Abstract:
:The hyperpolarization-activated cyclic nucleotide-gated (HCN) channels play an important role in the generation of pacemaker activity of cardiac sinoatrial node cells and immature cardiomyocytes. HCN channels are also present in adult atrial and ventricular cardiomyocytes, where the physiological role is currently under investigation. In different cardiac pathologies, dysfunctional HCN channels have been suggested to be a direct cause of rhythm disorders. While loss-of-function mutations of HCN channels are associated with sinus bradycardia, HCN channel gain-of-function in atrial fibrillation, ventricular hypertrophy and failure might help enhance ectopic electrical activity and promote arrhythmogenesis. Blockade of HCN channels with ivabradine, a selective bradycardic agent currently available for clinical use, improves cardiac performance and counteracts functional remodeling in experimental hypertrophy. Accordingly, ivabradine ameliorates clinical outcome in patients with chronic heart failure. Novel compounds with enhanced selectivity for cardiac HCN channel isoforms are being studied as potential candidates for new drug development.
journal_name
Curr Drug Targetsjournal_title
Current drug targetsauthors
Sartiani L,Romanelli MN,Mugelli A,Cerbai Edoi
10.2174/1389450116666150531152047subject
Has Abstractpub_date
2015-01-01 00:00:00pages
868-76issue
8eissn
1389-4501issn
1873-5592pii
CDT-EPUB-67766journal_volume
16pub_type
杂志文章,评审abstract::Fluoroquinolones are one of the world's most valuable and popularly used categories of antimicrobial agents. This paper attempts to review the substantial progress of fluoroquinolones from their discovery to black box warning. Antibiotic drug choice will remain difficult in the presence of increasing resistance, but t...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200621193355
更新日期:2020-01-01 00:00:00
abstract::The popular use of antioxidative vitamins illustrates the growing awareness of oxidative stress as an important hazard to our health and as an important factor in the ageing process. Superoxide radicals and superoxide-derived reactive oxygen species (ROS) are constantly formed in most cells and tissues. To ensure that...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450110607011505
更新日期:2006-11-01 00:00:00
abstract::Enzymes are proteins that act as biological catalysts to speed up cellular biochemical processes. According to their main Enzyme Commission (EC) numbers, enzymes are divided into six categories: EC-1: oxidoreductase; EC-2: transferase; EC-3: hydrolase; EC-4: lyase; EC-5: isomerase and EC-6: synthetase. Different enzym...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450119666181002143355
更新日期:2019-01-01 00:00:00
abstract::Androgen and androgen receptor (AR) play a critical role in the development of prostate cancer. Androgen deprivation therapy (ADT) has become the therapeutic mainstay for patients with metastatic prostate cancer. ADT can reduce the serum testosterone level from the normal range between 500 and 600 ng/dl to the castrat...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666141024114736
更新日期:2014-01-01 00:00:00
abstract::Efforts to interfere with the initiation and promotion of breast and other cancers by endocrine manipulation are not new. It is of obvious benefit to cancer patients to administer substances that combine minimal general toxicity with maximal oestrogen inhibition. Raloxifene is a relatively recent addition to a group o...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450013348263
更新日期:2001-12-01 00:00:00
abstract::Radiation-induced myelosuppression remains a rate-limiting factor of radiotherapy and chemotherapy. Therefore, hematological targets of radiation damage are of great significance for radiation oncology and normal tissue injury and protection. Protection of hematopoietic stem and progenitor cells is pivotal. In order t...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450111009011375
更新日期:2010-11-01 00:00:00
abstract::Retinal neovascularization and macular edema are central features of diabetic retinopathy, a major cause of blindness in working age adults. The currently established treatment for diabetic retinopathy targets the vascular pathology by laser photocoagulation. This approach is associated with significant adverse effect...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450054021981
更新日期:2005-06-01 00:00:00
abstract::Diacylglycerol (DAG) kinase (DGK) modulates the balance between the two signaling lipids, DAG and phosphatidic acid (PA), by phosphorylating (consuming) DAG to yield PA. Ten mammalian DGK isozymes have been identified to date. In addition to two or three cysteine-rich C1 domains (protein kinase C-like zinc finger stru...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008785132394
更新日期:2008-08-01 00:00:00
abstract::Viral myocarditis is a cardiac disease caused by Group B Coxsackie virus of Enterovirus genus in the Picorna viridae family. It causes heart failure in children, young and adults. Ten Percent (10%) of acute heart failure and 12% of sudden deaths in young and adults who are less than 40 years is due to this viral myoca...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450120666190618124722
更新日期:2019-01-01 00:00:00
abstract::Multifunctional rational drug design of protein tyrosine kinases inhibitors allows a potent drug to be utilized to treat more than one disease for greater patient benefits. Many protein tyrosine kinases (PTK), including Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), have been identified as potential drug ta...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945006776054997
更新日期:2006-03-01 00:00:00
abstract::Post-translational modification represents an important mechanism to regulate protein function in cardiac cells. Ubiquitin (Ub) and ubiquitin-like proteins (UBLs) are a family of protein modifiers that share a certain extent of sequence and structure similarity. Conjugation of Ub or UBLs to target proteins is dynamica...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450117666151209114608
更新日期:2018-01-01 00:00:00
abstract::Thrombus formation at a site of arterial injury (eg, rupture of an atherosclerotic plaque in a carotid artery), a crucial step in the pathogenesis of cerebral ischemia, is initiated by the adhesion of platelets to the arterial wall. In vivo, activated platelets release adenosine diphosphate (ADP), whose binding to the...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010790711987
更新日期:2010-03-01 00:00:00
abstract::The aim of the present article is to review the indications, the monitoring and the complications of sedation in the post-anaesthesia care unit (PACU). In this setting, sedation is often an unwanted side effect of anaesthetic drugs that delay discharge, however it could be specifically indicated. Such indications incl...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945005774574542
更新日期:2005-11-01 00:00:00
abstract::The complexity of the central nervous system (CNS) exposes it to a number of different diseases, often caused by only small variations in gene sequence or expression level. Antisense oligonucleotides and RNA interference-mediated therapies hold great promise for the treatment of CNS diseases in which neurodegeneration...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450053344920
更新日期:2005-02-01 00:00:00
abstract::Ulcerative colitis (UC) is an inflammatory bowel disease (IBD) characterized by chronic inflammation affecting the colonic mucosa, that can extend to the whole large bowel. The severity of mucosal lesions directly reflects the disease activity and severity and may be prognostic for an aggressive behavior of the pathol...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945011796818216
更新日期:2011-09-01 00:00:00
abstract::As early as 1940, Abraham and Chain described "an enzyme able to destroy penicillin". In the late 1940's, penicillin-resistant strains of Staphylococcus aureus were found to be a clinical problem. They produced a penicillinase that could hydrolyze the amide bond in the β-lactam ring. Later, an enzyme mediated by an R-...
journal_title:Current drug targets
pub_type: 历史文章,杂志文章,评审
doi:10.2174/1389450116666151001112859
更新日期:2016-01-01 00:00:00
abstract::Escalating resistance to almost every class of antibiotics is reducing the utility of currently available antimicrobial drugs. A part of this menace is attributed to poor pharmacokinetics and pharmacodynamics of the drug. Improvement in drug delivery is the most challenging task encountered by the pharmaceutical indus...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666151019101826
更新日期:2017-01-01 00:00:00
abstract::Seventy five percent of hospitalized patients with Crohn's disease suffer from malnutrition. One third of Crohn's disease patients have a body mass index below 20. Sixty percent of Crohn's disease patients have sarcopenia. However some inflammatory bowel disease (IBD) patients are obese or suffer from sarcopenic-obesi...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450115666140930150047
更新日期:2014-01-01 00:00:00
abstract::Saponins are plant glycosides that consist of a steroid, steroid alkaloid or triterpenoid aglycone and one or more sugar chains that are covalently linked by glycosidic binding to the aglycone. Glucose, galactose, glucuronic acid, xylose and rhamnose are commonly bound monosaccharides. Saponins are found in all organs...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945009787354584
更新日期:2009-02-01 00:00:00
abstract::The hedgehog signal transduction network is a critical regulator of metazoan development. Inappropriate activation of this network is implicated in several different cancers, including breast. Genetic evidence in mice as well as molecular biological studies in human cells clearly indicate that activated signaling can ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010792006753
更新日期:2010-09-01 00:00:00
abstract::Phytometabolites are functional elements derived from plants and most of them exhibit therapeutic characteristics such as anti-cancer, anti-inflammatory and anti-oxidant effects. Phytometabolites exert their anti-cancer effect by targeting multiple signaling pathways. One of the remarkable phenomena targeted by phytom...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450117666160401124842
更新日期:2017-01-01 00:00:00
abstract::Transport molecules can significantly affect the pharmacodynamics and pharmacokinetics of drugs. An important transport molecule, the 170 kDa P-glycoprotein (Pgp), is constitutively expressed at several organ sites in the human body. Pgp is expressed at the blood-brain barrier, in the kidneys, liver, intestines and in...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945006778019264
更新日期:2006-08-01 00:00:00
abstract::Hepatic diseases are turning into one of the few diseases that cannot be effectively cured due to some reasons although various receptors existed in the liver. Currently, several passive targeting delivery systems have been used in the drug/gene delivery for the treatment of hepatic diseases. For example, Zinostatin s...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140309232100
更新日期:2014-06-01 00:00:00
abstract::The incidence of lung cancer in 2007 is estimated to be 213,380 with 160,390 deaths in the United States. It will contribute to 31% of male and 26% of female cancer-related deaths and is the largest cause of cancer-related mortality in both men and women. Despite some advances in the treatment of advanced non-small ce...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010790031027
更新日期:2010-01-01 00:00:00
abstract::The production of reactive oxygen species is a normal part of cell physiology, but many internal and external stimuli are able to trigger the production of excess levels of oxidants that are potentially damaging. The threat of oxidative damage is particularly significant to DNA, as damaged bases can interfere with rep...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666150126111055
更新日期:2016-01-01 00:00:00
abstract::Endogenous opioid peptides have been studied extensively as potential therapeutics for the treatment of pain. The major problems of using natural opioid peptides as drug candidates are their poor receptor specificity, metabolic instability and inability to reach the brain after systemic administration. A lot of synthe...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450111314070008
更新日期:2013-06-01 00:00:00
abstract::Recent progress in molecular biology has provided application of gene transfer methods in arthritis. Two clinical trails using ex vivo retrovirus mediated delivery of interleukin -1 receptor antagonist gene for rheumatoid arthritis has begun in USA and Germany. However, there are still many issues to be elucidated; on...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450033490777
更新日期:2003-11-01 00:00:00
abstract::In the context of OA disease, NF-kappaB transcription factors can be triggered by a host of stress-related stimuli including pro-inflammatory cytokines, excessive mechanical stress and ECM degradation products. Activated NF-kappaB regulates the expression of many cytokines and chemokines, adhesion molecules, inflammat...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010791011938
更新日期:2010-05-01 00:00:00
abstract::Heme oxygenase-1 (HO-1) metabolizes heme to generate carbon monoxide (CO), biliverdin, and iron. Biliverdin is subsequently metabolized to bilirubin by biliverdin reductase. HO-1 has recently emerged as a promising therapeutic target in the treatment of vascular disease. Pharmacological induction or gene transfer of H...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450111009011504
更新日期:2010-12-01 00:00:00
abstract:BACKGROUND:Galanin (GAL) constitutes a family of neuropeptides composed of four peptides: (i) galanin (GAL), (ii) galanin-message associated peptide (GAMP), (iii) galanin-like peptide (GALP), and (iv) alarin. GAL contains 29/30 amino acids, and its biological action occurs through the interactions with its various rece...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200225112055
更新日期:2020-01-01 00:00:00