Abstract:
:Putative druggable targets to selectively enhance cardiac conduction can be considered from the level of the ion channels determining the initiation and duration of the cardiac action potential to the gap junction proteins responsible for optimal cellular electrical coupling. Nature has provided a number of inherited disorders of conduction, the pathophysiology of which offer novel insights into future therapeutic targets. This review will focus upon the potential cellular and molecular targets for drug development based upon our knowledge of their pathophysiological impact.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Gomes J,Lambiase PDdoi
10.1016/j.coph.2008.11.008subject
Has Abstractpub_date
2009-04-01 00:00:00pages
154-9issue
2eissn
1471-4892issn
1471-4973pii
S1471-4892(08)00194-Xjournal_volume
9pub_type
杂志文章abstract::It has been a few decades since Ca(2+) was identified as one of the important factors that can accelerate gastric wound repair as well as contribute to epithelial homeostasis and regulation of gastric secretions. The mechanistic basis has remained largely unexplored in vivo because it was not possible to track in real...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2014.07.012
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abstract::The GABA(A) receptor is a pluripotent drug target mediating anxiolytic, sedative, anticonvulsant, muscle relaxant and amnesic activity. These drug actions have now been attributed to defined receptor subtypes. Thus, precise guidelines are available for the development of novel drugs with more selective action and less...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s1471-4892(01)00008-x
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abstract::CLEC-2 is a C-type lectin-like molecule that has recently been identified as a receptor on the surface of platelets. Ligand binding by CLEC-2 promotes phosphorylation of a tyrosine in the cytoplasmic domain YXXL motif of CLEC-2 by Src kinases and further downstream signalling events trigger platelet activation and agg...
journal_title:Current opinion in pharmacology
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abstract::Obesity is characterized by the presence of chronic inflammation in adipose tissue, particularly in the visceral compartment, that has been causally linked to development of obesity-associated comorbidities. This link can be either direct or indirect, through induction of insulin resistance. This review summarizes rec...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2013.04.008
更新日期:2013-08-01 00:00:00
abstract::The first therapeutic aptamer was approved for human use in 2004, and a range of chemical substitutions that improve the drug-like properties of aptamers has recently been shown to increase the utility of this modality. Currently there are both anticoagulant and antithrombotic aptamers in the clinic, and additionally ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2007.12.005
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abstract::Recent advances in the development of potent and selective peptide and non-peptide ligands for peptidergic receptors are anticipated to help further unravel the roles of class I and II G-protein-coupled receptors in the pathogenesis of human diseases and to accelerate the clinical utility of small molecule peptidomime...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2003.06.003
更新日期:2003-10-01 00:00:00
abstract::In our enthusiasm to advocate apoptosis as a therapeutic strategy for the management of disease we need to be mindful that the clearance of apoptotic cells is itself immunomodulatory and that it may not always be as benign or beneficial as we think. Indeed, the existence of free apoptotic cells in situ may potentially...
journal_title:Current opinion in pharmacology
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abstract::MicroRNAs (miRs) have recently emerged as a novel class of gene expression regulators. The number of studies documenting an altered miR expression pattern in cancer continues to expand rapidly. Critical information is continuously gained regarding how aberrantly expressed miRs contribute to carcinogenesis. Current stu...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2011.09.006
更新日期:2011-12-01 00:00:00
abstract::The hypocretins (abbreviated 'Hcrts' - also called 'orexins') are two neuropeptides secreted exclusively by a small population of neurons in the lateral hypothalamus. These peptides bind to two receptors located throughout the brain in nuclei associated with diverse cognitive and physiological functions. Initially, th...
journal_title:Current opinion in pharmacology
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journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2016.07.002
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abstract::Chronic liver diseases with different etiologies represent a major public health issue worldwide. Liver fibrosis is the common feature of almost all chronic liver diseases and remains a key determinant of clinical prognosis. Over the last two decades, basic science studies have uncovered molecular mechanisms underlyin...
journal_title:Current opinion in pharmacology
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abstract::The development of HIV protease inhibitors (HIV PIs) has been one of the most significant advances of the past two decades in controlling HIV infection. HIV PIs have been used successfully in highly active anti-retroviral therapy (HAART) for HIV infection, which is currently the most effective treatment available. Inc...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2014.07.008
更新日期:2014-12-01 00:00:00
abstract::The deployment of artemisinin-based combination therapies (ACTs) has been, and continues to be, integral to reducing the number of malaria cases and deaths. However, their efficacy is being increasingly jeopardized by the emergence and spread of parasites that are resistant (or partially resistant) to the artemisinin ...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2018.07.010
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abstract::The activation of airway afferent neurons initiates a variety of reflexes including cough and bronchoconstriction. Like somatic afferent neurons involved in inflammation-induced hyperalgesia, the excitability of airway afferent neurons is not fixed but, rather, can be increased by the action of a variety of mediators ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s1471-4892(02)00147-9
更新日期:2002-06-01 00:00:00
abstract::Gut microbiota has a crucial role in the maintenance of health. Increasing evidence suggests that changes or disturbances in gut microbiota may be associated with various diseases. Therefore, preclinical and clinical studies related to gut microbiota are becoming increasingly important. Germ-free animal experimentatio...
journal_title:Current opinion in pharmacology
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abstract::Phosphodiesterase-5 (PDE5) inhibitors and other agents that modulate intracellular cGMP are now emerging as promising, safe, and easy to administer therapies for pulmonary hypertension, with relatively few side effects. Recent studies have shown that PDE5 inhibitors are potent acute pulmonary vasodilators in experimen...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2004.12.008
更新日期:2005-06-01 00:00:00
abstract::Biomarker profiling is utilized to identify diagnostic and prognostic candidates for stroke. Clinical and preclinical biomarker data suggest altered circulating immune responses may illuminate the mechanisms of stroke recovery. However, the relationship between peripheral blood biomarker profile(s) and brain profiles ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2015.10.004
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abstract::The CD28 and B7 protein families are critical regulators of immune responses and, in the past few years, several new family members have been identified. Preclinical studies exploring the role of members of the CD28 and B7 families support the targeting of these pathways for new therapeutic approaches. Indeed, recent ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2005.02.003
更新日期:2005-08-01 00:00:00
abstract::In spite of the recent advancement in the molecular characterization of malignant gliomas and medulloblastomas, the treatment of primary brain tumors remains suboptimal. The use of small molecule inhibitors of intracellular signaling pathways, inhibitors of angiogenesis, and immunotherapic agents is limited by systemi...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2018.02.005
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abstract::Heart failure is a leading cause of death in the United States. Diabetes, also known as diabetes mellitus (DM), exponentially increases the risk of heart failure. The increase in oxidative stress and metabolic dysfunction caused by DM can lead to DNA damage and the development of diabetic cardiomyopathy. Ataxia telang...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2020.06.007
更新日期:2020-10-01 00:00:00
abstract::Idiopathic pulmonary fibrosis is the most common form of the interstitial lung diseases and is characterized by chronic progressive pulmonary parenchymal fibrosis. Although the diagnosis and pathophysiology of this disease have been better characterized over the past few years, there remains no effective therapy for t...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
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journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s1471-4892(02)00205-9
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abstract::Light offers unique advantages for studying and manipulating biomolecules and the cellular processes that they control. Optical control of ionotropic and metabotropic glutamate receptors has garnered significant interest, since these receptors are central to signaling at neuronal synapses and only optical approaches p...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2014.12.008
更新日期:2015-02-01 00:00:00
abstract::Antidepressants are among the most widely prescribed drugs, however the mechanism underlying their therapeutic efficacy is not known. Neurotrophic factors represent a promising class of targets for antidepressant treatments. We recently characterized a role for vascular endothelial growth factor (VEGF) in cellular and...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2007.10.013
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abstract::About one third of people in the world suffer from metabolic syndrome (MetS), with symptoms such as hypertension and elevated blood cholesterol, and with increased risk of developing additional diseases such as diabetes mellitus and heart disease. The progression of this multifactorial pathology, which targets various...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2011.09.012
更新日期:2011-12-01 00:00:00
abstract::Information about the activity of airway sensory afferent nerves in vivo can be obtained electrophysiologically by extracellular recording of action potentials. Apart from data capture, the basic techniques used for recording sensory nerve activity have not advanced greatly in 50 years. However, clearly they continue ...
journal_title:Current opinion in pharmacology
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abstract::The non-nucleoside reverse transcriptase inhibitors (NNRTIs) are allosteric inhibitors of HIV-1 reverse transcriptase and are classified into generations depending on their discovery and resistance profiles. The NNRTIs are used in combination regimens with antiretroviral agents that target two or more enzymes in the v...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2020.10.009
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abstract::An increasing number of genetic diseases are found to result from mutations that lead to retention of the affected proteins in the endoplasmic reticulum, where they are recognized as misfolded by the quality control system. Several of these conformational diseases involve mutations in G-protein-coupled receptors. Rece...
journal_title:Current opinion in pharmacology
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abstract::There have been significant developments in Ebola virus therapeutics. While the efficacy of several products was evaluated in the recent West Africa outbreak, a licensed treatment for EBOV disease remains elusive. Factors that negatively impacted the execution of clinical trials included an overall lack of world readi...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2016.08.016
更新日期:2016-10-01 00:00:00
abstract::The past decade has witnessed a growing interest in the trophic effects of antidepressant drugs. Antidepressants stimulate the production and signaling of plasticity-related proteins such as neurotrophins and cAMP response element binding protein, and neurotrophin signaling appears to be both sufficient and necessary ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
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