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 SureChEMBL for patents. In addition, two portals are outlined, GPCRdb and the IUPHAR/BPS Guide to PHARMACOLOGY (GtoPdb) that are based on expert annotation. The former has an emphasis on structures, sequences, point mutations, analysis tools and visualisation. The latter focuses on endogenous GPCR ligands, pharmacological modulation, approved drugs, clinical candidates and tool compounds. Since data growth is accelerating, those embarking on GPCR projects should not only check databases but also recent journal and patent publications.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Southan Cdoi
10.1016/j.coph.2016.07.002subject
Has Abstractpub_date
2016-10-01 00:00:00pages
38-43eissn
1471-4892issn
1471-4973pii
S1471-4892(16)30062-5journal_volume
30pub_type
杂志文章,评审abstract：:Irritable bowel syndrome, which affects 5-10% of the population includes around 25% with predominantly diarrhoea (IBS-D). Several lines of evidence suggest an increase in mucosal 5-HT availability in IBS-D including a decrease in the serotonin transporter (SERT) which is also seen following acute diverticulitis. 5-HT(...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.02.005
更新日期：2011-02-01 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：:Therapeutic drug monitoring (TDM) plays a vital role in implementing precision medicine in inflammatory bowel disease (IBD), and may contribute to increased effectiveness, lower rates of drug toxicity and cost savings. While expert panels advocate the use of reactive TDM for anti-tumor necrosis factor (anti-TNF) agent...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2020.09.002
更新日期：2020-12-01 00:00:00
abstract：:Inhibition of the DNA repair enzyme poly(ADP-ribose) polymerase-1 (PARP-1) has been extensively investigated in the pre-clinical setting as a strategy for chemo- or radio-potentiation. Recent evidence has suggested that PARP inhibitors might be active as single agents in certain rare inherited cancers that carry DNA r...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.02.004
更新日期：2006-08-01 00:00:00
abstract：:Chemokines in the brain have been recognised as essential elements in neurodegenerative diseases and related neuroinflammation. Recent studies suggest that in addition to the orchestration of chemotaxis of immune cells, chemokines are also involved in neurodevelopment and neurophysiological signalling. ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00122-9
更新日期：2002-02-01 00:00:00
abstract：:Metabotropic glutamate receptors (mGluRs) are heavily expressed throughout the basal ganglia (BG), where they modulate neuronal excitability, transmitter release and long term synaptic plasticity. Therefore, targeting specific mGluR subtypes by means of selective drugs could be a possible strategy for restoring normal...
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：: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：:Understanding the mechanisms of cell-cell interaction is a key unanswered question in modern pharmacology, given crosstalk defects are at the basis of many pathologies. Microfluidics represents a valuable tool for analyzing intercellular communication mediated by transmission of soluble signals, as occurring for examp...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2013.07.005
更新日期：2013-10-01 00:00:00
abstract：:Metabotropic GABAB receptors clearly modify cognitive performance in preclinical animal models, yet translation to treating human disease has been elusive. Compared to their ionotropic GABAA receptor counterpart GABAB receptors not only regulate postsynaptic excitability but also regulate diverse synaptic inputs by pr...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2017.09.012
更新日期：2017-08-01 00:00:00
abstract：:Increased understanding of gastrointestinal pathophysiology in functional bowel disorders is leading to improved focus on relevant enteric, vagal and spinal afferent nervous systems, and targets operating on these systems. These targets include receptors for tachykinins, motilin, ghrelin, corticotropin-releasing facto...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(02)00228-x
更新日期：2002-12-01 00:00:00
abstract：:Oxidation-specific epitopes (OSE), present on oxidized LDL (OxLDL), apoptotic cells, cell debris and modified proteins in the vessel wall, accumulate in response to hypercholesterolemia, and generate potent pro-inflammatory, disease-specific antigens. They represent an important class of 'danger associated molecular p...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2013.02.005
更新日期：2013-04-01 00:00:00
abstract：:Platelets are known to play a pivotal role not only in the formation of arterial thrombosis but also in the progression of atherosclerotic disease. Recent data suggest that these activities of platelets have become enhanced in patients with type 2 diabetes, accounting for many of the cardiovascular complications. Alth...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.01.005
更新日期：2005-04-01 00:00:00
abstract：:AMP-activated protein kinase (AMPK) was initially viewed as energy sensor and activated by increased intracellular concentrations of AMP following nutrient deprivation. Physiological or pathological stimuli that deplete cellular energy activate AMPK that coordinates a cellular program that limits further ATP depletion...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.11.009
更新日期：2010-04-01 00:00:00
abstract：:Two new approaches for the treatment of osteoporosis are summarized, each having arisen out of important new discoveries in bone biology. Odanacatib (ODN) inhibits the enzyme, cathepsin K, that is essential for the resorbing activity of osteoclasts. It is effective in preventing ovariectomy-induced bone loss in precli...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2014.03.004
更新日期：2014-06-01 00:00:00
abstract：:In the current of era of developing antibacterial agents, including those for unmet medical need, Sponsors are required to submit a robust pre-clinical pharmacokinetic-pharmacodynamic (PK-PD) data package in exchange for limited clinical data. However, the clinical data package also needs to be as robust as possible. ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2017.09.010
更新日期：2017-10-01 00:00:00
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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2019.09.006
更新日期：2019-12-01 00:00:00
abstract：:Invasive treatment in peripheral artery disease (PAD) has evolved as a viable alternative to surgical treatment. However, beyond the common pathophysiological substrate, as far as treatment is concerned, each site of atherosclerotic disease (subclavian and vertebral arteries; carotid arteries; intracranial arterial tr...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.01.013
更新日期：2018-04-01 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：:G protein-coupled receptors (GPCRs), in recent years, have been shown to signal via multiple distinct pathways. Furthermore, biased ligands for some receptors can differentially stimulate or inhibit these pathways versus unbiased endogenous ligands or drugs. Biased ligands can be used to gain a deeper understanding of...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2014.04.002
更新日期：2014-06-01 00:00:00
abstract：:Reactive oxygen species play important roles in the pathophysiology of chronic heart failure secondary to chronic left ventricular hypertrophy or myocardial infarction. Reactive oxygen species influence several components of the phenotype of the failing heart, including contractile function, interstitial fibrosis, end...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.10.008
更新日期：2006-04-01 00:00:00
abstract：:Among the methods based on molecular imaging, the measure of the tracer uptake variation between a baseline and follow-up scan with the SUV and [(18)F]FDG-PET/CT is a very powerful tool for assessing response to treatment in oncology. However, the development of new targeted therapeutics and tissue pharmacokinetic eva...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.07.016
更新日期：2012-10-01 00:00:00
abstract：:Adiponectin, a novel hormone made by fat tissue, regulates energy metabolism and endothelial activation. Serum levels of adiponectin are reduced in conditions that are associated with an increased risk of cardiovascular disease, such as diabetes and the metabolic syndrome. Adiponectin trimers assemble into higher-orde...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2005.01.001
更新日期：2005-04-01 00:00:00
abstract：:Chronic inflammation is a risk factor for several gastrointestinal malignancies, including colorectal cancer. Recent epidemiological studies and clinical trials demonstrate that long-term use of non-steroidal anti-inflammatory drugs (NSAIDs) markedly reduced the relative risk of colorectal cancer. Chronic inflammation...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.08.003
更新日期：2009-12-01 00:00:00
abstract：:It is known that antimicrobial agents possess several, beneficial, secondary properties which complement their primary antimicrobial activity like the immunomodulatory capacity that enforces host defense mechanisms or reduces host inflammatory response. In this review the current state of our recent research about the...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2014.07.011
更新日期：2014-10-01 00:00:00
abstract：:Over the past few years, several groups have used voltage-sensitive dyes or calcium-indicator dyes to optically monitor the activity of several enteric neurons simultaneously. Some of the initial practical problems have been solved and these studies have successfully shown the spread of electrical activation within th...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00097-2
更新日期：2001-12-01 00:00:00
abstract：:Airway epithelial cells provide mechanical and immune protection against pathogens and allergens. Following activation, these cells produce a wide range of cytokines including thymic stromal lymphopoietin (TSLP). Recently it was established that a high level of TSLP is associated with asthma in mice and in humans. The...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.03.002
更新日期：2008-06-01 00:00:00
abstract：:Since its discovery in 1993 and subsequent development of selective antagonists, a growing number of studies support the use of serotonin 5-HT(6) receptor antagonism as a promising mechanism for treating cognitive dysfunction. Lately, several studies with structurally different compounds have shown that not only antag...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.01.004
更新日期：2011-02-01 00:00:00
abstract：:Acetylcholine, a major regulator of airway function, is not solely produced by neurons but also by a variety of non-neurons cells including various airway epithelial cells utilizing a molecular machinery of acetylcholine synthesis and release that differs from that of neurons. While canonical neuronal cholinergic sign...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2014.03.001
更新日期：2014-06-01 00:00:00
abstract：:Angiotensin type 1 (AT1) receptors are key effector elements of the renin-angiotensin system, mediating virtually all of the classical physiological actions of angiotensin II. Pharmacological blockade of the AT1 receptor effectively lowers blood pressure in a substantial proportion of patients with hypertension, indic...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2015.01.006
更新日期：2015-04-01 00:00:00
abstract：:The pharmaceutical industry is currently abandoning its antibacterial discovery research efforts. This seems to be part of a cyclical pattern in this therapeutic area. The reasons behind these ongoing cycles of feast and famine are multiple, but most revolve around the perception of market opportunities from the conti...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2003.04.003
更新日期：2003-10-01 00:00:00
