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

doi: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

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

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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 language	English
Pages (from-to)	5753-5756
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	19
Early online date	13 Aug 2010
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.138
Publication status	Published - 1 Oct 2010

Keywords

AMPA receptor
hit-to-lead
SBDD
allosteric modulator

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10.1016/j.bmcl.2010.07.138

Jamieson-etal-BMCL-2010-A-novel-series-of-positive-modulators-of-the-AMPA-receptorAccepted author manuscript, 710 KBLicence: CC BY-NC-ND 4.0

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Jamieson, C., Basten, S., Campbell, R. A., Cumming, I. A., Gillen, K. J., Gillespie, J., Kazemier, B., Kiczun, M., Lamont, Y., Lyons, A. J., Maclean, J. K. F., Moir, E. M., Morrow, J. A., 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, 20(19), 5753-5756. https://doi.org/10.1016/j.bmcl.2010.07.138

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title = "A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies",

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.",

keywords = "AMPA receptor, hit-to-lead, SBDD , allosteric modulator",

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

year = "2010",

month = oct,

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doi = "10.1016/j.bmcl.2010.07.138",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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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

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

N2 - 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.

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

SN - 0960-894X

VL - 20

SP - 5753

EP - 5756

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

A novel series of positive modulators of the AMPA receptor: discovery and structure based hit-to-lead studies

Abstract

Keywords

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