Abstract:
:Prostaglandins serve as the connecting link between inflammation and cancer. mPGES1, the downstream enzyme in the prostaglandin pathway is considered a better target than COX-2 against the progression of cancer due to the cardiovascular and other complications associated with the inhibition of the latter. Despite the discovery of several compounds that inhibit mPGES1 none could enter the market as drugs because of the problems concerning specificity and unacceptable pharmacokinetic properties. Expression of mPGES1 is inducible in conditions of inflammation and hypoxia and its expression is regulated by a number of transcriptional factors. Targeting these transcription factors could be an alternative approach in the drug discovery process. In this review, the characteristics of the transcription factors, their ability to bind to the promoter of mPGES1 gene and the inhibitors against them have been discussed. The Structure Activity Relationship of the reported inhibitors is highlighted. Finally, practical challenges to further the drug development and future research directions are discussed. These novel compounds that are inhibitors of the major transcription factors are promising candidates for further development as inhibitors of mPGES1.
journal_name
Curr Drug Targetsjournal_title
Current drug targetsauthors
Ramanan M,Doble Mdoi
10.2174/1389450117666160826093137subject
Has Abstractpub_date
2017-01-01 00:00:00pages
119-131issue
1eissn
1389-4501issn
1873-5592pii
CDT-EPUB-78014journal_volume
18pub_type
杂志文章,评审abstract::Hepatic diseases are turning into one of the few diseases that cannot be effectively cured due to some reasons although various receptors existed in the liver. Currently, several passive targeting delivery systems have been used in the drug/gene delivery for the treatment of hepatic diseases. For example, Zinostatin s...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140309232100
更新日期:2014-06-01 00:00:00
abstract::Antimicrobial resistance of human pathogenic bacteria is an emerging problem for global public health. This resistance is often associated with the overproduction of membrane transport proteins that are capable to pump chemotherapeutics, antibiotics, detergents, dyes and organic solvents out of the cell. In Gram-negat...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008785747789
更新日期:2008-09-01 00:00:00
abstract::Adipose tissue plays an active role in energy balance because it is not only a lipid storing and mobilizing tissue but consists of functionally specialized tissues able to produce heat (in brown adipose tissue) and to produce or release a vast number of so called adipokines or adipocytokines. These consist of polypept...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450043490523
更新日期:2004-04-01 00:00:00
abstract::Excessive production of reactive oxygen species is an important mechanism underlying the pathogenesis of diabetes associated macrovascular and microvascular complications including diabetic nephropathy. Diabetic nephropathy is characterized by glomerular enlargement, early albuminuria and progressive glomerulosclerosi...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140321120635
更新日期:2014-05-01 00:00:00
abstract::The fibrinolytic system consists of a balance between rates of plasminogen activation and fibrin degradation, both of which are finely regulated by spatio-temporal mechanisms. Three distinct inhibitors of the fibrinolytic system that differently regulate these two steps are plasminogen activator inhibitor type-1 (PAI-...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450120666190715102510
更新日期:2019-01-01 00:00:00
abstract::The androgen receptor (AR) signalling pathway remains a key driver of prostate cancer progression despite castrate levels of testosterone in advanced disease. The androgen biosynthesis inhibitor abiraterone and the anti-androgen enzalutamide have been shown to prolong survival in randomized clinical trials both pre-an...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666150907101044
更新日期:2016-01-01 00:00:00
abstract::Escalating resistance to almost every class of antibiotics is reducing the utility of currently available antimicrobial drugs. A part of this menace is attributed to poor pharmacokinetics and pharmacodynamics of the drug. Improvement in drug delivery is the most challenging task encountered by the pharmaceutical indus...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666151019101826
更新日期:2017-01-01 00:00:00
abstract::Ceruloplasmin contains 95% of the copper in human serum and plays an important role in iron efflux from mammalian cells, including brain cells, due to the activity of ferroxidase, which oxidizes ferrous iron following its transfer to the cell surface via the iron transporter, ferroportin, and delivers ferric iron to e...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945012802002320
更新日期:2012-08-01 00:00:00
abstract::Programmed cell death, commonly associated with the term apoptosis, is an integrated intracellular program that plays a critical role in lymphoid tissue homeostasis. Alterations in this highly regulated process is a common feature of most lymphoid malignancies, thus facilitating tumor escape from traditional chemother...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945010791320863
更新日期:2010-07-01 00:00:00
abstract::The α7-nAChR plays critical roles in numerous organs and cells by regulating highly organ and cell typespecific functions. In this special issue different Authors have contributed to clarify the different roles played by the α7- nAChR. Post-translational processes such as receptor "underactivation" or "overactivation"...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/138945012800398946
更新日期:2012-05-01 00:00:00
abstract::The liver is essential for the control of glucose and lipid metabolism. Excessive accumulation of fat in the liver disturbs its function and leads to the development of fatty liver diseases. The nonalcoholic fatty liver disease (NAFLD) is a common type of fatty liver disease found in patients who have not consumed sig...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450116666150325231015
更新日期:2015-01-01 00:00:00
abstract::Recently, a significant number of breast cancer (BC) patients have been diagnosed at an early stage. It is therefore critical to accurately predict the risk of recurrence and distant metastasis for better management of BC in this setting. Clinicopathologic patterns, particularly lymph node status, tumor size, and horm...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200312105908
更新日期:2020-01-01 00:00:00
abstract::Treatment of chronic myeloid leukemia (CML) with interferon-alpha (IFN-α) was introduced in the early 1980s. Several clinical trials showed a survival advantage for patients treated with IFN-α compared to conventional chemotherapy. Some patients achieved longstanding complete cytogenetic remissions (i.e. >2 log tumor ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945011794815301
更新日期:2011-03-01 00:00:00
abstract::Adenocarcinoma of the prostate is the most common type of cancer, excluding skin cancer, and the second leading cause of cancer death in adult men in the United States. The lifetime risk for developing symptomatic prostate cancer is one in five for an American man. A pivotal step in carcinogenesis is a shift in the ba...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450033491118
更新日期:2003-04-01 00:00:00
abstract::The emergency of responsive drug delivery systems has contributed to the reduced cytotoxicity, the improved permeability in tissues and extended circulation time of the active drug. Of particular, enzyme-responsive nanoplatforms have attracted a lot due to the specificity and efficiency of an enzyme-catalyzed reaction...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450122666210114095614
更新日期:2021-01-13 00:00:00
abstract::The overuse of antibiotics which exerts the selective pressure for bacterial pathogens has facilitated the spread of antibiotics' resistance. Metallo-β-lactamases (MβLs) are zinc enzymes produced by an increasing number of bacterial pathogens. They can readily cleave carbapenems and most other β-lactams that are mains...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140326094504
更新日期:2014-01-01 00:00:00
abstract::Most pathological conditions that result in human diseases are associated with altered gene expression. With the advent of new technologies that might control gene expression and a broader knowledge of transcription factors and pathways, new strategies have emerged that offer promising first results for therapeutical ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945006777435326
更新日期:2006-06-01 00:00:00
abstract::The present article aims to review the literature on the relationship between psychology and inflammatory bowel disease (IBD). In particular, the first section is dedicated to explore the role of psychological factors in the etiopathology of the disease, its development and the efficacy of treatments, while the second...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450115666140627151702
更新日期:2014-01-01 00:00:00
abstract::Measurement of 25-hydroxyvitamin D (25-OHD) is widely used for assessing vitamin D status. There has been a dramatic increase in 25-OHD requests over recent years prompting many laboratories to consider the use of automated immunoassays. To achieve higher throughput, these methods have abandoned the traditional solven...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945011793591608
更新日期:2011-01-01 00:00:00
abstract:BACKGROUND:Recently, there are scientific attempts to discover new drugs in the biotechnology industry in order to treat various diseases including atherosclerosis. OBJECTIVE:The main objective of the present review was to highlight the cellular, molecular biology and inflammatory process related to the atheromatous p...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450117666160502151600
更新日期:2017-01-01 00:00:00
abstract::Antiphospholipid syndrome (APS) is characterized by a combination of clinical features consisted of thrombotic or pregnancy-related events and autoimmune antiphospholipid antibodies. In the 1998 International Consensus Preliminary Criteria, APS is defined by the concomitant presence of these clinical features and labo...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450054545999
更新日期:2005-08-01 00:00:00
abstract::The contribution of proteases to developmental, physiological and pathological processes has been well accepted. Cleavage of matrix proteins is a key requirement for cell migration and remodeling of the extracellular environment. The constant process of matrix turnover is dependent on the delicate balance between degr...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945008785909365
更新日期:2008-10-01 00:00:00
abstract::The heterogeneity of proteoglycans (PG)s contributes to their functional diversity. Many functions depend on their ability to bind and modulate the activity of components of the extracellular matrix (ECM). The ability of PGs to interact with other molecules, such as growth factors, is largely determined by the fine st...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450054863662
更新日期:2005-09-01 00:00:00
abstract:BACKGROUND:Nanotechnology deals with the manufacturing of materials at the atomic and molecular scale. According to the National Nanotechnology Initiative, nanotechnology denotes those structures which are nearly in 1-100 nm size regime in at least one dimension. OBJECTIVE:Nanotechnology in drug delivery has been evid...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450119666180131105822
更新日期:2018-01-01 00:00:00
abstract::It is well known that calorie restriction (CR) can retard the aging process in organisms ranging from yeast to non-human primates, and delay the onset of numerous age-related diseases including neurodegenerative disorders. Translation of the knowledge gained from CR research in animal models to disease prevention stra...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450111007011281
更新日期:2010-10-01 00:00:00
abstract::Alzheimer's disease (AD) has become linked to inflammation and metal biology. Metals (copper, zinc and iron) and inflammatory cytokines are significant factors that increase the onset of sporadic late onset forms of the dementia. The genetic discovery that alleles in the hemochromatosis gene accelerate the onset of di...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450043345272
更新日期:2004-08-01 00:00:00
abstract::Retinal neovascularization and macular edema are central features of diabetic retinopathy, a major cause of blindness in working age adults. The currently established treatment for diabetic retinopathy targets the vascular pathology by laser photocoagulation. This approach is associated with significant adverse effect...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1389450054021981
更新日期:2005-06-01 00:00:00
abstract:BACKGROUND:Different clinical studies have given inconsistent results on whether the use of antipsychotics increases the risk of thromboembolism. In this paper, we reviewed all relevant literature to provide suggestions for clinical diagnosis and treatment. METHODS:PubMed, Web of Science, EMBASE, MEDLINE, Cochrane and...
journal_title:Current drug targets
pub_type: 杂志文章
doi:10.2174/1389450121666200422084414
更新日期:2020-01-01 00:00:00
abstract:BACKGROUND:Osteosarcoma is considered the most frequent primary bone malignancy. Lung metastasis is the leading cause of death and the most consistent factor for predicting negative patient outcome in osteosarcoma. Third-generation nitrogen-containing bisphosphonates, such as zoledronic acid, have been shown to reduce ...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/1573399811666150615145409
更新日期:2018-01-01 00:00:00
abstract::Type 2 diabetes, which has dramatically increased during the last decade normally results from a combination of pancreatic beta cell dysfunction and insulin resistance. One of the most recent risk factors identified for type 2 diabetes is a sub-optimal fetal and neonatal environment. Numerous human epidemiological stu...
journal_title:Current drug targets
pub_type: 杂志文章,评审
doi:10.2174/138945007781386866
更新日期:2007-08-01 00:00:00