Jim Turner
Princeton University
12 Papers
279 Citations
Jim Turner is an academic researcher from Princeton University. The author has contributed to research in topics: Ligand (biochemistry) & Chemistry. The author has an hindex of 8, co-authored 11 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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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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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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Thiophene substituted acylguanidines as BACE1 inhibitors.
William Floyd Fobare,William Ronald Solvibile,Albert J. Robichaud,Michael S. Malamas,E.S. Manas,Jim Turner,Yun Hu,Erik Wagner,Rajiv Chopra,Rebecca Cowling,Guixan Jin,Jonathan A. Bard +11 more
TL;DR: A series of thiophene-substituted acylguanidines were designed from a pyrrole substituted acylGUanidine HTS lead, which provided a 25-fold enhancement in potency to yield compound 10a, which was 150 nM in a BACE1 FRET assay.
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Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.
Michael S. Malamas,Keith D. Barnes,Matthew R. Johnson,Yu Hui,Ping Zhou,Jim Turner,Yun Hu,Erik Wagner,Kristi Fan,Rajiv Chopra,Andrea Olland,Jonathan A. Bard,Menelas N. Pangalos,Peter H. Reinhart,Albert J. Robichaud +14 more
TL;DR: The identification of highly selective small molecule di-substituted pyridinyl aminohydantoins as beta-secretase inhibitors is reported and these ligands have also shown an exceptional selectivity against cathepsin D as well as the other aspartyl proteases mentioned.
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