2009
DOI: 10.1021/jm801445c
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Inhibition of Heat Shock Induction of Heat Shock Protein 70 and Enhancement of Heat Shock Protein 27 Phosphorylation by Quercetin Derivatives

Abstract: Inhibitors of heat-induced heat shock protein 70 (HSP70)a expression have the potential to enhance the therapeutic effectiveness of heat induced radiosensitization of tumors. Among known small molecule inhibitors, quercetin has the advantage of being easily modified for structure-activity studies. Herein, we report the ability of five mono-methyl and five carbomethoxymethyl derivatives of quercetin to inhibit heat-induced HSP70 expression and enhance HSP27 phosphorylation in human cells. While quercetin and se… Show more

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Cited by 48 publications
(53 citation statements)
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References 58 publications
(130 reference statements)
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“…The activity shown by S3 fraction was very similar to quercetin, decreasing not only the heat stress inducible HSP70 protein expression (Figure 3 A, B) but also its constitutive form (data not shown). The behavior exhibited by the S2 fraction under our experimental conditions was similar to that of rutin (quercetin glycoside), a compound known to increase the HSP70 level on the plasma membrane, rising tumor cell sensitivity to be lysed by NK cells (15).…”
Section: Palliacea Fractions Regulate Intracellular Hsp70 Expressionsupporting
confidence: 57%
See 1 more Smart Citation
“…The activity shown by S3 fraction was very similar to quercetin, decreasing not only the heat stress inducible HSP70 protein expression (Figure 3 A, B) but also its constitutive form (data not shown). The behavior exhibited by the S2 fraction under our experimental conditions was similar to that of rutin (quercetin glycoside), a compound known to increase the HSP70 level on the plasma membrane, rising tumor cell sensitivity to be lysed by NK cells (15).…”
Section: Palliacea Fractions Regulate Intracellular Hsp70 Expressionsupporting
confidence: 57%
“…The HSP70 protein expression was evaluated by Western blot. Quercetin, a flavonoid well known to decrease HSP70 expression (15,16) was used as a positive control. The activity shown by S3 fraction was very similar to quercetin, decreasing not only the heat stress inducible HSP70 protein expression (Figure 3 A, B) but also its constitutive form (data not shown).…”
Section: Palliacea Fractions Regulate Intracellular Hsp70 Expressionmentioning
confidence: 99%
“…One of our initial hypotheses, that liposomal doxorubicin would reduce heat-shock protein production was disproved. Nevertheless, these fi ndings raise the possibility of potentially extending the ablation zone by eliminating heat-shock protein expression with agents such as quercetin ( 49 ).…”
Section: Experimental Studies: Increasing Stress and Apoptosis At Ablmentioning
confidence: 99%
“…Que, however, not only suppresses HSP70 synthesis, but also features a host of physiologic activities, including antioxidant and anti-inflammatory activity. 27 The compound also suppresses the growth of cultured cells, glycolysis, and protein kinases and ATPase. 15 Factors other than HSP70 may therefore contribute to the effects of MW and Gln on OA.…”
Section: Hsp70 Induced Therapy For Osteoarthritismentioning
confidence: 99%