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 repair defects. As a result, potent PARP-1 inhibitors have in the past three years entered early clinical trials in cancer patients, and the final results of these trials are eagerly awaited.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Plummer ERdoi
10.1016/j.coph.2006.02.004subject
Has Abstractpub_date
2006-08-01 00:00:00pages
364-8issue
4eissn
1471-4892issn
1471-4973pii
S1471-4892(06)00084-1journal_volume
6pub_type
杂志文章,评审abstract::The GABA(A) receptor is a pluripotent drug target mediating anxiolytic, sedative, anticonvulsant, muscle relaxant and amnesic activity. These drug actions have now been attributed to defined receptor subtypes. Thus, precise guidelines are available for the development of novel drugs with more selective action and less...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s1471-4892(01)00008-x
更新日期:2001-02-01 00:00:00
abstract::Over the past years tremendous amounts of clinical and fundamental data have been generated about GLP-1 and related therapeutic strategies for the treatment of type 2 diabetes. However, the cellular and physiological mechanisms through which GLP-1 is secreted, controls glycemia, and behaves as a therapeutic agent are ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2009.09.003
更新日期:2009-12-01 00:00:00
abstract::There is a growing body of evidence that although medical or surgical castration blocks the generation of gonadal testosterone in prostate cancer, androgens originating from other sources may continue to drive androgen receptor (AR) signaling. Recent studies have demonstrated high intratumoral levels of androgens and ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2008.06.004
更新日期:2008-08-01 00:00:00
abstract::Pseudomonas aeruginosa is an opportunistic pathogen that significantly contributes to morbidity and mortality in patients with cystic fibrosis. Defective mucociliary clearance associated with the absence of the functional cystic fibrosis transmembrane conductance regulator in airway epithelium plays a critical role in...
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::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::Recent advances in the management of gastric cancer, especially in the arena of chemotherapy, are paving the way for optimization of treatment that maximizes effectiveness while minimizing toxicity. The expansion of the chemotherapeutic armamentarium has led to multiple combinations of cytotoxic agents. Unfortunately,...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2006.05.002
更新日期:2006-08-01 00:00:00
abstract::COPD is a disease manifested as persistent airflow obstruction with an enhanced inflammatory response in the airways and lungs to noxious particles and gases which evokes symptoms of dyspnea on exertion, cough and mucus production. Airway smooth muscle plays a central role in the COPD diathesis and is implicated in ma...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.01.014
更新日期:2012-06-01 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::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::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::Recent advances in the development of potent and selective peptide and non-peptide ligands for peptidergic receptors are anticipated to help further unravel the roles of class I and II G-protein-coupled receptors in the pathogenesis of human diseases and to accelerate the clinical utility of small molecule peptidomime...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2003.06.003
更新日期:2003-10-01 00:00:00
abstract::Gut microbiota has a crucial role in the maintenance of health. Increasing evidence suggests that changes or disturbances in gut microbiota may be associated with various diseases. Therefore, preclinical and clinical studies related to gut microbiota are becoming increasingly important. Germ-free animal experimentatio...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2019.03.016
更新日期:2019-12-01 00:00:00
abstract::Viral and non-viral gene transfer technologies have been used to efficiently generate therapeutic T cells with desired cancer-specificity. Chimeric antigen receptors (CARs) redirect T cell specificity toward antibody-recognized antigens expressed on the surface of cancer cells, while T cell receptors (TCRs) extend the...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2015.08.006
更新日期:2015-10-01 00:00:00
abstract::The non-nucleoside reverse transcriptase inhibitors (NNRTIs) are allosteric inhibitors of HIV-1 reverse transcriptase and are classified into generations depending on their discovery and resistance profiles. The NNRTIs are used in combination regimens with antiretroviral agents that target two or more enzymes in the v...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2020.10.009
更新日期:2020-10-01 00:00:00
abstract::A single sub-psychotomimetic dose of ketamine, an ionotropic glutamatergic n-methyl-D-aspartate (NMDA) receptor antagonist, produces a fast-acting antidepressant response in patients suffering from major depressive disorder. Depressed patients report alleviation of core symptoms within 2 h of a single low-dose intrave...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2014.11.005
更新日期:2015-02-01 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::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::Stroke and multiple sclerosis (MS) illustrate how clinical imaging can facilitate early phase drug development and most effective medicine use in the clinic. Imaging has enhanced understanding of the dynamics of evolution of disease pathophysiology, better defining treatment targets. Imaging measures can enable strati...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2013.10.006
更新日期:2014-02-01 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::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::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::Neuromuscular blocking drugs were introduced into clinical practice in 1942. Although these drugs made new surgical techniques possible, they also led to morbidity and mortality owing to respiratory muscle paralysis and paralysis in the face of inadequate anesthesia. Newer competitive antagonists at the neuromuscular ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2004.12.009
更新日期:2005-06-01 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::Breast tumor kinase (Brk), also termed PTK6, is known to function in cell-type and context-dependent processes governing normal differentiation. However, in tumors in which Brk is overexpressed, this unusual soluble tyrosine kinase is emerging as a mediator of cancer cell phenotypes, including increased proliferation,...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2010.08.007
更新日期:2010-12-01 00:00:00
abstract::The activation of airway afferent neurons initiates a variety of reflexes including cough and bronchoconstriction. Like somatic afferent neurons involved in inflammation-induced hyperalgesia, the excitability of airway afferent neurons is not fixed but, rather, can be increased by the action of a variety of mediators ...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/s1471-4892(02)00147-9
更新日期:2002-06-01 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::Cholesterol epoxide hydrolase (ChEH) catalyzes the hydration of cholesterol-5,6-epoxides (5,6-EC) into cholestane-3β,5α,6β-triol. ChEH is a hetero-oligomeric complex called the anti-estrogen binding site (AEBS) comprising 3β-hydroxysterol-Δ(8)-Δ(7)-isomerase (D8D7I) and 3β-hydroxysterol-Δ(7)-reductase (DHCR7). D8D7I a...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2012.07.007
更新日期:2012-12-01 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::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
更新日期:2016-06-01 00:00:00
abstract::About one third of people in the world suffer from metabolic syndrome (MetS), with symptoms such as hypertension and elevated blood cholesterol, and with increased risk of developing additional diseases such as diabetes mellitus and heart disease. The progression of this multifactorial pathology, which targets various...
journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2011.09.012
更新日期:2011-12-01 00:00:00