Abstract:
:Ionotropic neurotransmitter receptors mediate fast synaptic transmission by localizing at postsynapses. Changes in receptor number at synapses induce synaptic plasticity. Thus, mechanisms for the synaptic localization of receptors in basal transmission and synaptic plasticity have been investigated extensively. Recent findings reveal that synaptic localization of tetrameric AMPA receptors in basal transmission requires the PDZ binding of TARP auxiliary subunits, which modulate receptor properties and pharmacology. On the other hand, pentameric GABAA receptors require multiple receptor subunits for their synaptic localization in basal transmission. AMPA receptors seem to utilize distinct mechanisms for basal synaptic localization and synaptic insertion during plasticity. Revealing precise mechanisms for receptor synaptic localization may establish new approaches to control synaptic transmission.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Martenson JS,Tomita Sdoi
10.1016/j.coph.2014.11.011subject
Has Abstractpub_date
2015-02-01 00:00:00pages
102-8eissn
1471-4892issn
1471-4973pii
S1471-4892(14)00166-0journal_volume
20pub_type
杂志文章,评审abstract::Neurodegenerative diseases represent a large group of neurological disorders with heterogeneous clinical and pathological profiles. The majority of current therapeutic strategies provide temporary symptomatic relief but do not target the underlying disease pathobiology and thus do not affect disease progression. G pro...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2017.02.001
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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
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abstract::Type 1 human ether-a-go-go-related gene (hERG1) potassium channels are a key determinant of normal repolarization of cardiac action potentials. Loss of function mutations in hERG1 channels cause inherited long QT syndrome and increased risk of cardiac arrhythmia and sudden death. Many common medications that block hER...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2013.11.006
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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
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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
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abstract::Although only 5-10% of patients with asthma are relatively unresponsive to treatment with inhaled corticosteroids, refractory asthma represents an important condition, as these patients suffer considerable morbidity and mortality and consume a disproportionately large amount of health resource. Treatment options are l...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2007.03.001
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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.2005.10.003
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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
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abstract::Bone remodelling is an essential process for shaping and maintaining bone mass in the mature skeleton. During our lifetime bone is constantly being removed by osteoclasts and new bone is formed by osteoblasts. The activities of osteoclasts and osteoblasts must be regulated under a strict balance to ensure that bone ho...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2016.02.003
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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
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abstract::Sulfonylurea receptor 1 (SUR1) is a molecule with more diverse and critically important functions than previously recognized. Long viewed simply as a subunit involved in formation of a subset of K(ATP) channels, accumulating evidence indicates that SUR1 is newly upregulated in CNS ischemia and injury and is surprising...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2007.10.004
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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
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doi:10.1016/j.coph.2012.07.006
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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
更新日期:2016-02-01 00:00:00
abstract::A nuclear protein, high mobility group box 1 (HMGB1), is released passively by necrotic cells, and actively by macrophages/monocytes in response to exogenous and endogenous inflammatory stimuli. After binding to the receptor for advanced glycation end products (RAGE) or toll-like receptor 4 (TLR4), HMGB1 activates vas...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2005.10.010
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journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2019.09.010
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abstract::Immunotherapies revolutionised the treatment of several disorders but show specific side-effect profiles which frequently involve psychological symptoms. Long term interferon-alpha (IFN-alpha) therapy can cause wide-ranging psychiatric side-effects from fatigue, insomnia, anxiety to full-blown depression. This treatme...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2016.06.008
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abstract::Although oral administration of drugs is the most favorable route, the precise mechanism of intestinal epithelial permeation is not well understood. Recently, compelling evidence has emerged to show that absorptive transporters such as OATPs contribute to intestinal drug absorption. Since changes in intestinal transpo...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2013.09.001
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abstract::The inflammatory response is regulated by the production of different extracellular mediators, including lipids and extracellular nucleotides. In the extracellular environment, intermediate lipids activate specific G-protein-coupled receptors (GPCRs) in target cells and promote cell recruitment and activation. Extrace...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2019.02.004
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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::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
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doi:10.1016/j.coph.2005.01.001
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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
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doi:10.1016/j.coph.2018.08.001
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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::Rhabdomyolysis is a clinical condition of potential life threatening destruction of skeletal muscle caused by diverse mechanisms including drugs and toxins. Given the fact that structurally not related compounds cause an identical phenotype pinpoints to common targets or pathways, responsible for executing rhabdomyoly...
journal_title:Current opinion in pharmacology
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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 ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章
doi:10.1016/j.coph.2008.11.008
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abstract::Nanotechnology in medicine-nanomedicine-is extensively employed to diagnose, treat, and prevent pulmonary diseases. Over the last few years, this brave new world has made remarkable progress, offering opportunities to address historical clinical challenges in pulmonary diseases including multidrug resistance, adverse ...
journal_title:Current opinion in pharmacology
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abstract::Neuropathic pain is the most important type of chronic pain because it is refractory to available medications. Neuropathic pain occurs after peripheral nerve injury (PNI) or nerve damage by various reasons. In recent decades, a growing body of evidence shows that spinal microglia and P2X4 receptor (P2X4R), a subtype o...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2019.02.001
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abstract::Clostridium difficile disease is the major, known cause of nosocomial diarrhea and is an emerging cause of community-associated diarrhea. Recent outbreaks due to a strain of apparent increased virulence, BI/NAP1, and recognition of increasing metronidazole treatment failures as well as the morbidity associated with re...
journal_title:Current opinion in pharmacology
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abstract::Treatment strategies for inflammatory bowel disease (IBD) now increasingly target deep remission, yet the resultant more aggressive use of medical therapy is associated with potentially serious adverse events and significant costs. It is, therefore, of vital importance to consider when, how and in whom medical therapy...
journal_title:Current opinion in pharmacology
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abstract::Heteromerization of dopamine receptors has been shown for both the D(1)/D(5) and D(2)/D(3)/D(4) receptor families, which couple positively and negatively, respectively, to adenylyl cyclase. The present article reviews data on dopamine heteromers formed by D(3), focusing in particular on associations with their D(2) co...
journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2009.10.001
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