et al.
Reviews of infectious diseases, 12 Suppl 5, S513-S520 (1990-07-01)
AIDS has remained a significant and worsening medical problem since its first description as a new clinical entity in 1981. In the past 6 years, substantial progress has been made in the chemotherapy for this disease; such progress is likely
N N Guimarães et al.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 53, 299-309 (2012-12-25)
Nucleoside reverse-transcriptase inhibitor (NRTI) drugs are a major component of highly-active antiretroviral therapy (HAART). NRTI combinations have been demonstrated as producing a sustained reduction in plasma viremia with an increased CD4 count, thereby showing clear clinical benefits. Therefore, the secondary
Jan Balzarini et al.
European journal of medicinal chemistry, 42(7), 993-1003 (2007-02-27)
A series of novel thiazolidin-4-ones bearing a lipophilic adamantyl substituent at position 2, and versatile substituents on the nitrogen atom of the thiazolidine ring, were synthesized whereas several compounds exhibited a modest anti-HIV-1 activity, (+/-)-2-adamantan-1-yl-3-(4,6-dimethyl-pyridin-2-yl)-thiazolidin-4-one 22 was endowed with a
Yuan-Zhen Xiong et al.
European journal of medicinal chemistry, 43(6), 1230-1236 (2007-09-18)
A series of novel 6-naphthyloxy substituted DATA analogues bearing different substituents on the C-6 position of triazine ring were synthesized and evaluated for their in vitro anti-HIV activity in MT-4 cells. The results demonstrated that most of the compounds in
Vici Varghese et al.
Antimicrobial agents and chemotherapy, 53(5), 2196-2198 (2009-02-19)
Q145M, a mutation in a conserved human immunodeficiency virus type 1 reverse transcriptase (RT) region, was reported to decrease susceptibility to multiple RT inhibitors. We report that Q145M and other Q145 mutations do not emerge with RT inhibitors nor decrease
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
Manthena V S Varma et al.
Journal of medicinal chemistry, 52(15), 4844-4852 (2009-05-19)
Kidney plays an important role in the elimination of drugs, especially with low or negligible hepatic clearance. An analysis of the interrelation of physicochemical properties and the human renal clearance for a data set of 391 drugs or compounds tested
Larry J Jolivette et al.
Journal of pharmaceutical sciences, 94(7), 1467-1483 (2005-05-28)
Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data. Recent data suggest that extrapolation of monkey pharmacokinetic data tends to be the most accurate method for predicting human clearance. In this study, the
Tracey Seier et al.
Proceedings of the National Academy of Sciences of the United States of America, 109(16), 6171-6174 (2012-04-05)
The accumulation of mutations causes cell lethality and can lead to carcinogenesis. An important class of mutations, which are associated with mutational hotspots in many organisms, are those that arise by nascent strand misalignment and template-switching at the site of
R B Pollard
AIDS (London, England), 14(16), 2421-2428 (2000-01-11)
Factors affecting patient adherence to therapy, such as frequent daily dosing and complex dosing schedules, are widely understood to be key obstacles to the durability of effective anti-HIV therapy. Didanosine, a nucleoside analogue reverse transcriptase inhibitor (NRTI) that is a
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