Development of HIV-1 protease inhibitors
Molecular Docking Studies; Dietary Compounds As HIV 1 Protease Inhibitors
... Originally, structure-based drug design was equated with De novo design or building a molecule from ground up [16]. The active site of the protein was a space to be filled with a molecule that complemented in terms of ...
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Benzoyl isothiocyanates derived ligands as potential HIV-1 protease inhibitors and their reactions with gold ions
... multiclade HIV epidemics impacts viral diagnosis and pathogenicity and treatment which poses daunting challenges for effective vaccine ...virus 1 (HIV-1) synthesizes its genomic DNA in the ...
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QSAR MODELING FOR INHIBITORY ACTIVITY OF NON PEPTIDE HIV 1 PROTEASE INHIBITORS: A MLR APPROACH
... www.wjpr.net Vol 3, Issue 9, 2014. 1307 From table 3 the correlation matrix between the descriptors and antiviral activity was obtained. The correlation coefficient between the pIC 50 and X 3 V (r = 0.76) was significant ...
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Exploring QSARs for Inhibitory Activity of Non-peptide HIV-1 Protease Inhibitors by GA-PLS and GA-SVM
... selected descriptors, which are TE2, Ui, GATS5e, Mor13e, ATS7m, Ss, Mor27e, and RDF035e were found to be important factors con- trolling the inhibitory activity. Comparison between PLS and SVM methods demonstrates that ...
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Design and synthesis of inhibitors for the HIV 1 protease
... moderate inhibitors (pM) of the HIV-1 ...hydroxyethylamine inhibitors were not followed by the phosphonamidate methyl ...hydroxyl-containing inhibitors Is more easily achieved as these ...
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Protease mediated maturation of HIV: Inhibitors of protease and the maturation process
... clinical development of BVM necessitates the need for a second-generation maturation inhibitor to over- come the problem of intrinsic drug resistance encountered by ...maturation inhibitors has highlighted ...
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HIV protease inhibitors: a review of molecular selectivity and toxicity
... of HIV protease inhibitors might be a pos- sible solution to eliminate drug side ...of HIV protease inhibitors pos- sessing novel chemical structures and alternative binding ...
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Safety of protease inhibitors in HIV-infected pregnant women
... of protease inhibitors across the placenta is known to be minimal, and current data about birth defects and fetal malignan- cies are ...with protease inhibitor-based regimens, but concerns about the ...
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HIV 1 protease inhibitor mutations affect the development of HIV 1 resistance to the maturation inhibitor bevirimat
... Maturation inhibitors are an experimental class of anti- retrovirals that prevent HIV-1 replication by targeting the structural proteins essential for particle maturation and thus formation of ...
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A combined 3D-QSAR and docking studies for the In-silicoprediction of HIV-protease inhibitors
... of HIV, drug resistance and their side effects are the big- gest challenge to develop an effective anti-AIDS ...therapy. HIV-1 Protease is emerging as one of the major druggable target for the ...
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Gender-specific effects of HIV protease inhibitors on body mass in mice
... In the present study, ritonavir suppressed serum leptin levels, and increased food intake in both male and female mice. This increase in food intake did not translate to increased abdominal fat deposition or weight gain. ...
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Predictive factors of virological success to salvage regimens containing protease inhibitors in HIV 1 infected children
... more protease resistance mutations as well as the use of boosting-PI combinations has been associated with significant virological response in adults who initiated rescue intervention based on boosting-PI ...the ...
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Selection of Drug-Resistant Feline Immunodeficiency Virus (FIV) Encoding FIV/HIV Chimeric Protease in the Presence of HIV-Specific Protease Inhibitors
... against HIV-1 ...geting HIV-1 PR in infected patients, and multidrug therapy com- bining them with drugs against other targets, primarily RT, has greatly improved the quality of life of ...
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Structure Function Studies Of Hiv-1 Protease
... 6.1 HIV-1 Drug resistance remains a major problem for HIV-1 treatment, although many strides have been made in the last ...multiple inhibitors have very poor prognoses, and the ...
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Non-Cleavage Site Gag Mutations in Amprenavir-Resistant Human Immunodeficiency Virus Type 1 (HIV-1) Predispose HIV-1 to Rapid Acquisition of Amprenavir Resistance but Delay Development of Resistance to Other Protease Inhibitors
... Statistical analysis of selection profiles of infectious HIV-1 clones. The selec- tion profiles of various infectious HIV-1 clones were compared as follows. The logarithms of the ...
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An in-silico investigation of Morita-Baylis-Hillman accessible heterocyclic analogues for applications as novel HIV-1 C protease inhibitors
... subtype HIV-1 viral strains, they display subtle differences in the drug responses and development of resistance in their proteases (Ahmed et ...the development and incorporation of novel ...
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The Genetic Basis of HIV-1 Resistance to Reverse Transcriptase and Protease Inhibitors
... and protease enzymes, the molecular targets of antiretroviral ...that HIV-1 RT and protease susceptibility testing be used to help select antiretroviral drugs for HIV-1-infected ...
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QSAR Study and Determination of More Potent Peptidic HIV-1- Protease Inhibitors
... Department of Chemistry, Shia P.G. College, Lucknow, U.P., INDIA Abstract QSAR study of three sets of peptidic HIV-protease inhibitors has been studied. The descriptor used for study is log P. For ...
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The L76V mutation in HIV-1 protease is potentially associated with hypersusceptibility to protease inhibitors Atazanavir and Saquinavir: is there a clinical advantage?
... Wiesmann 1* , Jan Vachta 1 , Robert Ehret 1 , Hauke Walter 2 , Rolf Kaiser 3 , Martin Stürmer 4 , André Tappe 5 , Martin Däumer 6 , Thomas Berg 7 , Gudrun Naeth 1 , Patrick Braun 1 , ...
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Studies directed towards the synthesis of chromone carbaldehyde-derived HIV-1 protease inhibitors
... Schematic representation of hydrogen-bonding interactions between compound 263 (conformer 1) and the HIV -1 protease receptor cavity in the presence of a s tructural water molecul[r] ...
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