Thursday, November 14, 2013
Publication and contact
Engineered bacterial LeuT
to detail antidepressant binding mechanisms
An engineered bacterial
homolog of eukaryotic biogenic amine transporters could be useful for
informing how marketed antidepressants interact with their targets. Biogenic
amine transporters are targeted by classes of drugs including selective serotonin
reuptake inhibitors, serotonin-noradrenaline reuptake inhibitors and
tricyclic antidepressants. Bacterial LeuT was engineered to have human
biogenic amine transporter-like pharmacology and then crystallized in complex
with drugs from four classes of antidepressants. Crystallographic analysis
showed that drugs from all four antidepressant classes have similar modes of
binding to the engineered LeuT and lock the protein in an outward-facing,
open conformation. Next steps could include generating additional crystal
structures of LeuT in complex with additional drug classes and using this
information to inform compound design.
Published online Nov. 14, 2013
Patent and licensing status
Wang, H. et al. Nature;
published online Oct. 13, 2013;
Contact: Eric Gouaux, Oregon Health & Science
University, Portland, Ore.
All contents Copyright © 1993-2017 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]