Per-Eric Lund
AstraZeneca
11 Papers
68 Citations
Per-Eric Lund is an academic researcher from AstraZeneca. The author has contributed to research in topics: Sodium channel blocker & Voltage-Gated Sodium Channel Blockers. The author has an hindex of 9, co-authored 11 publications.
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Papers
Potency optimization of Huwentoxin-IV on hNav1.7: a neurotoxin TTX-S sodium-channel antagonist from the venom of the Chinese bird-eating spider Selenocosmia huwena.
Jefferson D. Revell,Per-Eric Lund,John E. Linley,Jacky Metcalfe,Nicole Burmeister,Sudharsan Sridharan,Clare A. Jones,Lutz Jermutus,Maria A. Bednarek +8 more
TL;DR: The spider venom peptide Huwentoxin-IV (HwTx-IV) 1 is a potent antagonist of hNav1.7 and several peptides bearing mutations in these positions showed significantly increased potency on this channel, while maintaining the original selectivity profile of the wild-type peptide 1 on hNav 1.5.
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3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Istvan Macsari,Yevgeni Besidski,Gabor Csjernyik,Nilsson Linda I,Lars Sandberg,Ulrika Yngve,Kristofer Åhlin,Tjerk Bueters,Anders B. Eriksson,Per-Eric Lund,Elisabet Venyike,Sandra Oerther,Karin Hygge Blakeman,Lei Luo,Per I. Arvidsson,Per I. Arvidsson +15 more
TL;DR: The optimization, structure-activity relationships, and in vitro and in vivo characterization of a novel series of Na(V)1.7 inhibitors based on the oxoisoindoline core are presented, which may be valuable for further investigations for pain therapeutics.
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Cellular HTS Assays for Pharmacological Characterization of NaV1.7 Modulators
Shephali Trivedi,Kim Dekermendjian,Ronald Julien,Jian Huang,Per-Eric Lund,Johannes J. Krupp,Robert Kronqvist,Olof Larsson,Robert Bostwick +8 more
TL;DR: This paper describes the first comparison between all the HTS assays available today to study voltage-gated NaVs, and the results suggest that the Li-AAS assay is more suited as a first HTS assay when starting an NaV drug discovery campaign.
Ryanodine receptor-operated activation of TRP-like channels can trigger critical Ca2+ signaling events in pancreatic β-cells
Amanda Jabin Gustafsson,Hanna M. Ingelman-Sundberg,Mensur Dzabic,Justina Awasum,Nguyen Khanh Hoa,Claes-Göran Östenson,Cristina Pierro,Patrizia Tedeschi,Orison O. Woolcott,Shiue Chiounan,Per-Eric Lund,Olof Larsson,Md. Shahidul Islam +12 more
TL;DR: Activation of RY receptors leads to coherent changes in Ca2+ signaling, which includes activation of TRP‐like channels, membrane depolarization, activation of the voltage‐gated Ca 2+ channels and CICR.
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Ion Channel Screening Technology
Michael Dabrowski,Kim Dekermendjian,Per-Eric Lund,Johannes J. Krupp,Jon Sinclair,Olof Larsson +5 more
TL;DR: The variety of technologies available for ion channel screening are described and the opportunities these technologies provide are discussed and the challenges that remain to be addressed are highlighted.
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