Activity Profiles of Linear, Cyclic Monomer and Cyclic Dimer of Enkephalin

Title
Activity Profiles of Linear, Cyclic Monomer and Cyclic Dimer of Enkephalin
Author(s)
홍남주김동희
Keywords
INVERSO MODIFIED ANALOGS; COMPUTER-SIMULATIONS; RECEPTOR SELECTIVITY; OPIOID RECEPTORS; DERMORPHIN; H-1-NMR; PEPTIDOMIMETICS; CONFORMATIONS; PHENYLALANINE; PENTAPEPTIDES
Issue Date
201201
Publisher
KOREAN CHEMICAL SOC
Citation
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.33, no.1, pp.261 - 269
Abstract
The cyclic dimers of enkephalin were isolated as minor components during the solution synthesis of the corresponding cyclic monomers. The ratio of cyclic dimer to monomer was approximately 1:4 from the percent of yields. In the receptor binding assay of two cyclic dimmers, (Tyr(2)-C[D-Glu-Phe-gPhe](2) 6, Tyr(2)-C[D-Asp-Phe-gPhe-rLeu](2) 8), both analogs exhibited the high preference for 5 receptor compared to monocyclic counterparts. In the nociceptive activity, both showed about 5 times less potent than the cyclic monomers. The repeated synthesis of 14-membered cyclic analog, Tyr-C[D-Glu-Phe-gPhe-D-rLeu] 14, which was known as having three distinct cis-trans isomers, gave rise to apparently different conformational analog arousing only trans isomer. In the receptor binding assay, it showed tremendously high selectivity toward mu receptor (delta/mu = 160).
URI
http://hdl.handle.net/YU.REPOSITORY/30032http://dx.doi.org/10.5012/bkcs.2012.33.1.261
ISSN
0253-2964
Appears in Collections:
생명공학부 > 생명공학부 > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE