Affiliation: University of Cagliari
- The use of a new in vitro reaction substrate reproducing both U3 and U5 regions of the HIV-1 3'-ends increases the correlation between the in vitro and in vivo effects of the HIV-1 integrase inhibitorsEnzo Tramontano
Department of Sciences and Biomedical Technologies, University of Cagliari, Cittadella Universitaria SS554, 09142 Monserrato, Cagliari, Italy
Biochem Pharmacol 67:1751-61. 2004....
- HIV-1 RNase H: recent progress in an exciting, yet little explored, drug targetEnzo Tramontano
Department of Sciences and Biomedical Technologies, University of Cagliari, Cittadella di Monserrato, 09142 Monserrato Cagliari, Italy
Mini Rev Med Chem 6:727-37. 2006..All drugs shown to inhibit HIV-1 RNase H are reported, including the recently described classes of compounds that interact with the metal ions in the active site...
- HIV-1 Reverse Transcriptase Still Remains a New Drug Target: Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of ActionsFrancesca Esposito
Department of Life and Environmental Sciences, University of Cagliari, Cittadella Universitaria di Monserrato, SS 554, 09042 Monserrato, Italy
Mol Biol Int 2012:586401. 2012..This paper describes the HIV-1 RT function and molecular structure, illustrates the currently approved RTIs, and focuses on the mechanisms of action of the newer classes of RTIs...
- Pyrosequencing of the Camptotheca acuminata transcriptome reveals putative genes involved in camptothecin biosynthesis and transportYongzhen Sun
The Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Education, Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, PR China
BMC Genomics 12:533. 2011..Despite its importance, little is known about the transcriptome of C. acuminata and the mechanism of CPT biosynthesis, as only few nucleotide sequences are included in the GenBank database...
- The exploding field of the HCV polymerase non-nucleoside inhibitors: summary of a first generation compoundsEnzo Tramontano
Department of Sciences and Biomedical Technologies, University of Cagliari, Monserrato Cagliari, Italy
Mini Rev Med Chem 8:1298-310. 2008..All small molecules which have been identified to be selective non-nucleoside inhibitors (NNI) of the HCV RdRp to date are reported...
- 6-[1-(4-Fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester a novel diketo acid derivative which selectively inhibits the HIV-1 viral replication in cell culture and the ribonuclease H activity in vitroEnzo Tramontano
Department of Sciences and Biomedical Technologies, University of Cagliari, Cittadella Universitaria SS554, 09142 Monserrato Cagliari, Italy
Antiviral Res 65:117-24. 2005..Similar results were obtained against the Y181C and Y181C/K103N HIV-1 NNRTI resistant mutant strains. RDS 1643 may be the first HIV-1 inhibitor selectively targeted to the viral RT-associated RNase-H function...
- Biochemical characterization of HIV-1 reverse transcriptases encoding mutations at amino acid residues 161 and 208 involved in resistance to phosphonoformateE Tramontano
Dipartimento di Biologia Sperimentale, Sezione di Microbiologia, Universita di Cagliari, Italy
Biochem Pharmacol 56:1583-9. 1998..Overall, these results suggest that codons 161 and 208 of the HIV-1 RT gene are involved in substrate binding as well as in NRTI recognition, and provide more insights into the mechanism by which HIV-1 becomes resistant to PFA...
- Effects of new quinizarin derivatives on both HCV NS5B RNA polymerase and HIV-1 reverse transcriptase associated ribonuclease H activitiesE Tramontano
Department of Life and Environmental Sciences, University of Cagliari, Monserrato, Italy
J Chemother 23:273-6. 2011..Our results demonstrate that anthraquinone derivatives are promising anti-polymerase viral inhibitors...
- Purification and functional characterization of the full length recombinant Ebola virus VP35 protein expressed in E. coliLuca Zinzula
Department of Applied Sciences in Biosystems, University of Cagliari, Cittadella di Monserrato SS554, Monserrato, Cagliari, Italy
Protein Expr Purif 66:113-9. 2009....
- 6-aryl-2,4-dioxo-5-hexenoic acids, novel integrase inhibitors active against HIV-1 multiplication in cell-based assaysRoberta Costi
Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, I 00185 Rome, Italy
Bioorg Med Chem Lett 14:1745-9. 2004..9 microM; 3'-processing: IC(50)=7.0 microM). A preliminary molecular modeling study was carried out to compare the spatial conformation of 8a with those of L-731988 (4) and 5CITEP (7) in the IN core...
- 2,6-Bis(3,4,5-trihydroxybenzylydene) derivatives of cyclohexanone: novel potent HIV-1 integrase inhibitors that prevent HIV-1 multiplication in cell-based assaysRoberta Costi
Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici, Universita degli Studi di Roma La Sapienza, P le A Moro 5, I 00185, Rome, Italy
Bioorg Med Chem 12:199-215. 2004..A Q(2) of 0.73 was obtained with the final model, confirming the predictive ability of the model. By studying the PLS coefficients in informative 3-D contour plots, ideas for the synthesis of new compounds could be generated...
- New anti-human immunodeficiency virus type 1 6-aminoquinolones: mechanism of actionCristina Parolin
Department of Histology, Microbiology and Medical Biotechnologies, Section of Microbiology and Virology, University of Padua, Italy
Antimicrob Agents Chemother 47:889-96. 2003..6 nM). These data indicate that WM5 is a promising lead compound for the development of a new class of HIV-1 transcription inhibitors characterized by recognition of viral RNA target(s)...