General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors

Research output: Contribution to journalJournal articleResearchpeer-review

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General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors. / Lucas, Simon; Poulsen, Mette H; Nørager, Niels G; Barslund, Anne F; Bach, Tinna B; Kristensen, Anders S; Strømgaard, Kristian.

In: Journal of Medicinal Chemistry, Vol. 55, No. 22, 26.11.2012, p. 10297-10301.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Lucas, S, Poulsen, MH, Nørager, NG, Barslund, AF, Bach, TB, Kristensen, AS & Strømgaard, K 2012, 'General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors', Journal of Medicinal Chemistry, vol. 55, no. 22, pp. 10297-10301. https://doi.org/10.1021/jm301255m

APA

Lucas, S., Poulsen, M. H., Nørager, N. G., Barslund, A. F., Bach, T. B., Kristensen, A. S., & Strømgaard, K. (2012). General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors. Journal of Medicinal Chemistry, 55(22), 10297-10301. https://doi.org/10.1021/jm301255m

Vancouver

Lucas S, Poulsen MH, Nørager NG, Barslund AF, Bach TB, Kristensen AS et al. General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors. Journal of Medicinal Chemistry. 2012 Nov 26;55(22):10297-10301. https://doi.org/10.1021/jm301255m

Author

Lucas, Simon ; Poulsen, Mette H ; Nørager, Niels G ; Barslund, Anne F ; Bach, Tinna B ; Kristensen, Anders S ; Strømgaard, Kristian. / General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors. In: Journal of Medicinal Chemistry. 2012 ; Vol. 55, No. 22. pp. 10297-10301.

Bibtex

@article{abf3fd4da0f549238073b82776254226,
title = "General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors",
abstract = "Certain spiders contain large pools of polyamine toxins, which are putative pharmacological tools awaiting further discovery. Here we present a general synthesis strategy for this class of toxins and prepare five structurally varied polyamine toxins. Electrophysiological testing at three ionotropic glutamate receptor subtypes reveals that two of these, Nephila polyamine toxins 1 (NPTX-1) and 8 (NPTX-8), comprise intriguing pharmacological activities by having subnanomolar IC(50) values at kainate receptors.",
keywords = "Animals, Asparagine, Indoleacetic Acids, Molecular Structure, Polyamines, Receptors, Ionotropic Glutamate, Receptors, Kainic Acid, Spider Venoms, Spiders, Structure-Activity Relationship, Toxins, Biological, beta-Alanine",
author = "Simon Lucas and Poulsen, {Mette H} and N{\o}rager, {Niels G} and Barslund, {Anne F} and Bach, {Tinna B} and Kristensen, {Anders S} and Kristian Str{\o}mgaard",
year = "2012",
month = "11",
day = "26",
doi = "10.1021/jm301255m",
language = "English",
volume = "55",
pages = "10297--10301",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "22",

}

RIS

TY - JOUR

T1 - General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors

AU - Lucas, Simon

AU - Poulsen, Mette H

AU - Nørager, Niels G

AU - Barslund, Anne F

AU - Bach, Tinna B

AU - Kristensen, Anders S

AU - Strømgaard, Kristian

PY - 2012/11/26

Y1 - 2012/11/26

N2 - Certain spiders contain large pools of polyamine toxins, which are putative pharmacological tools awaiting further discovery. Here we present a general synthesis strategy for this class of toxins and prepare five structurally varied polyamine toxins. Electrophysiological testing at three ionotropic glutamate receptor subtypes reveals that two of these, Nephila polyamine toxins 1 (NPTX-1) and 8 (NPTX-8), comprise intriguing pharmacological activities by having subnanomolar IC(50) values at kainate receptors.

AB - Certain spiders contain large pools of polyamine toxins, which are putative pharmacological tools awaiting further discovery. Here we present a general synthesis strategy for this class of toxins and prepare five structurally varied polyamine toxins. Electrophysiological testing at three ionotropic glutamate receptor subtypes reveals that two of these, Nephila polyamine toxins 1 (NPTX-1) and 8 (NPTX-8), comprise intriguing pharmacological activities by having subnanomolar IC(50) values at kainate receptors.

KW - Animals

KW - Asparagine

KW - Indoleacetic Acids

KW - Molecular Structure

KW - Polyamines

KW - Receptors, Ionotropic Glutamate

KW - Receptors, Kainic Acid

KW - Spider Venoms

KW - Spiders

KW - Structure-Activity Relationship

KW - Toxins, Biological

KW - beta-Alanine

U2 - 10.1021/jm301255m

DO - 10.1021/jm301255m

M3 - Journal article

C2 - 23092360

VL - 55

SP - 10297

EP - 10301

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 22

ER -

ID: 45806724