A novel series of positive modulators of the AMPA receptor

discovery and structure based hit-to-lead studies

Craig Jamieson, Stephanie Basten, Robert A. Campbell, Iain A. Cumming, Kevin J. Gillen, Jonathan Gillespie, Bert Kazemier, Michael Kiczun, Yvonne Lamont, Amanda J. Lyons, John K.F. Maclean, Elizabeth M. Moir, John A. Morrow, Marianthi Papakosta, Zoran Rankovic, Lynn Smith

Research output: Contribution to journalArticle

30 Citations (Scopus)
76 Downloads (Pure)

Abstract

Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.
Original languageEnglish
Pages (from-to)5753-5756
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number19
Early online date13 Aug 2010
DOIs
Publication statusPublished - 1 Oct 2010

Fingerprint

AMPA Receptors
Drug Design
Glutamate Receptors
Modulators
Demonstrations
Pharmaceutical Preparations
Lead

Keywords

  • AMPA receptor
  • hit-to-lead
  • SBDD
  • allosteric modulator

Cite this

Jamieson, Craig ; Basten, Stephanie ; Campbell, Robert A. ; Cumming, Iain A. ; Gillen, Kevin J. ; Gillespie, Jonathan ; Kazemier, Bert ; Kiczun, Michael ; Lamont, Yvonne ; Lyons, Amanda J. ; Maclean, John K.F. ; Moir, Elizabeth M. ; Morrow, John A. ; Papakosta, Marianthi ; Rankovic, Zoran ; Smith, Lynn. / A novel series of positive modulators of the AMPA receptor : discovery and structure based hit-to-lead studies. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 19. pp. 5753-5756.
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Jamieson, C, Basten, S, Campbell, RA, Cumming, IA, Gillen, KJ, Gillespie, J, Kazemier, B, Kiczun, M, Lamont, Y, Lyons, AJ, Maclean, JKF, Moir, EM, Morrow, JA, Papakosta, M, Rankovic, Z & Smith, L 2010, 'A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 19, pp. 5753-5756. https://doi.org/10.1016/j.bmcl.2010.07.138

A novel series of positive modulators of the AMPA receptor : discovery and structure based hit-to-lead studies. / Jamieson, Craig; Basten, Stephanie; Campbell, Robert A.; Cumming, Iain A.; Gillen, Kevin J.; Gillespie, Jonathan; Kazemier, Bert; Kiczun, Michael; Lamont, Yvonne; Lyons, Amanda J.; Maclean, John K.F.; Moir, Elizabeth M.; Morrow, John A.; Papakosta, Marianthi ; Rankovic, Zoran; Smith, Lynn.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 19, 01.10.2010, p. 5753-5756.

Research output: Contribution to journalArticle

TY - JOUR

T1 - A novel series of positive modulators of the AMPA receptor

T2 - discovery and structure based hit-to-lead studies

AU - Jamieson, Craig

AU - Basten, Stephanie

AU - Campbell, Robert A.

AU - Cumming, Iain A.

AU - Gillen, Kevin J.

AU - Gillespie, Jonathan

AU - Kazemier, Bert

AU - Kiczun, Michael

AU - Lamont, Yvonne

AU - Lyons, Amanda J.

AU - Maclean, John K.F.

AU - Moir, Elizabeth M.

AU - Morrow, John A.

AU - Papakosta, Marianthi

AU - Rankovic, Zoran

AU - Smith, Lynn

PY - 2010/10/1

Y1 - 2010/10/1

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AB - Starting from an HTS derived hit 1, application of biostructural data facilitated rapid optimization to lead 22, a novel AMPA receptor modulator. This is the first demonstration of how structure based drug design can be exploited in an optimization program for a glutamate receptor.

KW - AMPA receptor

KW - hit-to-lead

KW - SBDD

KW - allosteric modulator

UR - http://www.sciencedirect.com/science/article/pii/S0960894X10011108

U2 - 10.1016/j.bmcl.2010.07.138

DO - 10.1016/j.bmcl.2010.07.138

M3 - Article

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EP - 5756

JO - Bioorganic and Medicinal Chemistry Letters

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