Glutamate receptor agonists: stereochemical aspects

Research output: Contribution to journalReviewResearchpeer-review

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Glutamate receptor agonists : stereochemical aspects. / Vogensen, Stine Byskov; Greenwood, Jeremy R; Bunch, Lennart; Clausen, Rasmus Prætorius.

In: Current Topics in Medicinal Chemistry, Vol. 11, No. 7, 04.2011, p. 887-906.

Research output: Contribution to journalReviewResearchpeer-review

Harvard

Vogensen, SB, Greenwood, JR, Bunch, L & Clausen, RP 2011, 'Glutamate receptor agonists: stereochemical aspects', Current Topics in Medicinal Chemistry, vol. 11, no. 7, pp. 887-906. https://doi.org/10.2174/156802611795164990

APA

Vogensen, S. B., Greenwood, J. R., Bunch, L., & Clausen, R. P. (2011). Glutamate receptor agonists: stereochemical aspects. Current Topics in Medicinal Chemistry, 11(7), 887-906. https://doi.org/10.2174/156802611795164990

Vancouver

Vogensen SB, Greenwood JR, Bunch L, Clausen RP. Glutamate receptor agonists: stereochemical aspects. Current Topics in Medicinal Chemistry. 2011 Apr;11(7):887-906. https://doi.org/10.2174/156802611795164990

Author

Vogensen, Stine Byskov ; Greenwood, Jeremy R ; Bunch, Lennart ; Clausen, Rasmus Prætorius. / Glutamate receptor agonists : stereochemical aspects. In: Current Topics in Medicinal Chemistry. 2011 ; Vol. 11, No. 7. pp. 887-906.

Bibtex

@article{65fe91ac3c5c4c7a86b555e463594a9a,
title = "Glutamate receptor agonists: stereochemical aspects",
abstract = "The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally a-amino acids with one or more stereogenic centers due to strict requirements in the agonist binding pocket of the activated state of the receptor. By contrast, there are many examples of achiral competitive antagonists. The present review addresses how stereochemistry affects the activity of glutamate receptor ligands. The review focuses mainly on agonists and discusses stereochemical and conformational considerations as well as biostructural knowledge of the agonist binding pockets, which is useful in the design of glutamate receptor agonists. Examples are chosen to demonstrate how stereochemistry not only determines how the agonist binding pocket is filled, but also how it affects the conformational space of the ligand and in this way restricts the recognition of various glutamate receptors, ultimately leading to selectivity.",
keywords = "Former Faculty of Pharmaceutical Sciences",
author = "Vogensen, {Stine Byskov} and Greenwood, {Jeremy R} and Lennart Bunch and Clausen, {Rasmus Pr{\ae}torius}",
note = "Keywords: agonist, glutamate, ionotropic, metabotropic, stereochemistry, selectivity, X-ray structures",
year = "2011",
month = "4",
doi = "10.2174/156802611795164990",
language = "English",
volume = "11",
pages = "887--906",
journal = "Current Topics in Medicinal Chemistry",
issn = "1568-0266",
publisher = "Bentham Science Publishers",
number = "7",

}

RIS

TY - JOUR

T1 - Glutamate receptor agonists

T2 - stereochemical aspects

AU - Vogensen, Stine Byskov

AU - Greenwood, Jeremy R

AU - Bunch, Lennart

AU - Clausen, Rasmus Prætorius

N1 - Keywords: agonist, glutamate, ionotropic, metabotropic, stereochemistry, selectivity, X-ray structures

PY - 2011/4

Y1 - 2011/4

N2 - The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally a-amino acids with one or more stereogenic centers due to strict requirements in the agonist binding pocket of the activated state of the receptor. By contrast, there are many examples of achiral competitive antagonists. The present review addresses how stereochemistry affects the activity of glutamate receptor ligands. The review focuses mainly on agonists and discusses stereochemical and conformational considerations as well as biostructural knowledge of the agonist binding pockets, which is useful in the design of glutamate receptor agonists. Examples are chosen to demonstrate how stereochemistry not only determines how the agonist binding pocket is filled, but also how it affects the conformational space of the ligand and in this way restricts the recognition of various glutamate receptors, ultimately leading to selectivity.

AB - The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally a-amino acids with one or more stereogenic centers due to strict requirements in the agonist binding pocket of the activated state of the receptor. By contrast, there are many examples of achiral competitive antagonists. The present review addresses how stereochemistry affects the activity of glutamate receptor ligands. The review focuses mainly on agonists and discusses stereochemical and conformational considerations as well as biostructural knowledge of the agonist binding pockets, which is useful in the design of glutamate receptor agonists. Examples are chosen to demonstrate how stereochemistry not only determines how the agonist binding pocket is filled, but also how it affects the conformational space of the ligand and in this way restricts the recognition of various glutamate receptors, ultimately leading to selectivity.

KW - Former Faculty of Pharmaceutical Sciences

U2 - 10.2174/156802611795164990

DO - 10.2174/156802611795164990

M3 - Review

C2 - 21291400

VL - 11

SP - 887

EP - 906

JO - Current Topics in Medicinal Chemistry

JF - Current Topics in Medicinal Chemistry

SN - 1568-0266

IS - 7

ER -

ID: 33265460