E
Eugene J. Eisenberg
Publications - 41
Citations - 1803
Eugene J. Eisenberg is an academic researcher. The author has contributed to research in topics: Prodrug & Pharmacokinetics. The author has an hindex of 18, co-authored 40 publications receiving 1702 citations.
Papers
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Journal ArticleDOI
Mechanism of Active Renal Tubular Efflux of Tenofovir
Adrian S. Ray,Tomas Cihlar,Kelly L. Robinson,Leah Tong,Jennifer E. Vela,Michael D. Fuller,Lani M. Wieman,Eugene J. Eisenberg,Gerry R. Rhodes +8 more
TL;DR: Members of the ATP-binding cassette family of efflux pumps expressed at the apical side of proximal-tubule cells were studied for the ability to transport TFV and ATP-dependent uptake of TFV was observed in membrane vesicles containing MRP4 but not in vesicle lacking the transporter.
Journal ArticleDOI
Selective Intracellular Activation of a Novel Prodrug of the Human Immunodeficiency Virus Reverse Transcriptase Inhibitor Tenofovir Leads to Preferential Distribution and Accumulation in Lymphatic Tissue
William A. Lee,Gong-Xin He,Eugene J. Eisenberg,Tomas Cihlar,S. Swaminathan,Andrew Mulato,Kenneth C. Cundy +6 more
TL;DR: An isopropylalaninyl monoamidate phenyl monoester prodrug of tenofovir was prepared, and its in vitro antiviral activity, metabolism, and pharmacokinetics in dogs were determined.
Journal ArticleDOI
Identification of GS 4104 as an Orally Bioavailable Prodrug of the Influenza Virus Neuraminidase Inhibitor GS 4071
Weixing Li,Paul A. Escarpe,Eugene J. Eisenberg,Kenneth C. Cundy,Clive Sweet,Kenneth J. Jakeman,James R. Merson,Willard Lew,Matthew A. Williams,Lijun Zhang,Choung U. Kim,Norbert Bischofberger,Ming S. Chen,Dirk B. Mendel +13 more
TL;DR: Results demonstrate that GS 4104 is an orally bioavailable prodrug of GS 4071 in animals and that it has the potential to be an oral agent for the prevention and treatment of influenza A and B virus infections in humans.
Patent
Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
Becker Mark W,Chapman Harlan H,Tomas Cihlar,Eugene J. Eisenberg,He Gong-Xin,Kernan Michael R,William A. Lee,Prisbe Ernest J,John C. Rohloff,Sparacino Mark L +9 more
TL;DR: In this article, a method is provided for screening prodrugs of methoxyphosphonate nucleotide analogues to identify drugs selectively targeting desired tissues with antiviral or antitumor activity.
Journal ArticleDOI
RNase H Active Site Inhibitors of Human Immunodeficiency Virus Type 1 Reverse Transcriptase: Design, Biochemical Activity, and Structural Information
Thorsten A. Kirschberg,Mini Balakrishnan,Neil H. Squires,Tiffany Barnes,Katherine M. Brendza,Xiaowu Chen,Eugene J. Eisenberg,Weili Jin,Nilima Kutty,Stephanie A. Leavitt,Albert Liclican,Liu Qi,Xiaohong Liu,John Mak,Jason K. Perry,Michael Wang,William J. Watkins,Eric B. Lansdon +17 more
TL;DR: Pyrimidinol carboxylic acids were designed as inhibitors of HIV-1 RNase H function and binding was demonstrated via a solid state structure of the isolated p15-Ec domain of HIV -1 RT showing inhibitor and two Mn(II) ions bound to theRNase H active site.