Abstract:
:The SERCA (sarcoplasmic/endoplasmic reticulum Ca2+-ATPase) is probably the most extensively studied membrane protein transporter. There is a vast array of diverse inhibitors for the Ca2+ pump, and many have proved significant in helping to elucidate both the mechanism of transport and gaining conformational structures. Some SERCA inhibitors such as thapsigargin have been used extensively as pharmacological tools to probe the roles of Ca2+ stores in Ca2+ signalling processes. Furthermore, some inhibitors have been implicated in the cause of diseases associated with endocrine disruption by environmental pollutants, whereas others are being developed as potential anticancer agents. The present review therefore aims to highlight some of the wide range of chemically diverse inhibitors that are known, their mechanisms of action and their binding location on the Ca2+ ATPase. Additionally, some ideas for the future development of more useful isoform-specific inhibitors and anticancer drugs are presented.
journal_name
Biochem Soc Transjournal_title
Biochemical Society transactionsauthors
Michelangeli F,East JMdoi
10.1042/BST0390789subject
Has Abstractpub_date
2011-06-01 00:00:00pages
789-97issue
3eissn
0300-5127issn
1470-8752pii
BST0390789journal_volume
39pub_type
杂志文章,评审abstract::We have shown that yeast mutants with defects in the Ada adaptor proteins are defective in hormone-dependent gene activation by ectopically expressed human glucocorticoid receptor (GR). Others have shown that the Ada2 protein is required for physical interactions between some activation domains and TBP (TATA-binding p...
journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:
更新日期:2000-01-01 00:00:00
abstract::Extracellular electron transfer has, in one decade, emerged from an environmental phenomenon to an industrial process driver. On the one hand, electron transfer towards anodes leads to production of power or chemicals such as hydrogen, caustic soda and hydrogen peroxide. On the other hand, electron transfer from catho...
journal_title:Biochemical Society transactions
pub_type: 杂志文章
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journal_title:Biochemical Society transactions
pub_type: 杂志文章
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0341271
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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journal_title:Biochemical Society transactions
pub_type: 杂志文章
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journal_title:Biochemical Society transactions
pub_type: 杂志文章
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0360263
更新日期:2008-04-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章
doi:10.1042/BST20190109
更新日期:2020-06-30 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0320655
更新日期:2004-11-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2019-04-30 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/0300-5127:0290661
更新日期:2001-11-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0330423
更新日期:2005-04-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0391149
更新日期:2011-10-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST20130217
更新日期:2013-12-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0341058
更新日期:2006-12-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2011-10-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2006-04-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/bst0310087
更新日期:2003-02-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2007-08-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2004-04-01 00:00:00
abstract::Mitogenic tyrosine kinase receptors such as the EGFR (epidermal growth factor receptor) are endocytosed once they are activated at the cell surface. After reaching the early endosome, they are ubiquitinated within their cytosolic domain and are consequently sorted away from recycling receptors. They are then incorpora...
journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0370146
更新日期:2009-02-01 00:00:00
abstract::The fission yeast Schizosaccharomyces pombe primarily detects glucose via a cAMP-signalling pathway. Components of this pathway include the Git3 G-protein-coupled receptor and a heterotrimeric G-protein, from which the Gpa2 Galpha subunit activates adenylate cyclase (Git2/Cyr1). Three additional proteins, Git1, Git7 a...
journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2005-02-01 00:00:00
abstract::The structural maintenance of chromosomes hinge domain containing protein 1 (SMCHD1) is a large multidomain protein involved in epigenetic gene silencing. Variations in the SMCHD1 gene are associated with two debilitating human disorders, facioscapulohumeral muscular dystrophy (FSHD) and Bosma arhinia microphthalmia s...
journal_title:Biochemical Society transactions
pub_type: 杂志文章
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更新日期:2020-08-28 00:00:00
abstract::Gap junctions are channels which allow electrical signals to propagate through the heart from the sinoatrial node and through the atria, conduction system and onwards to the ventricles, and hence are essential for co-ordinated cardiac contraction. Twelve connexin (Cx) proteins make up one gap junction channel, of whic...
journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2015-06-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2004-04-01 00:00:00
abstract::Functional cardiomyocytes can now be derived routinely from hPSCs (human pluripotent stem cells), which collectively include embryonic and induced pluripotent stem cells. This technology presents new opportunities to develop pharmacologically relevant in vitro screens to detect cardiotoxicity, with a view to improving...
journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
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更新日期:2010-08-01 00:00:00
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journal_title:Biochemical Society transactions
pub_type: 杂志文章,评审
doi:10.1042/BST0361011
更新日期:2008-10-01 00:00:00