Abstract：
:Hypothalamic gonadotropin-releasing hormone (GnRH) is a decapeptide that stimulates pituitary synthesis and secretion of gonadotropins and, therefore, gonadal hormones. GnRH antagonists, of which thousands have been formulated, inhibit the hormone from binding to its receptor, inducing a pharmacological hypophysectomy. Peptide derivations of GnRH and non-peptide compounds are both in clinical trials or approved for assisted reproduction. As these compounds reach the market, the use of antagonists might expand to treatment of other hormonally dependent diseases, hormonal male contraception and growth inhibition of extra-pituitary cancer cells expressing GnRH receptors.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Herbst KLdoi
10.1016/j.coph.2003.06.009keywords:
subject
Has Abstractpub_date
2003-12-01 00:00:00pages
660-6issue
6eissn
1471-4892issn
1471-4973pii
S1471489203001577journal_volume
3pub_type
杂志文章,评审abstract：:Diabetes-induced hyperglycemia is a causal factor for cardiovascular disease (CVD) and, specifically, peripheral artery disease (PAD). Metformin is the cornerstone drug therapy for glucose-lowering that exerts beneficial effects beyond glycemic control. New glucose-lowering drugs have recently been shown cardiovascula...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.03.001
更新日期：2018-04-01 00:00:00
abstract：:DNA-targeted chemotherapies remain fundamental in clinical management of both common solid tumours and hematologic malignancies. Recent studies indicate that novel combinations of cytotoxic chemotherapy may have significant activity even in tumours regarded as being resistant to conventional chemotherapy. In addition,...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2012.03.008
更新日期：2012-08-01 00:00:00
abstract：:In part because it is amphetamine derived, ecstasy has inherited some of its parent compound's reputation for being neurotoxic. However, whereas amphetamine and methamphetamine undoubtedly cause irreversible brain damage with long-term use, the jury is still out on the party drug ecstasy. The deadly reputation of ecst...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.08.007
更新日期：2005-02-01 00:00:00
abstract：:Calcitonin gene related peptide (CGRP) has been proposed to contribute to pain transmission and inflammation and for these reasons to the mechanism of migraine. CGRP is, in fact, expressed in and released from a subset of polymodal primary sensory neurons of the trigeminal ganglion. Release of CGRP in the dorsal spina...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.12.007
更新日期：2009-02-01 00:00:00
abstract：:The advent of near physiological organoid technology has produced a step change in our understanding of stem cells and has provided the research community with a powerful new cell based tool to model human physiology and disease. We review the pros and cons of intestinal organoid culture systems. The molecular and gen...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2017.09.003
更新日期：2017-12-01 00:00:00
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：:The bioavailability of drugs with an absorption window in the upper small intestine is generally limited with conventional pharmaceutical dosage forms. The residence time of such systems and, thus, of their drug release into the stomach and upper intestine is often short. To overcome this restriction and to increase t...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2006.04.007
更新日期：2006-10-01 00:00:00
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：: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：:New anti-infective drugs are an unmet necessity of modern medicine. The use of ∼omics technologies has exponentially increased the knowledge on active anti-infective structures, where to search for them and their mechanisms of action. Research involving extreme and unique environments (such as endophytes) revealed the...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2019.02.008
更新日期：2019-10-01 00:00:00
abstract：:High-quality monoclonal antibodies (mAbs) with specificity for relevant disease molecules can now be produced in abundance. Anti-tumour necrosis factor-alpha therapies have set a new standard for symptom control in rheumatoid arthritis, and blockade of tumour necrosis factor has the potential to protect joints from st...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(03)00032-8
更新日期：2003-06-01 00:00:00
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
更新日期：2013-12-01 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：:Reporter-gene assays offer an alternative to biochemical assays for following signal transduction pathways from receptors at the cell surface to nuclear gene transcription in living cells. Specific reporter-gene systems are now available for the study of ligand activity at G alpha(i/o), G alpha(s) and G alpha(q) G-pro...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/s1471-4892(01)00091-1
更新日期：2001-10-01 00:00:00
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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2013.11.006
更新日期：2014-04-01 00:00:00
abstract：:During the past decade, evidence has accumulated for the involvement of purines and purine receptors in the pathogenesis and pathophysiology of asthma and chronic obstructive pulmonary diseases. In particular, the indirect bronchospasmic and inflammatory actions of purines via the activation and degranulation of mast ...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2004.01.010
更新日期：2004-06-01 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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2018.02.005
更新日期：2018-02-01 00:00:00
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：: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：: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
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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2020.09.014
更新日期：2020-12-01 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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2008.12.018
更新日期：2009-02-01 00:00:00
abstract：:Myocardial apoptosis primarily triggered during reperfusion has been associated with cardiac dysfunction and extension of infarction. Although potential signaling pathways involved in triggering apoptosis remain to be clearly defined, an increasing number of experiments have implicated the generation of reactive oxyge...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2003.10.010
更新日期：2004-04-01 00:00:00
abstract：:The second messenger, cAMP, is one of the most important regulatory signals for control of steroidogenesis. This review focuses on current knowledge about regulation of cyclic nucleotides by phosphodiesterases (PDEs) in steroidogenic tissues. The first PDE known to directly regulate steroidogenesis was PDE2, the cGMP-...
journal_title：Current opinion in pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2011.09.003
更新日期：2011-12-01 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
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：: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
更新日期：2017-02-01 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
doi：10.1016/j.coph.2006.03.003
更新日期：2006-06-01 00:00:00
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
pub_type： 杂志文章,评审
doi：10.1016/j.coph.2009.10.001
更新日期：2010-02-01 00:00:00
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
