Rational design of a novel AMPA receptor modulator through a hybridization approach

Tools

Caldwell, Nicola and Harms, Jonathan E. and Partin, Kathryn M. and Jamieson, Craig (2015) Rational design of a novel AMPA receptor modulator through a hybridization approach. ACS Medicinal Chemistry Letters. (https://doi.org/10.1021/ml5004553)

[thumbnail of Caldwell-etal-ACSMCL-2015-Rational-design-of-a-novel-AMPA-receptor-modulator] PDF. Filename: Caldwell_etal_ACSMCL_2015_Rational_design_of_a_novel_AMPA_receptor_modulator.pdf
Accepted Author Manuscript
Download (445kB)

Abstract

The α-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptors are a family of glutamate ion channels of considerable interest in excitatory neurotransmission and associated disease processes. Here, we demonstrate how exploitation of the available X-ray crystal structure of the receptor ligand binding domain enabled the development of a new class of AMPA receptor positive allosteric modulators (7) through hybridization of known ligands (5 and 6), leading to a novel chemotype with promising pharmacological properties.

ORCID iDs

Caldwell, Nicola, Harms, Jonathan E., Partin, Kathryn M. and Jamieson, Craig ORCID logoORCID: https://orcid.org/0000-0002-6567-8272;
  • Item type:Article
    ID code:51911
    Dates:
    Date
    Event
    2015
    Published
    11 February 2015
    Published Online
    11 February 2015
    Accepted
    Subjects:Science > Chemistry
    Department:Faculty of Science > Pure and Applied Chemistry
    Depositing user: Pure Administrator
    Date deposited:25 Feb 2015 05:12
    Last modified:30 Nov 2024 01:07
    URI:https://strathprints.strath.ac.uk/id/eprint/51911
CORE (COnnecting REpositories)