Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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New Peptidic Neuroprotectants Against NMDA Neurotoxicity: Syntheses and Biological Evaluations of Linear Complestatin Analogs

Author(s): Ho-Joon Park, Seung-Woo Kim, Young-Gyun Shin, Yun-Jung Kim, Ja-Kyeong Lee, Suk Bin Kong, Sung-Hwa Yoon.

Abstract:

Linear peptide analogs of complestatin were synthesized via solid phase peptide synthesis and tested in vitro as inhibitors against N-methyl-D-aspartic acid (NMDA) neurotoxicity as possible new peptidic neuroprotectants. While none of the analogs were as potent as the parent compound (IC50 = 2.5 μM), hexamer 11c and heptamer 1c, which contain all D-amino acids, showed modestly potent neuroprotective effects with IC50 values of 23.8 μM and 22.5 μM, respectively. The results indicate that the bicyclic ring structure of complestatin plays an important role for its inhibitory activity, and the D-stereochemistry of tryptophan (component F) is important for the potency of the linear peptide analogs.

Keywords: NMDA, Neurotoxicity, Complestatin, LDH release, 3,5-dichloro-4-hydroxyphenylglycine

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Article Details

VOLUME: 5
ISSUE: 2
Year: 2008
Page: [104 - 107]
Pages: 4
DOI: 10.2174/157018008783928526
Price: $58