Abstract：
:Resveratrol, a natural phytoalexin that shows health-promoting benefits, is an inhibitor of store-operated calcium entry (SOCE). Knowledge of the molecular mechanism underlying this inhibition is required for the proper design of therapies that include resveratrol or related stilbenoids, but remains largely unknown. To unravel this mechanism, using HEK293 cells as a model, we found that resveratrol inhibited the ERK1/2 activation triggered by Ca²⁺ store depletion. As a consequence, resveratrol inhibited STIM1 phosphorylation at residues Ser575, Ser608, and Ser621. Because this phosphorylation regulates the dissociation of STIM1 from the microtubule plus-end binding protein EB1 under store depletion conditions, resveratrol inhibited STIM1-EB1 dissociation. This inhibition had downstream effects such as inhibition of STIM1 multimerization in response to store depletion, and a significant impairment in the binding of STIM1 to ORAI1. Although additional targets for resveratrol in the molecular mechanism that governs SOCE cannot be discarded, the present results demonstrate that ERK1/2 pathway is a major target for resveratrol, and that the impairment of its activation produces a significant inhibition of SOCE.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Casas-Rua V,Alvarez IS,Pozo-Guisado E,Martín-Romero FJdoi
10.1016/j.bcp.2013.09.018subject
Has Abstractpub_date
2013-12-01 00:00:00pages
1555-63issue
11eissn
0006-2952issn
1873-2968pii
S0006-2952(13)00623-0journal_volume
86pub_type
杂志文章abstract：:Intact, biological active insulin and pancreatic RNase can be absorbed from the intestinal lumen into the blood circulation. The absorption is dependent on the addition of bile acid (sodium cholate) and proteinase inhibitor. The quantitative absorption of insulin and pancreatic RNase has been demonstrated in an in sit...
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