A novel prodrug approach has been evaluated using the anti-HIV-active TSAO molecule as the prototype drug to prove the kinetics with purified enzyme and the principles of conversion to the parent compound in sera and cell culture. When a variety of tetrapeptidyl amide prodrugs of NAP-TSAO were synthesized and exposed to purified dipeptidyl-peptidase IV (DPPIV/CD26) as well as human and bovine sera, they are converted to the parent NAP-TSAO drug in two successive steps by both purified CD26 and human and bovine serum. The efficiency of conversion strongly depends on the nature of the amino acid that has to be cleaved-off from the prodrug molecule. The tetrapeptidyl prodrug 20 showed a more than 10-fold improved water-solubility in comparison to that of the parent compound NAP-TSAO. The antiviral activity of the prototype NAP-TSAO could also be modulated by introducing different tetrapeptide moieties on the molecule resulting, in some cases, in a superior antiviral potential in cell culture than the parent drug.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.antiviral.2007.06.009 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Responsible Use of Population Neuroscience Data in the ABCD: Towards Standards of Accountability and Integrity.
Eur J Neurosci
January 2025
Department of Psychiatry and Biobehavioral Sciences, University of California, Los Angeles, California, USA.
This editorial focuses on the issue of data misuse that is increasingly evidenced in social media as well as some premiere scientific journals. This issue is of critical importance to open science projects in general, and ABCD in particular, given the broad array of biological, behavioural and environmental information collected on this American sample of 12,000 youth and parents. ABCD data are already widely used with over 1,200 publications and twice as many citations per year as expected (relative citation index based on year, field and journal).
View Article and Find Full Text PDFHospital attendance, malaria prevalence and self-medication with an antimalarial drug before and after the start of COVID-19 pandemic in a sentinel site for malaria surveillance in Gabon.
Malar J
January 2025
Department of Parasitology-Mycology and Tropical Medicine, Université Des Sciences de La Santé de Libreville, BP 4009, Libreville, Gabon.
Background: The negative impact of COVID-19 pandemic on healthcare service utilization has been reported in several countries. In Gabon, data on the preparedness for future pandemic are lacking. The aim of the present study was to assess the trends of hospital attendance, malaria and self-medication prevalences as well as ITN use before and during Covid-19 first epidemic waves in a paediatric wards of a sentinel site for malaria surveillance, in Libreville, Gabon.
View Article and Find Full Text PDFNutrient-Nutrient Interactions Among Broccoli Glucosinolates and Their Implications for Breeding Cruciferous Crops to Enhance Human Health.
Nutrients
January 2025
Plants for Human Health Institute, North Carolina State University, 600 Laureate Way, Kannapolis, NC 28081, USA.
Unlabelled: While a balanced diet can fulfill most nutritional needs, optimizing the composition of specific foods like broccoli can amplify their health benefits.
Background/objectives: Broccoli ( L. Italica group) is a widely consumed cruciferous vegetable valued for its gastrointestinal and immune health benefits.
p97 Inhibitors Possessing Antiviral Activity Against SARS-CoV-2 and Low Cytotoxicity.
Pharmaceuticals (Basel)
January 2025
Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
p97 (also known as valosin-containing protein, VCP) is a member of the AAA+ ATPase family and is intimately associated with protein quality control and homeostasis regulation. Therefore, pharmaceutical inhibition of p97 has been actively pursued as an anticancer strategy. Recently, p97 has emerged as an important pro-viral host factor and p97 inhibitors are being evaluated as potential antiviral agents.
View Article and Find Full Text PDFIdentification of a New Pentafluorosulfanyl-Substituted Chalcone with Activity Against Hepatoma and Human Parasites.
Pharmaceuticals (Basel)
January 2025
Institute of Physiology, Charité-Universitätsmedizin Berlin, Corporate Member of the Freie Universität Berlin, Humboldt-Universität zu Berlin and Berlin Institute of Health, Charitéplatz 1, 10117 Berlin, Germany.
Background/objectives: New drugs are required for the treatment of liver cancers and protozoal parasite infections. Analogs of the known anticancer active and antileishmanial 2',4',6'-trimethoxychalcone SU086 were prepared and investigated.
Methods: The chalcones were prepared according to the Claisen-Schmidt condensation protocol and analyzed.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!