M
Michael J. Sofia
Researcher at Princeton University
Publications - 55
Citations - 3176
Michael J. Sofia is an academic researcher from Princeton University. The author has contributed to research in topics: Nucleoside & Prodrug. The author has an hindex of 27, co-authored 45 publications receiving 2872 citations.
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Journal ArticleDOI
Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus.
Michael J. Sofia,Donghui Bao,Wonsuk Chang,Jinfa Du,Dhanapalan Nagarathnam,Rachakonda Suguna,P. Ganapati Reddy,Bruce S. Ross,Peiyuan Wang,Hai-Ren Zhang,Shalini Bansal,Christine Espiritu,Meg Keilman,Angela M. Lam,Holly M. Micolochick Steuer,Congrong Niu,Michael J. Otto,Phillip A. Furman +17 more
TL;DR: Phosphoramidate prodrugs of the 5'-phosphate derivative of the β-d- 2'-deoxy-2'-α-fluoro-2-β-C-methyluridine nucleoside showed significant potency in the HCV subgenomic replicon assay and produced high levels of triphosphates 6 in primary hepatocytes and in the livers of rats, dogs, and monkeys when administered in vivo.
Journal ArticleDOI
Mechanism of Activation of PSI-7851 and Its Diastereoisomer PSI-7977
Eisuke Murakami,Tatiana Tolstykh,Haiying Bao,Congrong Niu,Holly M. Micolochick Steuer,Donghui Bao,Wonsuk Chang,Christine Espiritu,Shalini Bansal,Angela M. Lam,Michael J. Otto,Michael J. Sofia,Phillip A. Furman +12 more
TL;DR: A phosphoramidate prodrug of 2′-deoxy-2′-α-fluoro-β-C-methyluridine-5′-monophosphate, PSI-7851, demonstrates potent anti-hepatitis C virus (HCV) activity both in vitro and in vivo.
Journal ArticleDOI
Structural basis for RNA replication by the hepatitis C virus polymerase.
Todd Appleby,Jason K. Perry,Eisuke Murakami,Ona Barauskas,Joy Y. Feng,Aesop Cho,David A. Fox,Diana R. Wetmore,Mary E. McGrath,Adrian S. Ray,Michael J. Sofia,S. Swaminathan,Thomas E. Edwards +12 more
TL;DR: The details of HCV RNA replication are studied by determining crystal structures of stalled polymerase ternary complexes with enzymes, RNA templates, RNA primers, incoming nucleotides, and catalytic metal ions during both primed initiation and elongation of RNA synthesis.
Journal ArticleDOI
Nucleoside, Nucleotide, and Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA-Polymerase
Journal ArticleDOI
Synthesis of diastereomerically pure nucleotide phosphoramidates.
TL;DR: A class of stable phosphoramidating reagents containing an amino acid ester and two phenolic groups, one unsubstituted and the other with electron-withdrawing substituents is reported, used to prepare the HCV clinical candidate PSI-7977 in high yield and high diastereomeric purity.