Abstract:
:Human arylamine N-acetyltransferases 1 and 2 (NAT1 and NAT2) are polymorphic phase II xenobiotic-metabolising enzymes (XME) that acetylate arylamine compounds. They therefore play an important role in the detoxication and/or metabolic activation of certain therapeutic drugs, occupational chemicals and carcinogens. Although the use of the term "xenobiotic" implies that XME form a separate and distinct class of enzymes, possible endogenous substrates may exist. Unlike NAT2, NAT1 is produced in most tissues. Polymorphism at the NAT1 locus has been associated with the existence of at least 26 allelic variants, generating phenotypic variations in terms of NAT1 catalytic activity. This genetic variation affects the acetylator status of individuals, leading to interindividual differences in drug response and predisposition to disease in humans. Recent studies have shown that non-genetic factors may also regulate NAT1 activity at the posttranslational level, with potentially important consequences for drug toxicity. In this mini-review, we summarise what is currently known about the regulation of NAT1 activity by non-genetic factors, including substrates and oxidative stress. Recent findings presented here may account for the genotype/phenotype relationship for the NAT1 locus being less clear-cut than that for human NAT2.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Rodrigues-Lima F,Dupret JMdoi
10.2174/1381612043383845subject
Has Abstractpub_date
2004-01-01 00:00:00pages
2519-24issue
20eissn
1381-6128issn
1873-4286journal_volume
10pub_type
杂志文章,评审abstract::The drug discovery process in general is a very resource intensive undertaking that has existed for a very long time. In the last two decades, performing molecular simulations that determine the level of interaction between a protein and ligand have been refined to the point where they are now an essential part of the...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160414142530
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abstract::Ischaemic stroke of the brain accounts for about one third of all deaths in industrialized countries. Many of the patients who survive are severily impaired. Thus, there is an enormous need for pharmacotherapy for the treatment of ischaemic stroke. Why is such a treatment not available yet? Are the pathophysiological ...
journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990341
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150310101851
更新日期:2015-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2005-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160524144926
更新日期:2016-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,meta分析
doi:10.2174/1381612824666180406104516
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Sulfur mustard (SM)-induced airway injuries and chronic obstructive pulmonary disease (COPD) are characterized by chronic inflammation of the respiratory tract and share some similarities regarding the cellular and molecular mechanisms orchestrating airway destruction. Since available data regarding the immu...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160307150818
更新日期:2016-01-01 00:00:00
abstract::Carcinogenesis results from the long-term accumulation of genetic and epigenetic aberrations at the molecular level, which are under constant selection pressure for growth advantage. Recognizing that cancer is the result of this long-term, multi-step process provides opportunities for molecularly targeted cancer preve...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612023394935
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abstract::The involvement of the central nervous system (CNS) is one of the major causes of morbidity and mortality in systemic lupus erythematosus (SLE) patients and the less understood aspect of the disease. Its recognition and treatment continue to represent a major diagnostic and therapeutic challenge. Due to the lack of co...
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pub_type: 杂志文章,评审
doi:10.2174/138161208799316401
更新日期:2008-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161205774370843
更新日期:2005-01-01 00:00:00
abstract::ATP-binding cassette (ABC) transporters are a huge family of ATP-dependent transmembrane proteins whose main function is exporting or importing substances or molecules through the cell membranes, plasma cell membrane, or inner membranes in organelles. They fulfill these functions by maintaining cell integrity, metabol...
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pub_type: 杂志文章,评审
doi:10.2174/1381612822666160810120359
更新日期:2016-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150820110153
更新日期:2015-01-01 00:00:00
abstract::Synaptic transmission through descending motor pathways to lumbar motoneurons and then to leg muscles is essential for walking in humans and rats. Spinal cord injury (SCI), even when incomplete, results in diminished transmission to motoneurons and very limited recovery of motor function. Neurotrophins have emerged as...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990378
更新日期:2013-01-01 00:00:00
abstract::Gene delivery, a process of introducing foreign functional nucleic acids into target cells, has proven to be a very promising tool for inducing specific gene expression in host cells. Many different technologies have been developed for efficient gene delivery. Among them, electroporation has been adopted in gene deliv...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666151027152121
更新日期:2015-01-01 00:00:00
abstract::Aberrant expression of chemokines and their receptors play causative roles in the pathophysiology of numerous autoimmune and inflammatory disease processes. Moreover, an integral step in HIV infection involves binding to chemokine receptors, and hence chemokines are intimately linked to HIV-related diseases. Therefore...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612023393233
更新日期:2002-01-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2018-01-01 00:00:00
abstract::Parkinson's disease (PD) is one of common neurodegenerative diseases, which shows motor symptoms including tremor, bradykinesia, rigidity and postural instability. It also involves non-motor symptoms such as cognitive impairment, mental manifestation, autonomic disorder and sensory disturbance. Although treatments to ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170710163731
更新日期:2017-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209787315639
更新日期:2009-01-01 00:00:00
abstract::The treatment of skin wounds represents an important research area due to the important physiological and aesthetic role of this tissue. During the last years, nanoparticles have emerged as important platforms to treat skin wounds. Silver, gold, and copper nanoparticles, as well as titanium and zinc oxide nanoparticle...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00
abstract::Many, if not all, chronic medical, neurodegenerative and neuroprogressive illnesses are characterised by chronic immune activation, oxidative and nitrosative stress (O&NS) and systemic inflammation. These factors, notably elevated pro-inflammatory cytokines, activate indoleamine 2,3-dioxygenase (IDO) leading to an upr...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666151215102420
更新日期:2016-01-01 00:00:00
abstract::Erectile dysfunction (ED) has multifactor pathogenesis, with neurological, vascular, endocrinological and psychogenic components described. However, about 50-85% of ED population report the presence of one or more comorbidities i.e. hypertension, diabetes, cardiovascular disease, dyslipidemia which all impair endothel...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2006-01-01 00:00:00
abstract::Transient left ventricular dysfunction in patients under emotional stress, also known as Takotsubo cardiomyopathy, has been recognized as a distinct clinical entity. Recent studies have supported the concept notion that the cardiovascular system is regulated by cortical modulation. A network consisting of the insular ...
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pub_type: 杂志文章,评审
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更新日期:2017-01-01 00:00:00
abstract::Vascular smooth muscle cells (VSMC) respond to arterial wall injury by intimal proliferation and play a key role in atherogenesis by proliferating and migrating excessively in response to repeated injury, such as hypertension and atherosclerosis. In contrast, fully differentiated, quiescent VSMC allow arterial vasodil...
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更新日期:2010-01-01 00:00:00
abstract:BACKGROUND:There are controversial results available about using angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) and the development of cancers or improvement of clinical outcomes. Studies reported that using ACEI/ARB may enhance the development of hepatocellular carcinoma (HCC...
journal_title:Current pharmaceutical design
pub_type: meta分析
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更新日期:2020-01-01 00:00:00
abstract::Asthma is an allergic disease that affects approximately 300 million people worldwide. Two of its phenotypes routinely assessed at the clinic include airway hyperresponsiveness and IgE production. They can be measured in a non-invasive manner and have been used for genetic studies. The genetic complexity of asthma and...
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更新日期:2016-01-01 00:00:00
abstract::Mechanical loading provides an anabolic stimulus for bone. More importantly, the mechanosensing apparatus in bone directs osteogenesis to where it is most needed for improving bone strength. The biological processes involved in bone mechanotransduction are poorly understood and further investigation of the molecular m...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2004-01-01 00:00:00