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http://dx.doi.org/10.1016/S0140-6736(97)24021-3 | DOI Listing |
Med Sci (Paris)
November 2013
Université Paris Descartes, Inserm U1016, unité d'hépatologie, hôpital Cochin APHP, 27, rue du Faubourg Saint-Jacques, 75014 Paris, France.
The treatment of hepatitis C virus (HCV) infection markedly progressed these two last decades. Since 15 years, the combination of pegylated interferon α and ribavirin led to a sustained virologic response (SVR) which corresponds to a complete recovery in around 45 % of patients with HCV genotype 1, 65 % with HCV genotype 4, 70 % with HCV genotype 3 and around 85 % with HCV genotype 2. A better understanding of the HCV life-cycle recently resulted in the development of several potential direct-acting antiviral drugs (DAA) targeting viral proteins (NS3/4A protease inhibitors, NS5B nucleosidic and non nucleosidic polymerase inhibitors, NS5A replication complex inhibitors).
View Article and Find Full Text PDFExpert Opin Investig Drugs
December 2008
CV Therapeutics, Inc., Department of Bioorganic Chemistry, 3172 Porter Drive, Palo Alto, CA 94304, USA.
Background: The challenges in developing any A(1) adenosine receptor (A(1)-AdoR) agonist involve having the desired effect on target tissue while avoiding side effects due to activation of A(1)-AdoR on other tissues. A(1)-AdoR de-sensitization leading to tachyphylaxis is also another challenge.
Objectives: The major goal of this review is twofold: to highlight the structure affinity relationships (SAR) of A(1)-AdoR agonists, starting with initial lead compounds that were the genesis for second-generation compounds with high selectivity, affinity, and partial agonism; and to give an overview of the A(1)-AdoR agonists under development for various indications.
Infection
July 2000
Dept. of Virology, Geschäftsbereich Pharma, Bayer AG, Wuppertal, Germany.
Several first-generation nucleoside analogues have been tested against chronic hepatitis B virus (HBV) infection, but trials were unsuccessful or accompanied by toxicity. Recently, oral second-generation nucleoside analogues have been developed that have potent activity against HBV. The best-studied compound so far is lamivudine ((-)2'-deoxy-3'-thiacytidine; 3TC).
View Article and Find Full Text PDFNucleic Acids Symp Ser
July 1998
PE Applied Biosystems, Foster City, CA 94404, USA.
We have prepared and evaluated a series of structural analogues of TaqMan PCR probes in an effort to identify second-generation probes with improved physical properties and performance. Modifications have included non-nucleosidic dye linkers, 2'-O-Me RNA substitutions, and pyrimidine C5-propyne substitutions.
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