Abstract:
:The peroxisome proliferator-activated receptor (PPAR) family of nuclear receptors, a set of three receptor sub-types encoded by distinct genes, function as lipid sensors to regulate a broad range of genes in many metabolically active tissues. Synthetic PPAR agonists have exhibited therapeutic benefits in treating diabetes and cardiovascular diseases. The discovery of PPAR-specific ligands has led to significant advancement in our understanding of the structure of these receptor proteins and the molecular mechanism of their ligand-dependent activation. Herein, we present both recent progress in the functional analysis of these orphan receptors and the confirmation of the PPARs as molecular targets for the development of new medicines to treat human metabolic disease.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Shearer BG,Hoekstra WJdoi
10.2174/0929867033368295subject
Has Abstractpub_date
2003-02-01 00:00:00pages
267-80issue
4eissn
0929-8673issn
1875-533Xjournal_volume
10pub_type
杂志文章,评审abstract::The focus of this review is the cellular internalisation mechanism of nanostructured systems (NSs) and their endosomal escape for targeted drug delivery. Endocytosis is a cellular process of internalisation of different molecules and foreign microorganisms. It is currently being studied for drug delivery through nanos...
journal_title:Current medicinal chemistry
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abstract::The transport mechanisms of ascorbic acid (AA) are described. The metabolism of AA and its function as an antioxidant are covered in some detail. Subsequently, indications for postoperative substitution are discussed. The supplementation of up to 300 mg of AA per day in postoperative intensive care unit patients durin...
journal_title:Current medicinal chemistry
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abstract::Fluoxetine is an antidepressant drug, a potent and specific inhibitor of serotonin reuptake (SSRI). Evidence suggests that being compared with tricyclic antidepressants, fluoxetine may cause significantly fewer anticholinergic, antihistaminergic and cardiotoxic side effects in the treatment of major depressive disorde...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:
更新日期:1998-10-01 00:00:00
abstract::Many non-cardiovascular drugs of common clinical use cause, as an unwanted accessory property, the prolongation of the cardiac repolarisation process, due to the block of the HERG (Human Ether-a-go-go Related Gene) potassium channel, responsible for the repolarising I(Kr) current. This delayed cardiac repolarisation p...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2004-10-01 00:00:00
abstract::Histone deacetylase inhibitors have generated significant interest as anti-cancer agents due to their ability to cause growth arrest, terminal differentiation and/ or apoptosis in carcinoma cells. Abbott entered this area after the serendipitous discovery of the biaryl hydroxamate A-161906 in a TGF beta mimetic screen...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867033456576
更新日期:2003-11-01 00:00:00
abstract::In healthy individuals, natural and adaptive immune responses are able to control virus entry into the host. In particular, CD8(+)-mediated cytotoxicity, sustained by the intervention of CD4+ cells, represents the major key event leading to virus eradication. On the other hand, viruses are able to evade from host immu...
journal_title:Current medicinal chemistry
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journal_title:Current medicinal chemistry
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更新日期:2016-01-01 00:00:00
abstract::Magnetic resonance imaging (MRI) contrast agents are utilized adjunctively to enhance the contrast between normal and abnormal structures on MRI scans. Along with the rapid evolution of the field has come a new appreciation for the medicinal chemistry of this unique class of metallopharmaceuticals. The efficacy of MRI...
journal_title:Current medicinal chemistry
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更新日期:2005-01-01 00:00:00
abstract::Drug-loaded nanoparticles have shown great potential in the study of carriers for disease-targeting drug delivery. Drug-loaded nanoparticles are excellent in keeping the drug in the systemic circulation for a prolonged period of time, introducing targeting molecules to improve targeting efficiency and to reduce side e...
journal_title:Current medicinal chemistry
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更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Smac mimetics (also known as IAP antagonist) are a new class of targeted drugs having a goal to suppress the IAPs, reestablishing the apoptotic pathways and inducing cancer cell death. Therefore, development of Smac mimetics was considered an attractive strategy for the development of new anticancer drugs. L...
journal_title:Current medicinal chemistry
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更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:COVID-19 has brought the world to its knees and there is an urgent need for new strategies to identify molecules capable of fighting the pandemic. During the last few decades NMR (Nuclear Magnetic Resonance) spectroscopy has emerged as an intriguing structural biology instrument in the antiviral drug discove...
journal_title:Current medicinal chemistry
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更新日期:2020-12-28 00:00:00
abstract::Chronic obstructive pulmonary disease (COPD) represents a heightened inflammatory response in the lung generally resulting from tobacco smoking-induced recruitment and activation of inflammatory cells and/or activation of lower airway structural cells. Several mediators can modulate activation and recruitment of these...
journal_title:Current medicinal chemistry
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更新日期:2020-08-19 00:00:00
abstract::Bone pain arising from secondary skeletal malignancy constitutes one of the most common types of chronic pain among patients with cancer which can lead to rapid deterioration of the quality of life. Radionuclide therapy using bone-seeking radiopharmaceuticals based on the concept of localization of the agent at bone m...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867326666190201142814
更新日期:2020-01-01 00:00:00
abstract::Numerous compounds with a benzothiazole scaffold that have been described in the literature show promising activities against several Gram-positive and Gramnegative bacteria, and also against Mycobacterium tuberculosis. Benzothiazole-based antibacterial compounds bind to different biological targets in bacterial cells...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666171009103327
更新日期:2018-01-01 00:00:00
abstract::Nuclear magnetic resonance spectroscopy has been exploited to study the metabolic characteristics (phenotype) of genetic disorders by taking advantage of some unique characteristics of the technique. The first application, metabolic profiling for diagnosis and therapeutic monitoring in vitro, demonstrates the exceptio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708783330719
更新日期:2008-01-01 00:00:00
abstract::Photodynamic therapy (PDT) involves the administration of a photosensitizer (PS) followed by illumination with visible light, leading to generation of reactive oxygen species. The mechanisms of resistance to PDT ascribed to the PS may be shared with the general mechanisms of drug resistance, and are related to altered...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711795843272
更新日期:2011-01-01 00:00:00
abstract::Small conductance Ca(2+)-activated K(+) (SK(Ca)) channels comprise an important subclass of K(+) channels. Selective blockade of SK(Ca) channels may find application in the therapy of myotonic muscular dystrophy, gastrointestinal dysmotilities, memory disorders, narcolepsy, and alcohol abuse. In the cyclophanes descri...
journal_title:Current medicinal chemistry
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更新日期:2008-01-01 00:00:00
abstract::This review presents a general overview of the subtype-selective dopamine receptor radioligands for in vivo imaging of dopamine receptor expression by positron emission tomography (PET). Besides the (11)C- and (18)F-labeled radioligands which are already in clinical use, a summary of subtype-selective radioligands whi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712802002518
更新日期:2012-01-01 00:00:00
abstract::Patients with peripheral arterial disease (PAD) suffer from increased cardiovascular morbidity and mortality. The ankle brachial index has been widely used as an easy tool to identify and stratify patients with PAD, however its predictive value remains limited. Higher levels of inflammatory and prothrombotic biomarker...
journal_title:Current medicinal chemistry
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doi:10.2174/092986712800492959
更新日期:2012-01-01 00:00:00
abstract::Virtual screening is an important means for lead compound discovery. The scoring function is the key to selecting hit compounds. Many scoring functions are currently available; however, there are no all-purpose scoring functions because different scoring functions tend to have conflicting results. Recently, neural net...
journal_title:Current medicinal chemistry
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更新日期:2020-05-26 00:00:00
abstract:BACKGROUND:In the last two decades, there have been significant technological advances in the early detection of brain tumors. However, no notable improvements have been observed in the treatment of Glioblastoma Multiforme (GBM), the most common brain neoplasm coupled with the worst prognosis. GBM is characterized by a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170303122241
更新日期:2017-01-01 00:00:00
abstract::Ion channel dysfunction has been identified as a contributor to symptom development and neurodegeneration in multiple sclerosis (MS). The molecular insights have been translated into new lines of research, with ion channel modulation now representing a therapeutic approach in MS. Studies of Na+ channel function have d...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867322666151029104452
更新日期:2015-01-01 00:00:00
abstract::Current strategies in pharmaceutical research comprise two methodologically different but complementary approaches for lead finding purposes, namely the random screening of compound libraries and the structure-based effort, commonly termed rational drug design. The structure-based approach is aimed to exploit 3D struc...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2000-09-01 00:00:00
abstract::Rutin (quercetin-3-O-rutinoside) is a multifunctional natural flavonoid glycoside with profound effects on the various cellular functions under pathological conditions. Due to the ability of rutin and/or its metabolites to cross the blood brain barrier, it has also been shown to modify the cognitive and various behavi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2016-01-01 00:00:00
abstract::β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their a...
journal_title:Current medicinal chemistry
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更新日期:2010-01-01 00:00:00
abstract::Lipoxygenases (LOXs) are non-heme iron containing dioxygenases involved in the oxygenation of polyunsaturated fatty acids (PUFAs) such as arachidonic acid (AA). Depending on the position of insertion of oxygen, LOXs are classified into 5-, 8-, 9-, 12- and 15-LOX. Among these, 5-LOX is the most predominant isoform asso...
journal_title:Current medicinal chemistry
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更新日期:2012-01-01 00:00:00
abstract::Systemic Lupus Erythematosus (SLE) is a chronic and relapsing heterogenous autoimmune disease that primarily affects women of reproductive age. Genetic and environmental risk factors are involved in the pathogenesis of SLE, and susceptibility genes have recently been identified. However, as gene therapy is far from cl...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867326666190404140658
更新日期:2020-01-01 00:00:00
abstract::Tuberculosis (TB) is the leading cause of mortality due to a single infectious agent. The currently used combination drug regimens produce cure rates that exceed 95%, given good patient adherence during the multiple months treatment period. However the recent surge in HIV infections and the synergy between HIV and TB ...
journal_title:Current medicinal chemistry
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更新日期:2008-01-01 00:00:00
abstract::There is a need for novel drugs for the treatment of infectious diseases, autoimmunity and cancer. Cyclic peptides constitute a class of compounds that have made crucial contributions to the treatment of certain diseases. Penicillin, Vancomycin, Cyclosporin, the Echinocandins and Bleomycin are well-known cyclic peptid...
journal_title:Current medicinal chemistry
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更新日期:2006-01-01 00:00:00
abstract::This investigation aims to evaluate strategies for an efficient selection of bioactive compounds from the multitude and biodiversity of the plant kingdom. Statistics prove natural products (NPs) as a source leading most consistently to successful development of new drugs. However, there are several reasons why the int...
journal_title:Current medicinal chemistry
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更新日期:2006-01-01 00:00:00