Erik Wagner
Princeton University
15 Papers
372 Citations
Erik Wagner is an academic researcher from Princeton University. The author has contributed to research in topics: Small molecule & Amyloid precursor protein. The author has an hindex of 11, co-authored 15 publications.
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Papers
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.
Michael S. Malamas,Jim Erdei,Iwan Gunawan,Jim Turner,Yun Hu,Erik Wagner,Kristi Fan,Rajiv Chopra,Andrea Olland,Jonathan A. Bard,Steve Jacobsen,Ronald L. Magolda,Menelas N. Pangalos,Albert J. Robichaud +13 more
TL;DR: The comparatively large binding pocket of the BACE1 enzyme was methodically explored and key interactions between the ligand and the protein that contributed to the affinity were identified.
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Enhanced clearance of Aβ in brain by sustaining the plasmin proteolysis cascade
Jacobsen Js,Thomas A. Comery,Robert Martone,Elokdah H,Crandall Dl,Oganesian A,S. Aschmies,Yolanda Kirksey,Gonzales C,J. Xu,Hua Zhou,Kevin Atchison,Erik Wagner,M.M. Zaleska,Das I,Robert L. Arias,Jonathan A. Bard,David Riddell,Stephen J. Gardell,Magid Abou-Gharbia,Albert J. Robichaud,Ronald L. Magolda,George P. Vlasuk,Bjornsson T,Peter H. Reinhart,Menelas N. Pangalos +25 more
TL;DR: PAI-1 inhibitors augment the activity of tPA and plasmin in hippocampus, significantly lower plasma and brain Aβ levels, restore long-term potentiation deficits in hippocampal slices from transgenic Aβ-producing mice, and reverse cognitive deficits in these mice.
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Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors
Michael S. Malamas,Jim Erdei,Iwan Gunawan,Keith D. Barnes,Matthew R. Johnson,Yu Hui,Jim Turner,Yun Hu,Erik Wagner,Kristi Fan,Andrea Olland,Jonathan A. Bard,Albert J. Robichaud +12 more
TL;DR: These analogues demonstrate low nannomolar potency for BACE1 in a FRET assay, exhibit comparable activity in a cell-based (ELISA) assay, and show >100x selectivity for the other structurally related aspartyl proteases BACE2, cathepsin D, renin, and pepsin.
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Acylguanidines as Small-Molecule β-Secretase Inhibitors
Derek Cecil Cole,E.S. Manas,Joseph Raymond Stock,Jeffrey Scott Condon,Lee D. Jennings,Ann Aulabaugh,Rajiv Chopra,Rebecca Cowling,John W. Ellingboe,Kristi Fan,Boyd L. Harrison,Yun Hu,Steve Jacobsen,Guixan Jin,Laura Lin,Frank E. Lovering,Michael S. Malamas,Mark L. Stahl,James Strand,Mohani N. Sukhdeo,Kristine Svenson,M. James Turner,Erik Wagner,Junjun Wu,and Ping Zhou,Jonathan A. Bard +25 more
TL;DR: In this article, small-molecule acylguanidine inhibitors of BACE1 were identified, which form unique hydrogen-bonding interactions with the catalytic site aspartic acids and stabilize the protein in a flap-open conformation.
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Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability.
Michael S. Malamas,Albert J. Robichaud,Jim Erdei,Dominick Anthony Quagliato,William Ronald Solvibile,Ping Zhou,Koi Michele Morris,Jim Turner,Erik Wagner,Kristi Fan,Andrea Olland,Steve Jacobsen,Peter H. Reinhart,David Riddell,Menelas N. Pangalos +14 more
TL;DR: The identification of small molecule aminohydantoins as potent and selective human β-secretase inhibitors is reported, and the plasma and brain protein binding properties of these new analogs are affected by substitutions at the P1 phenyl moiety.
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