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Cardiac ischemic conditioning has been shown to decrease ischemic injury in experimental models and clinically. Activation of survival pathways leading to heat shock proteins (HSP) modulation is an important contributor to this effect. We have previously shown that celastrol, an HSP90 modulator, achieves cardioprotection through activation of cytoprotective HSP's and heme-oxygenase-1 (HO-1). This is the first comparative evaluation of several modulators of HSP90 activity for cardioprotection. Furthermore, basic celastrol structure-activity relationship was characterized in order to develop novel potent infarct sparing agents suitable for clinical development.
This article was published in the following journal.
Name: Life sciences
To develop multifunctional drugs, a series of celastrol/NO donor hybrids were designed, synthesized and evaluated. The detection of NO release amounts showed that the more NO of these hybrids released...
Celastrol is an active ingredient of Chinese medicine Tripterygium wilfordii which is clinically used to treat the immune diseases. Currently, celastrol is documented as a potent agent for treating ca...
Celastrol, a naturally occurring pentacyclic triterpene, has attracted considerable interest because it exhibits potent anti-inflammatory and anti-tumor properties. However, the effects of celastrol i...
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Heat-shock proteins (HSP) have been very highly conserved throughout the evolution of species and are characterized by their chaperone function, thanks to their ability to prevent aggregat...
The purpose of this study is to see how safe the study drug is and to determine the best dose to use in cancer patients in the future. The study drug is designed to reduce the activity of...
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Substances that possess antiestrogenic actions but can also produce estrogenic effects as well. They act as complete or partial agonist or as antagonist. They can be either steroidal or nonsteroidal in structure.
Important modulators of the activity of plasminogen activators. Four inhibitors, all belonging to the serpin family of proteins, have been implicated in plasminogen activation inhibition. They are PAI-1; PAI-2; protease-nexin; and PROTEIN C INHIBITOR; (PAI-3). All inhibit both the tissue-type and urokinase-type plasminogen activators.
A class of MOLECULAR CHAPERONES whose members act in the mechanism of SIGNAL TRANSDUCTION by STEROID RECEPTORS.
Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.
A potent mycotoxin produced in feedstuffs by several species of the genus FUSARIUM. It elicits a severe inflammatory reaction in animals and has teratogenic effects.