Abstract:
:Tumour resistance to anticancer agents remains a challenge in oncological practice, because it results in exposure to toxicities, unnecessary costs and, most importantly, delay of a potentially more effective treatment. Drug uptake by tumours may be impaired by several resistance pathways. Reasons for primary resistance may be that the drug is not delivered to the tumour or that its uptake by the tumour is not sufficient. Drug delivery depends on its distribution within the body, its bioavailability in the circulation and its transport to the tumour. Binding of drugs to circulating cells and proteins, formation of inactive metabolites as well as a rapid drug clearance may limit bioavailability. Furthermore, drug delivery to tumours is regulated by tumour vascularisation. Finally, tumour targets such as hormone receptors and efflux pumps also influence drug uptake by tumours. The use of specific PET tracers such as radiolabelled anticancer drugs (e.g. [(18)F]fluoropaclitaxel and [(18)F]5-fluorouracil) provide a unique means for individualized treatment planning and drug development. Combining these specific tracers with other less specific tracers, such as tracers for blood flow (e.g. [(15)O]H(2)O) and efflux (e.g. [(11)C]verapamil), may provide additional information on drug resistance mechanisms. Furthermore, radiolabelled anticancer agents may be valuable to evaluate the optimal timing of combination therapies. This review will focus on how PET can reveal different mechanisms of tumour resistance and thus may play a role in drug development and prediction of tumour response.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
van der Veldt AA,Luurtsema G,Lubberink M,Lammertsma AA,Hendrikse NHdoi
10.2174/138161208786404344subject
Has Abstractpub_date
2008-01-01 00:00:00pages
2914-31issue
28eissn
1381-6128issn
1873-4286journal_volume
14pub_type
杂志文章,评审abstract::Monocytes are leading component of the mononuclear phagocytic system that play a key role in phagocytosis and removal of several kinds of microbes from the body. Monocytes are bone marrow precursor cells that stay in the blood for a few days and migrate towards tissues where they differentiate into macrophages. Monocy...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190102104642
更新日期:2018-01-01 00:00:00
abstract::Nitric oxide is a ubiquitous molecule involved in a variety of biological processes. The specific action of NO depends on its enzymatic sources namely neuronal nitric oxide synthase (nNOS), endothelial NOS (eNOS) and inducible NOS (iNOS) and all three isoforms have been localized in the gastrointestinal tract. Constit...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612013398491
更新日期:2001-01-01 00:00:00
abstract::DAP12 is a novel immunoreceptor tyrosine-based activation motifs (ITAM)-bearing transmembrane adapter molecule. This molecule, together with its partner receptor complex molecules including the killer cell activating receptors (KARs), myeloid DAP12 associating lectin-1 (MDL-1), triggering receptor expressed on myeloid...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033392503
更新日期:2003-01-01 00:00:00
abstract::Low density lipoproteins (LDL) and high density lipoproteins (HDL) are independent risk factors for coronary heart disease (CHD); decreasing LDL-cholesterol (LDL-C) levels with statin therapy represents the primary goal in the management of cardiovascular disease. However, despite the efficacy of statins in reducing c...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990298
更新日期:2013-01-01 00:00:00
abstract::From a complications standpoint, diabetes mellitus is a disease of the vasculature. Diabetics face a considerably higher risk of developing cardiovascular and cerebrovascular diseases. Both large and small blood vessels are susceptible to alterations from diabetes. Endothelial cell dysfunction associated with small ve...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161208784705441
更新日期:2008-01-01 00:00:00
abstract::Pituitary adenylyl cyclase activating polypeptide (PACAP) is a neuropeptide with great neuroprotective effects and remarkable therapeutic potential. PACAP activates several cellular pathways to exert its protective effects. Emerging evidence shows that PACAP can modify the levels and activity of cell cycle components ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666181127102311
更新日期:2018-01-01 00:00:00
abstract::Mass spectrometry imaging (MSI) can uniquely detect thousands of compounds allowing both their identification and localization within biological tissue samples. MSI is an interdisciplinary science that crosses the borders of physics, chemistry and biology, and enables local molecular analysis at a broad range of lengt...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170111112550
更新日期:2017-01-01 00:00:00
abstract::Mass spectrometry information has long offered the potential of discovering biomarkers that would enable clinicians to diagnose disease, and treat it with targeted therapies. PeptideAtlas currently provides access to large-scale spectra data and identification information. This data, and the generation of targeted pep...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161212799277833
更新日期:2012-01-01 00:00:00
abstract::Large doses of omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) are used to treat several diseases including hypertriglyceridemia in humans. Modest levels of EPA and DHA may be obtained from food, particularly from fatty fish. This review presents the literature examining the differences ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209789909665
更新日期:2009-01-01 00:00:00
abstract::The increasing prevalence of persistent biofilm infections, such as wound infections, chronic lung infections or medical device- related infections, which usually tolerate conventional antibiotic treatment, calls for the development of new therapeutic strategies. To date, antimicrobial peptides (AMPs) are considered a...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140905124312
更新日期:2015-01-01 00:00:00
abstract::Agomelatine markedly differs from other classes of antidepressant drugs: its primary molecular targets in vivo are the melatonin MT(1) and MT(2) receptors, where it acts as a potent agonist, and the 5-HT(2C) receptors, where it exerts clear-cut antagonist properties. Agomelatine across a wide range of clinical trials ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209788168056
更新日期:2009-01-01 00:00:00
abstract::Atherosclerosis is an inflammatory vascular disease that is characterized by progressive accumulation of cholesterol in the arterial walls and it is a major cause of cardiovascular disease. Issues related to the side effects of synthetic drugs have in recent times, led to the misuse of drugs, a lack of patient consult...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666180911121525
更新日期:2018-01-01 00:00:00
abstract:AIMS:To compare the efficacy of pemafibrate (PF) and fenofibrate (FF) in treating dyslipidemia. METHODS:A comprehensive search was performed on the public database to identify relevant randomized controlled trials (RCTs), which compared the effects of PF and FF treatment in lipid parameters among patients with dyslipi...
journal_title:Current pharmaceutical design
pub_type: meta分析
doi:10.2174/1381612825666191126102943
更新日期:2019-01-01 00:00:00
abstract::Runx2/Cbfa/AML3 is a member of the runt homology domain family of transcription factors, essential for osteoblast differentiation and bone formation. Defining the molecular mechanisms by which Runx2 can function as a master regulatory gene for activating the program of osteoblastogenesis has provided novel insights fo...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612033453659
更新日期:2003-01-01 00:00:00
abstract::The brain is a complex, regulated organ with a highly controlled access mechanism: The Blood-Brain Barrier (BBB). The selectivity of this barrier is a double-edged sword, being both its greatest strength and weakness. This weakness is evident when trying to target therapeutics against diseases within the brain. Diseas...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612824666171201115126
更新日期:2018-01-01 00:00:00
abstract:PURPOSE:To summarize the main findings from research on food uses of Pine Bark Phenolic Extracts (PBPE), their origin, methods of extraction, composition, health effects, and incorporation into food products. METHODS:A narrative review of all the relevant papers known to the authors was conducted. RESULTS:PBPE are ma...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200212113903
更新日期:2020-01-01 00:00:00
abstract::Microdialysis is a technique for sampling the chemistry of the interstitial fluid of tissues and organs in animal and man. It is minimally invasive and simple to perform in a clinical setting. Although microdialysis samples essentially all small molecular substances present in the interstitial fluid the use of microdi...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612043384105
更新日期:2004-01-01 00:00:00
abstract::No-reflow, i.e., the lack of distal myocardial perfusion to fully recover following recanalization of an acutely occluded coronary artery, is not only a mere consequence of ischemic injury, as substantial microvascular alterations may also develop subsequently, after initial restoration of perfusion. Since part of per...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990357
更新日期:2013-01-01 00:00:00
abstract::Drug design based on the structure of specific enzymes playing a role in carcinogenesis, e.g. tyrosine kinases, has been successful at identifying novel effective anticancer drugs. In contrast, no success has been achieved in drug design attempts, in which transcription factors or DNA-transcription factor complexes in...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161207781757097
更新日期:2007-01-01 00:00:00
abstract::These are exciting times for bioinformaticians, computational biologists and drug designers with the genome and proteome sequences and related structural databases growing at an accelerated pace. The post-genomic era has triggered high expectations for a rapid and successful treatment of diseases. However, in this bio...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990379
更新日期:2013-01-01 00:00:00
abstract::A small but increasing number of gene expression based biomarkers are becoming available for routine clinical use, principally in oncology and transplantation. These underscore the potential of gene expression arrays and RNA sequencing for biomarker development, but this potential has not yet been fully realized and m...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150313130256
更新日期:2015-01-01 00:00:00
abstract::The intracellular hydric balance is an essential process of mammalian cells. The water movement across cell membranes is driven by osmotic and hydrostatic forces and the speed of this process is dependent on the presence of specific aquaporin water channels. Since the molecular identification of the first water channe...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161207781368738
更新日期:2007-01-01 00:00:00
abstract::Telomerase is a specialized enzymatic complex responsible for the synthesis of telomeric repeats 5'-TTAGGG-3' localized at the ends of eukaryotic chromosomes. This mechanism prevents shortening of telomeres after each cell division. The enzyme is detected in about 85% of human tumors, but it is not expressed in normal...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140630092721
更新日期:2014-01-01 00:00:00
abstract::Reduced levels of high-density lipoprotein cholesterol (HDL) are associated with a substantially increased risk of coronary disease and cardiovascular events. Furthermore, numerous studies have suggested that HDL may exert several potentially important antiatherosclerotic and endothelial-protective effects. In particu...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210791051013
更新日期:2010-05-01 00:00:00
abstract:BACKGROUND:In the last decade, the development of anti-inflammatory strategies emerged as new trend in cardiovascular (CV) pharmacotherapy. Anti-inflammatory properties have been previously identified in different classes of drugs used in primary CV prevention. However, the extent to which the modification of inflammat...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160822124546
更新日期:2016-01-01 00:00:00
abstract::Interest in opioid drugs like morphine, as the oldest and most potent pain-killing agents known, has been maintained through the years. One of the most frequent chronic pain sensations people experience is associated with pathological conditions of the musculoskeletal system. Chronic musculoskeletal pain is a major he...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990363
更新日期:2013-01-01 00:00:00
abstract::Research on Substance P (SP) has, until recently, focused on its role in pain and inflammation. However, a report that NK(1) receptor antagonists have utility in the treatment of depression has stimulated research into the function of SP and the NK(1)receptor in anxiety and depression. The distribution of SP and the N...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612053764779
更新日期:2005-01-01 00:00:00
abstract::Inhaled glucocorticoids, also know as corticosteroids (ICS), revolutionized the treatment of asthma by suppressing airways inflammation and ICS therapy now forms the basis of treatment of asthma of all severities. More recently and usually in combination with a long-acting β-agonist (LABA), ICS use has been establishe...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161210793797889
更新日期:2010-01-01 00:00:00
abstract::Iron oxide (Fe₃O₄) nanoparticles (IONPs) have received much attention for their utility in biomedical applications such as magnetic resonance imaging, drug delivery and hyperthermia. Recent studies reported that IONPs induced cytotoxicity in mammalian cells. However, little is known about the genotoxicity of IONPs fol...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612811319370011
更新日期:2013-01-01 00:00:00
abstract:BACKGROUND:Glioma is the most common human central nervous system tumour with a high degree of malignancy. Some Rab GTPases have significant effects on glioma. OBJECTIVE:This study aimed to investigate the effect of Rab3b (Rab GTPase3b) on human glioma cell proliferation and apoptosis by silencing Rab3b and to initial...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200917145228
更新日期:2020-09-17 00:00:00