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Modulation of GABA(A) Receptors by Natural Products and the Development of Novel Synthetic Ligands for the Benzodiazepine Binding Site.

Nilsson, Jakob LU and Sterner, Olov LU (2011) In Current drug targets 12. p.1674-1688
Abstract
Nature provides science and society with a virtually unlimited supply of structurally diverse and biologically active molecules; the natural products. While some are directly useful in commercial applications, others are valuable for studying and understanding biological phenomena at the molecular level. An example is the signaling of nerve cells, which has been explored in considerable detail using a number of bioactive natural products. This review concerns primarily a part of the GABA inhibitory system of the central nervous system, the GABA(A) receptors, and natural products that have been reported to affect GABA(A) receptors in various ways. As the major inhibitory neurotransmittor, GABA plays a central role in the function of the... (More)
Nature provides science and society with a virtually unlimited supply of structurally diverse and biologically active molecules; the natural products. While some are directly useful in commercial applications, others are valuable for studying and understanding biological phenomena at the molecular level. An example is the signaling of nerve cells, which has been explored in considerable detail using a number of bioactive natural products. This review concerns primarily a part of the GABA inhibitory system of the central nervous system, the GABA(A) receptors, and natural products that have been reported to affect GABA(A) receptors in various ways. As the major inhibitory neurotransmittor, GABA plays a central role in the function of the central nervous system and modulates the activities of all neurons. Malfunctions in the GABA-operated systems cause a number of severe mental disorders, which consequently, at least in theory, can be treated with drugs. The natural products discussed in this review, acting on the GABA(A) receptors, are divided into the three main classes; terpenoids, polyacetylenic alcohols, and flavonoids. In addition, in a second part of the review, it is exemplified how knowledge about quantitative structure-activity relationships for a molecular target can be used to design novel, potent and selective compounds targeting the benzodiazepine binding site of the GABA(A) receptors. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Current drug targets
volume
12
pages
1674 - 1688
publisher
Bentham Science Publishers
external identifiers
  • wos:000299116800010
  • pmid:21561420
  • scopus:80054084047
ISSN
1873-5592
language
English
LU publication?
yes
id
7e3fbe08-bb74-4316-be55-d8a0c3e1ff54 (old id 1972916)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/21561420?dopt=Abstract
date added to LUP
2011-06-21 17:19:45
date last changed
2017-01-22 03:47:14
@article{7e3fbe08-bb74-4316-be55-d8a0c3e1ff54,
  abstract     = {Nature provides science and society with a virtually unlimited supply of structurally diverse and biologically active molecules; the natural products. While some are directly useful in commercial applications, others are valuable for studying and understanding biological phenomena at the molecular level. An example is the signaling of nerve cells, which has been explored in considerable detail using a number of bioactive natural products. This review concerns primarily a part of the GABA inhibitory system of the central nervous system, the GABA(A) receptors, and natural products that have been reported to affect GABA(A) receptors in various ways. As the major inhibitory neurotransmittor, GABA plays a central role in the function of the central nervous system and modulates the activities of all neurons. Malfunctions in the GABA-operated systems cause a number of severe mental disorders, which consequently, at least in theory, can be treated with drugs. The natural products discussed in this review, acting on the GABA(A) receptors, are divided into the three main classes; terpenoids, polyacetylenic alcohols, and flavonoids. In addition, in a second part of the review, it is exemplified how knowledge about quantitative structure-activity relationships for a molecular target can be used to design novel, potent and selective compounds targeting the benzodiazepine binding site of the GABA(A) receptors.},
  author       = {Nilsson, Jakob and Sterner, Olov},
  issn         = {1873-5592},
  language     = {eng},
  pages        = {1674--1688},
  publisher    = {Bentham Science Publishers},
  series       = {Current drug targets},
  title        = {Modulation of GABA(A) Receptors by Natural Products and the Development of Novel Synthetic Ligands for the Benzodiazepine Binding Site.},
  volume       = {12},
  year         = {2011},
}