Binding site of AMPA-receptor allosteric modulator

I.G. Tikhonova, M.I. Lavrov, V.A. Palyulin, N.S. Zefirov

Research output: Contribution to journalArticlepeer-review

4 Citations (Scopus)


The computer molecular docking of piperonyl acid piperidide (BDP) and some its analogs already known as ampakins was conducted for estimating their possible binding with AMPA-receptor glutamate domains in cyclothiazide binding area and for further design of new structures maximally complimentary to the receptor. On the base of the conducted docking it can be suggested that the binding site of BDP (amides of benzodioxane-6-carboxylic and piperonyl acids) analogs is located in AMPA-receptor cyclothiazide binding pocket. It is shown that formation of protein-ligand complexes of AMPA-receptor with benzodioxane-6-carboxylic and piperonyl acid derivatives, similarly to cyclothiazide, proceeds with interaction with Ser497, Leu751, which significance is confirmed by site-specific mutagenesis.
Original languageEnglish
Pages (from-to)268-270
Number of pages3
JournalDoklady Akademii nauk SSSR
Issue number2
Publication statusPublished - 01 Jan 2004

ASJC Scopus subject areas

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