Abstract：
:Gastroesophageal reflux disease (GERD) is increasingly common worldwide; symptoms differ between individuals and endoscopically visible injury is present in only about 50% of cases. Although GERD is a disorder of gastrointestinal motility and structure, the most effective therapy is based on the use of acid antisecretory drugs. Proton pump inhibitors (PPIs), the most effective class of acid suppression agents to date, have revolutionised the management of GERD. However, PPIs do have some shortcomings and recent developments include documentation of increased healing rates with more prolonged acid suppression, more prolonged acid suppression with a new PPI (tenatoprazole) and more rapid onset of acid suppression with a new class of drugs, the reversible, potassium-competitive acid blockers. Studies with motility agents, such as the 5-HT(4) partial agonist tegaserod and the GABA(B) agonist baclofen, indicate that motility is important in the pathogenesis of GERD but, for several reasons, it will be a challenge to develop new classes of drug that outperform current PPIs with respect to efficacy, broad applicability and safety.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Armstrong Ddoi
10.1016/j.coph.2005.09.001keywords:
subject
Has Abstractpub_date
2005-12-01 00:00:00pages
589-95issue
6eissn
1471-4892issn
1471-4973pii
S1471-4892(05)00156-6journal_volume
5pub_type
杂志文章,评审abstract：:11beta-hydroxysteroid dehydrogenases (11beta-HSDs) catalyse the interconversion of active cortisol and inert cortisone. Two isozymes have been discovered, each with unique properties and powerful biological roles. 11beta-HSD2 potently inactivates cortisol, protecting key tissues. By contrast, 11beta-HSD1 regenerates c...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.09.001
更新日期：2004-12-01 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
更新日期：2008-04-01 00:00:00
abstract：:Toll-like receptors (TLRs) play a crucial role in host defence and inflammation. Given that a significant amount of evidence implicates TLRs in the pathogenesis of immune diseases and cancer, and their activation occurs early in the inflammatory cascade, they are attractive targets for novel therapeutic agents. Potent...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.06.002
更新日期：2012-08-01 00:00:00
abstract：:Multiple myeloma is a tumour with a remarkably destructive effect on its host organ, the bone marrow. Through expression or secretion of adhesion molecules, growth factors, exosomes, miRNAs, chemokines and inhibitors, the tumour substantially alters its microenvironment, promoting both tumour survival and osteolytic b...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2016.02.013
更新日期：2016-06-01 00:00:00
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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.11.001
更新日期：2009-04-01 00:00:00
abstract：:The majority of kidney cancers are clear-cell carcinomas (ccRCC), characterized by the accumulation of cholesterol, cholesterol esters, other neutral lipids and glycogen. Rather than being a passive bystander, the clear-cell phenotype is suggested to be a biomarker of deregulated cholesterol and lipid biosynthesis, wh...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.08.002
更新日期：2012-12-01 00:00:00
abstract：:Improvements in databases have already impacted GPCR research. The purpose of the review is to give a snapshot of the GPCR data available and provide utility examples. Consequently, this review covers a small set of major databases, including UniProt for proteins, Ensembl for genes, ChEMBL for bioactive chemistry and ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2016.07.002
更新日期：2016-10-01 00:00:00
abstract：:Successful cancer therapy requires the selective killing of cancer cells. Many molecular components of the pathways that lead to cell death have recently been identified and a number of these, including p53, Apaf-1, and members of the inhibitor of apoptosis protein and Bcl-2 gene families, have been found to be altere...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00059-5
更新日期：2001-08-01 00:00:00
abstract：:Fibrosis can occur in most organs and is characterised by excessive and progressive extracellular matrix deposition and destruction of normal tissue architecture and function. In many cases treatment options are limited. Fibrotic diseases are therefore associated with high morbidity and mortality. Tissue biopsies rema...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2019.09.010
更新日期：2019-12-01 00:00:00
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journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.12.005
更新日期：2007-06-01 00:00:00
abstract：:G-protein-coupled receptors (GPCRs), the largest family of membrane proteins, represent ideal therapeutic targets for a number of disorders and diseases. Besides cell-based assays and high throughput screening (HTS), and thanks to the availability of milligram quantities of active purified receptors, protein-based app...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.04.002
更新日期：2009-10-01 00:00:00
abstract：:The use and utility of computational models in drug development has significantly grown in the last decades, fostered by the availability of high throughput datasets and new data analysis strategies. These in silico approaches are demonstrating their ability to generate reliable predictions as well as new knowledge on...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.08.007
更新日期：2018-10-01 00:00:00
abstract：:In response to the emergence of parasite drug resistance to currently deployed antimalarials, the scientific community, in partnership with the pharmaceutical industry and public organizations, has fashioned an antimalarial drug development portfolio for the sustained development and registration of safe, effective an...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.05.004
更新日期：2005-10-01 00:00:00
abstract：:Most of the G-protein-coupled receptors (GPCRs) in the human genome have been described. Investigation will now shift from discovery to analysis. Like many other genes, those encoding GPCRs are frequently found adjacent to each other in clusters. Duplicated genes often share ligands, signalling pathways and amino acid...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(02)00214-x
更新日期：2002-10-01 00:00:00
abstract：:Human pluripotent stem cells can be differentiated into specific, relevant cell types of interest including the cells of the retina and optic nerve. These cells can then be used to study fundamental biology as well as disease modelling and subsequent screening of potential treatments. Many models of differentiation an...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2019.09.003
更新日期：2019-10-01 00:00:00
abstract：:Angiotensin II blockade has become a standard anti-fibrotic therapy in renal diseases because it slows progression to end-stage renal disease. However, current data support the notion that angiotensin II blockade alone cannot stop progressive fibrotic disease. Of an increasing number of therapies showing efficacy in a...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(02)00144-3
更新日期：2002-04-01 00:00:00
abstract：:The evolving policies regarding the use of therapeutic Cannabis have steadily increased the public interest in its use as a complementary and alternative medicine in several disorders, including inflammatory bowel disease. Endocannabinoids represent both an appealing therapeutic strategy and a captivating scientific d...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.08.009
更新日期：2018-12-01 00:00:00
abstract：:Functional gastrointestinal disorders (FGIDs) are common conditions diagnosed by established symptom-based criteria. Dysregulation of the brain-gut axis is emerging as the primary pathophysiologic mechanism for FGIDs; this opens avenues for newer treatment modalities. Psychotropic agents act on a variety of neurotrans...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.07.012
更新日期：2008-12-01 00:00:00
abstract：:Treatment of complex diseases such as cancer, cardiovascular disease, diabetes or neurological disorders frequently warrants the utilization of drug combinations for therapeutic intervention. In fact, the most successful example is the current standard of care for HIV patients. However, identification of successful dr...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.07.008
更新日期：2018-10-01 00:00:00
abstract：:In most situations, the angiotensin AT2-receptor (AT2R) mediates physiological actions opposing those mediated by the AT1-receptor (AT1R), including a vasorelaxant effect. Nevertheless, experimental evidence vastly supports that systemic application of AT2R-agonists is blood pressure neutral. However, stimulation of A...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2015.01.004
更新日期：2015-04-01 00:00:00
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journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.03.004
更新日期：2018-02-01 00:00:00
abstract：:Heart disease is the most common cause of death in patients with chronic kidney disease (CKD), particularly in those receiving dialysis. Atherosclerosic cardiovascular (CV) disease (CVD) accounts for a large number of these deaths. Atherosclerosis is accelerated in patients with CKD due predominantly to the high preva...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.12.001
更新日期：2013-04-01 00:00:00
abstract：:Prostate cancer risk can be modified by environmental factors, however the molecular mechanisms affecting susceptibility to this disease are not well understood. As a result of a series of recently published studies, the steroidal lipid, cholesterol, has emerged as a clinically relevant therapeutic target in prostate ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.07.006
更新日期：2012-12-01 00:00:00
abstract：:Tuberculosis now ranks as the leading cause of death in the world due to a single infectious agent. Current standard of care treatment can achieve very high cure rates for drug-sensitive disease but requires a 6-month duration of chemotherapy. Drug-resistant disease requires significantly longer treatment durations wi...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.08.001
更新日期：2018-10-01 00:00:00
abstract：:The metabolic syndrome constitutes a group of metabolic conditions that increase the risk of developing diseases, including cardiovascular disease (CVD) and type 2 diabetes (T2D). LXRα/β are regulators of lipogenesis, cholesterol/glucose homoeostasis and inflammatory pathways, processes that are intertwined with devel...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2010.07.003
更新日期：2010-12-01 00:00:00
abstract：:Over the past few years small molecule inhibitors of both Src family kinases and focal adhesion kinase (FAK) have entered clinical studies for the treatment of solid tumours. These adhesion-linked kinases are involved in a number of pathways that have impact on the behaviour of tumour cells and the challenge is now, h...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.06.012
更新日期：2008-08-01 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
doi：10.1016/j.coph.2003.10.004
更新日期：2004-02-01 00:00:00
abstract：:Extracellular nucleotides play pivotal roles in the regulation of neuronal and glial functions in the nervous system through P2X receptors (P2XRs) and P2Y receptors (P2YRs). A growing body of evidence shows that microglia express several subtypes of P2XRs and P2YRs, and that these receptors play a key role in pain sig...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.10.014
更新日期：2012-02-01 00:00:00
abstract：:In vitro surveillance data, which provide key information to interpret the results of pharmacokinetic/pharmacodynamics (PK-PD) target attainment studies, are used to support dose selection decisions and recommendations for in vitro susceptibility testing criteria for antibacterial agents during drug development. Consi...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2017.10.009
更新日期：2017-10-01 00:00:00
abstract：:Classical gene targeting has identified many genes important for fetal and placental development. Null mutation of these genes may lead to fetal growth restriction, malformation or embryonic death. Growth restriction of epigenetic basis can predispose to adult-onset diseases. The mechanisms underlying this process, te...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00108-4
更新日期：2001-12-01 00:00:00
