Abstract:
:Stimulation of β-adrenergic receptors in the heart is the most effective endogenous way to increase the mechanical performance of cardiac tissues to meet the requirements of a fight-or-flight situation or stress. On the other hand, sustained activation of cardiac β-receptors initiates maladaptive remodeling of the myocardium leading to cardiomyopathies and heart failure. Since both acute and chronic stimulation of β-adrenoceptors are arrhythmogenic, the application of β-receptor blockers exerts effective antiarrhytmic actions at both short and long time scale. Compared to other classes of antiarrhythmic agents, β-blockers are the class of antiarrhythmics that was shown to decrease mortality in postinfarct patients. Chemical, physiological, and pharmacological properties of the β-adrenoceptor related signaling, the role of β-1, β-2, and β-3 receptor subtypes, consequences of acute and long term β-adrenergic stimulation and the underlying proarrhythmic mechanisms, including the changes in cardiac ion currents and Ca(2+) handling, are reviewed in this paper together with the clinical relevance of cardioprotective β-blocking therapy.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Szentmiklosi AJ,Szentandrássy N,Hegyi B,Horvath B,Magyar J,Bányász T,Nanasi PPdoi
10.2174/1381612820666141029111240subject
Has Abstractpub_date
2015-01-01 00:00:00pages
1030-41issue
8eissn
1381-6128issn
1873-4286pii
CPD-EPUB-63125journal_volume
21pub_type
杂志文章,评审abstract::Growth factors (GFs) are extracellular signaling polypeptides regulating cell proliferation, differentiation and survival. They exert a wide spectrum of biological activities selectively binding to and activating specific membrane receptors which then transfer the message to cell interior inducing specific biochemical...
journal_title:Current pharmaceutical design
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abstract::Senescence is defined as an irreversible growth arrest that is characterised by a changed morphology, gene expression pattern and chromatin structure as well as an activated DNA damage response. Senescence has a dual role for tumour development-it acts as a tumour suppressor to prevent the proliferation of seriously d...
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abstract::Genetic variation in the receptors and other intracellular targets that mediate the pharmacodynamic effects of drugs can affect therapeutic outcomes. However, at present greater knowledge is available concerning the extent of gene variation in drug metabolizing enzymes that determine drug pharmacokinetics and, in turn...
journal_title:Current pharmaceutical design
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abstract::α-Synuclein aggregation is centrally implicated in Parkinson's disease (PD). It involves multi-step nucleated polymerization process via the formation of dimers, soluble toxic oligomers and insoluble fibrils. In the present study, we synthesized a novel compound viz., Curcumin-glucoside (Curc-gluc), a modified form of...
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abstract::Inhibition of fatty acid oxidation is well recognized as a potentially effective mechanism for controlling glycemia in non-insulin-dependent diabetes mellitus (NIDDM). However, a direct targeting of inhibition of the intramitochondrial beta-oxidation pathway or an indirect modulation of fatty acid oxidation by inhibit...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::Drug designing targeting protein-protein interactions is challenging. Because structural elucidation and computational analysis have revealed the importance of hot spot residues in stabilizing these interactions, there have been on-going efforts to develop drugs which bind the hot spots and out-compete the native prot...
journal_title:Current pharmaceutical design
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abstract::Tamoxifen is a selective oestrogen receptor modulator (SERM). SERMs act on oestrogen receptors to inhibit oestradiol mediated negative feedback on the hypothalamic-pituitary-gonadal (HPG) axis, thereby upregulating gonadotrophin secretion and release from the pituitary. Hence, Tamoxifen is used to upregulate activatio...
journal_title:Current pharmaceutical design
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abstract::Although escape from tumor dormancy has long been recognized as an important problem in the treatment of cancer, the molecular and cellular regulators underlying this transition remain poorly understood. The inability of the cancer cells to induce a complete and successful process of angiogenesis can result in tumor d...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract:BACKGROUND:Medical treatments are used either alone or in combination with assisted reproductive techniques for treatment of infertile patients with hypergonadotropic hypogonadism. A wide range of treatment options such as gonadotropins, aromatase inhibitors (AIs), selective estrogen receptor modulators (SERMs) and the...
journal_title:Current pharmaceutical design
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doi:10.2174/1381612826666201102110456
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract:BACKGROUNDS:Targeted therapy is the foundation of personalized medicine in cancer, which is often understood as the right patient using the right drug. Thinking from the viewpoint of determinants during personalized drug treatment, the genetics, epigenetics and metagenomics would provide individual-specific biological ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2018-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2013-01-01 00:00:00
abstract::Carbonic anhydrases (CAs, EC 4.2.1.1) are metalloenzymes which catalyze CO(2) hydration to bicarbonate and protons. Five genetically distinct classes are known, which represent an excellent example of convergent evolution. Inhibition of α-CAs from vertebrates, including humans, with sulfonamides was exploited clinical...
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pub_type: 杂志文章,评审
doi:10.2174/138161210793429797
更新日期:2010-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2013-01-01 00:00:00
abstract::Over the last several years, it has become increasingly clear that dendritic cells (DC) are not only critical for the initiation of T cell immunity, but these cells also determine the course of the subsequent immune response (i.e. tolerance vs. immunity, Th1 vs. Th2). However, the mechanisms by which DC can influence ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2001-07-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2019-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200110143706
更新日期:2020-01-01 00:00:00
abstract::Recent advances in DNA sequencing has made it possible to accurately decipher the entire genetic complement of a probiotic bacterium. Increases in sequencing capabilities have been enhanced through improved computer software that can annotate, or identify, the majority of genes encoded by the sequence. The availabilit...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612053382377
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abstract::Gonadotropin Releasing Hormone (GnRH) is at the centre of the scientific debate for the treatment of hypogonadotropic hypogonadism. Sexual maturation and reproductive function depend on the pulsatile secretion of GnRH are mainly congenital and may or may not be associated with other genetic anomalies or syndromes. Cli...
journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
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更新日期:2010-01-01 00:00:00
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journal_title:Current pharmaceutical design
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更新日期:2019-01-01 00:00:00
abstract::Treatment of chronic lymphocytic leukemia (CLL) has recently undergone revolutionary changes. Two large randomized trials demonstrated superiority of chemoimmunotherapy combining fludarabine and cyclophosphamide with monoclonal anti-CD20 antibody rituximab (FCR) over fludarabine and cyclophosphamide (FC) alone in firs...
journal_title:Current pharmaceutical design
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更新日期:2012-01-01 00:00:00
abstract::Approximately half of patients with schizophrenia have a lifetime diagnosis of substance abuse disorders. These dual diagnosis patients are more likely to have poorer outcomes, including more severe psychiatric symptoms with increased hospitalizations, higher utilization of services and frequent homelessness. Assessme...
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更新日期:2004-01-01 00:00:00
abstract::DNA methylation, a major regulator of epigenetic modifications has been shown to alter the expression of genes that are involved in aspects of glucose metabolism such as glucose intolerance, insulin resistance, β-cell dysfunction and other conditions, and it ultimately leads to the pathogenesis of type 2 diabetes mell...
journal_title:Current pharmaceutical design
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更新日期:2016-01-01 00:00:00
abstract::In order to develop an effective pharmacological treatment for obesity, an endogenous factor that promotes a positive energy balance by increasing appetite and decreasing fat oxidation could represent the drug target scientists have been looking for. The recently discovered gastric endocrine agent ghrelin, which appea...
journal_title:Current pharmaceutical design
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abstract::Metabolic syndrome (MetS) which is caused by poor dietary habits and sedentary behavior is a serious global health problem. MetS is a cluster of risk factors, represented by central obesity, hyperglycemia, dyslipidemia, and hypertension. In the 21st century, MetS and associated comorbidities, including obesity, diabet...
journal_title:Current pharmaceutical design
pub_type: 社论
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更新日期:2020-01-01 00:00:00