Abstract
We have chemically synthesized several stable analogs of the naturally occurring hepoxilins, 12-LO products derived from arachidonic acid, which we found to have promising actions in a variety of test systems of disease. The analogs, PBTs, afford chemical and biological stability to the hepoxilin molecule. This article reviews some of our latest observations with the PBTs in the areas of inflammation (inhibition of the bleomycin-evoked lung fibrosis in mice in vivo), platelet aggregation (antagonism of the thromboxane receptor in human platelets in vitro) and thrombosis (inhibitors in vivo), and cancer (apoptosis of the human leukemia cell line, K562 in vitro and in vivo). The demonstration that the PBTs are active in vivo suggests that they can serve as a platform for their further development as novel therapeutics in disease.
Keywords: Hepoxilin analogs, PBTs, inflammation, thrombosis, apoptosis, cancer, proof of concept
Current Pharmaceutical Design
Title: Hepoxilin Analogs, Potential New Therapeutics in Disease
Volume: 12 Issue: 8
Author(s): C. R. Pace-Asciak, X. Li, N. Qiao, D. Reynaud, P. Demin and M. Abdelhaleem
Affiliation:
Keywords: Hepoxilin analogs, PBTs, inflammation, thrombosis, apoptosis, cancer, proof of concept
Abstract: We have chemically synthesized several stable analogs of the naturally occurring hepoxilins, 12-LO products derived from arachidonic acid, which we found to have promising actions in a variety of test systems of disease. The analogs, PBTs, afford chemical and biological stability to the hepoxilin molecule. This article reviews some of our latest observations with the PBTs in the areas of inflammation (inhibition of the bleomycin-evoked lung fibrosis in mice in vivo), platelet aggregation (antagonism of the thromboxane receptor in human platelets in vitro) and thrombosis (inhibitors in vivo), and cancer (apoptosis of the human leukemia cell line, K562 in vitro and in vivo). The demonstration that the PBTs are active in vivo suggests that they can serve as a platform for their further development as novel therapeutics in disease.
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Cite this article as:
Pace-Asciak R. C., Li X., Qiao N., Reynaud D., Demin P. and Abdelhaleem M., Hepoxilin Analogs, Potential New Therapeutics in Disease, Current Pharmaceutical Design 2006; 12 (8) . https://dx.doi.org/10.2174/138161206776055903
DOI https://dx.doi.org/10.2174/138161206776055903 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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