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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Chemogenomic Investigation of AP-1 Transcriptional Regulation of LTC4 Synthase Expression

Author(s): Tiana Chong, Michael McMillan, Jia Ling Teo, William R. Henderson Jr. and Michael Kahn

Volume 1, Issue 3, 2004

Page: [211 - 216] Pages: 6

DOI: 10.2174/1570180043398920

Price: $65


Asthma has reached epidemic proportions with approximately 200 million individuals affected worldwide. The disease is characterized by an oxidant / antioxidant imbalance in the lungs leading to activation of redox-sensitive transcription factors e.g. activator protein 1 (AP-1) and nuclear factor kappa B (NF-kappa B). We have previously described PNRI-299, a small molecule beta-strand mimetic template compound, as an inhibitor of the multifunctional AP endonuclease / redox factor 1 (Ref-1) [1]. PNRI-299 has demonstrable effects on the reduction of AP-1 driven transcription and beneficial pharmacological effects in a mouse asthma model. We now report the synthesis of this molecule and the effects of PNRI-299 on the expression of Leukotriene C4 (LTC4) synthase, a crucial enzyme for the formation of the cysteinyl leukotrienes.

Keywords: ap-1 transcriptional regulation, redox-sensitive transcription factors, activator protein 1

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