T
Todd Appleby
Researcher at Valeant Pharmaceuticals
Publications - 21
Citations - 1120
Todd Appleby is an academic researcher from Valeant Pharmaceuticals. The author has contributed to research in topics: NS5B & Polymerase. The author has an hindex of 15, co-authored 20 publications receiving 971 citations.
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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
RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer.
Cory Iverson,Gary Larson,Chon Lai,Li-Tain Yeh,Claudia Dadson,Paul Weingarten,Todd Appleby,Todd Vo,Andreas Maderna,Jean-Michel Vernier,Robert Hamatake,Jeffrey N. Miner,Barry D. Quart +12 more
TL;DR: Using pharmacokinetic and pharmacodynamic data, it is shown that maintaining adequate MEK inhibition throughout the dosing interval is likely more important than achieving high peak levels because greater efficacy was achieved with more frequent but lower dosing.
Journal ArticleDOI
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
I. Wayne Cheney,Shunqi Yan,Todd Appleby,Heli Walker,Todd Vo,Nanhua Yao,Robert Hamatake,Zhi Hong,Jim Zhen Wu +8 more
TL;DR: A hydrogen bond matrix involving the Pim-1 inhibitor, two water molecules, and the catalytic core, together with a potential weak hydrogen bond between an aromatic hydrogen on the R(1) phenyl ring and a main-chain carbonyl of Pim -1 accounts for the overall potency of this inhibitor.
Journal ArticleDOI
Crystal Structure of Complete Rhinovirus RNA Polymerase Suggests Front Loading of Protein Primer
Todd Appleby,Hartmut Luecke,Jae Hoon Shim,Jim Zhen Wu,I. Wayne Cheney,Weidong Zhong,Lutz Vogeley,Zhi Hong,Nanhua Yao +8 more
TL;DR: The crystal structure of human rhinovirus 16 3D RNA-dependent RNA polymerase (HRV16 3Dpol) is reported, representing the first complete polymerase structure from the Picornaviridae family.
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Novel thiazolones as HCV NS5B polymerase allosteric inhibitors: Further designs, SAR, and X-ray complex structure
Shunqi Yan,Gary Larson,Jim Zhen Wu,Todd Appleby,Yili Ding,Robert Hamatake,Zhi Hong,Nanhua Yao +7 more
TL;DR: SAR explorations and further structure-based design led to the identifications of 2 and 3 as novel HCV NS5B inhibitors.