Abstract:
:Raltegravir, the only drug targeting the integration step in HIV-1 life cycle, makes β-ketoenol integrase (IN) strand transfer inhibitor (STI) gain a definitive place in the treatment of HIV-1 infection. However, the emergence of viral strains resistant to β-ketoenol STI demands a continued effort toward the discovery of novel IN inhibitors interfering with HIV-1 IN in a mechanistically different manner. Polyphenols, among the most developed IN inhibitors, exhibit a different mechanism of action compared with β-ketoenol STI. Some of them exhibit strong IN inhibitory activity and anti-viral activity at nanomolar level and 1,5-DCQA has been in phase II clinical trial in China. It is undoubted that this kind of compounds are attractive candidates for future inhibitor design, as they should be effective against STI resistant viral strains and display synergistic effect when combined with the current existing STI. However, almost all reviews about IN inhibitors have been focused on β-ketoenol STI, while the thorough evolution and general structure-activity relationship (SAR) summaries of polyphenols as IN inhibitors had never been specially discussed. In this review, we provide a comprehensive report of the nearly twenty years development of polyphenols as IN inhibitors: summarizing general SAR and suggesting the orientation for further research. Compilation of such data will prove beneficial in developing a novel generation of IN inhibitors.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Yu S,Zhao Gdoi
10.2174/092986712803833236subject
Has Abstractpub_date
2012-01-01 00:00:00pages
5536-61issue
32eissn
0929-8673issn
1875-533Xpii
CMC-EPUB-20120827-4journal_volume
19pub_type
杂志文章,评审abstract::Among the members of the 5'-nucleotidase family, there is only one membrane-bound ectosolic isoenzyme. This esterase prefers AMP as substrate but can hydrolyze a number of purine and pyrimidine phosphorylated compounds, indicating that no evolutive pressure to develop a more restricted specificity was exerted on this ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867311320340007
更新日期:2013-01-01 00:00:00
abstract::The synthesis and biological evaluation of carbohydrate mimetics has begun to more clearly define the diverse roles of carbohydrates in nature. Often the strategy invoves the design and synthesis of glycosyltransferase and glycosidase inhibitors both as tools to elucidate the mechanism of action of these enzymes and a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:
更新日期:1999-02-01 00:00:00
abstract::Paclitaxel has been proven to be effective against different types of cancer. A delivery system loaded with paclitaxel at tumor site should provide a high local concentration of the drug detrimental to malignant cells, which prevents the re-growth and metastasis of tumor. In this review, paclitaxel formulations for sy...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043455981
更新日期:2004-02-01 00:00:00
abstract::Since its discovery in 1995 adiponectin has garnered considerable interest from the academic, clinical and biotech communities due to its proposed salutary anti-inflammatory, anti-diabetic, anti-atherogenic and cardioprotective properties. As a result our appreciation of adiponectin's structure and the importance of p...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712803833155
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Stimuli-responsive carriers are a class of drug delivery systems which can change their physicochemical properties and/or structural conformations in response to specific stimuli. Although passive and active drug targeting has proved to reduce the side effects to normal cells, controlled intracellular drug r...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170830102409
更新日期:2019-01-01 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::Mammalian ecto ADP-ribosyltransferases (ARTs) constitute a family of structurally related proteins expressed on the cell surface or secreted in the extracellular compartment. Using NAD+ as substrate, they transfer ADP-ribose groups onto target proteins. In contrast to intracellular poly(ADP-ribosyl)transferases (PARPs...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043455611
更新日期:2004-04-01 00:00:00
abstract::Studies on enzyme inhibition remain an important area of pharmaceutical research since these studies have led to the discoveries of drugs useful in a variety of physiological conditions. The enzyme inhibitors can interact with enzymes and block their activity towards natural substrates. Urease inhibitors have recently...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867023369853
更新日期:2002-07-01 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::The glomerulonephritides are a collection of separate diseases with differing pathogeneses that collectively are common and important causes of renal disease. Effective, non-toxic immunomodulatory treatments for glomerulonephritis are lacking. This review will focus on our understanding of the role of leukocytes in im...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708783503230
更新日期:2008-01-01 00:00:00
abstract::Bile formation is an osmotic process driven by the vectorial transport of actively transferred biliary components across the basolateral (sinusoidal) and apical (canalicular) hepatocyte membranes, the latter being the rate-limiting step of the overall blood-to-bile transfer. The ATP-binding cassette (ABC) superfamily ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043455918
更新日期:2004-02-01 00:00:00
abstract::In this review, we report the functionalization of textiles composed of nanoscale reactive materials in the treatment of wounds and skin diseases such as acne. In view of the growing demand for high-quality textiles, much research is focused on the creation of antimicrobial finishings for fabrics, in order to protect ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666171229141635
更新日期:2018-01-01 00:00:00
abstract::The alphavbeta3 receptor, which are members of the group of the cellular adhesion molecules (CAM), are heterodimeric transmembrane glycoprotein receptors involved in processes such as cell-cell and cell-matrix adhesion, cell migration and signaling. Integrin alphavbeta3 receptor is expressed on almost all cells origin...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867053363522
更新日期:2005-01-01 00:00:00
abstract::Drug resistance is one of the major obstacles limiting the success of cancer chemotherapy. Biological mechanisms contributing to drug resistance may be present de novo and related to inherent features or may be raised after exposure to anticancer drugs. In recent years, both clinical observations and experimental stud...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711797379348
更新日期:2011-01-01 00:00:00
abstract::Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708784638861
更新日期:2008-01-01 00:00:00
abstract::gammadelta T lymphocytes are involved in the defence from viral and mycobacterial infections; however they are also responsible for autoimmune reactions. Herein, we discuss the characteristics of these cells, focusing on the mechanism(s) underlying extravasation and tissue localization. We show that Vdelta1 and Vdelta...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707782793835
更新日期:2007-01-01 00:00:00
abstract::Coral-derived microorganisms have been a major focus of many research efforts on marine ecology in recent decades. Importantly, research on bioactive compounds from these diverse microorganisms, which include fungi and bacteria, has experienced an explosive growth during the past five years. This has unveiled the ecol...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867322666151006093755
更新日期:2015-01-01 00:00:00
abstract::The development of new drugs with potential therapeutic applications is one of the most complex and difficult process in the pharmaceutical industry. Millions of dollars and man-hours are devoted to the discovery of new therapeutical agents. As, the activity of a drug is the result of a multitude of factors such as bi...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867003375317
更新日期:2000-02-01 00:00:00
abstract::Thymosin Beta-4 (Tβ4) is known as a major pleiotropic actin-sequestering protein that is involved in tumorigenesis. Tβ4 is a water-soluble protein that has different promising clinical applications in the remodeling and ulcerated tissues repair following myocardial infarction, stroke, plasticity and neurovascular remo...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867326666190716125456
更新日期:2020-01-01 00:00:00
abstract::Ageing is an aggravating factor leading to alterations in the biotransformation of drugs, and therefore their therapeutic efficacy and safety. In this review we discuss the influence of ageing on drug metabolizing enzymes in male Wistar rats. We report that drug metabolizing enzymes can be affected by ageing either by...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986707780090981
更新日期:2007-01-01 00:00:00
abstract::Despite the protective role of diets rich in fruit plant polyphenols against some cancers and chronic degenerative and inflammatory diseases, insufficient emphasis has been placed on oral health. Numerous studies have aimed to ascertain the role of polyphenols in the prevention and treatment of oral diseases; however,...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712799945012
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Pollutants are diverse chemical entities, including gases such as ozone and particulate matter PM. PM contains toxic chemicals such as polycyclic aromatic hydrocarbons (PAHs). Some PAHs can induce strong oxidative stress under UVA exposure. Pollution aggravates some skin diseases such as atopy or eczema, but...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170918123907
更新日期:2018-01-01 00:00:00
abstract::Although it has become acceptable that neuroretinal cells are also affected in diabetes, vascular lesions continue to be considered as the hallmarks of diabetic retinopathy. Animal models are essential for the understanding and treatment of human diabetic retinopathy, and the mouse is intensively used as a model becau...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/09298673113209990028
更新日期:2013-01-01 00:00:00
abstract::Fourier-transform infrared (FT-IR) based mapping and imaging is a fast emerging technology which is being increasingly applied to investigate tissues in the high-throughput mode. The high resolution close to the cellular level, the possibility to determine the bio-distribution of molecules of interest (proteins, pepti...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986709787002664
更新日期:2009-01-01 00:00:00
abstract::Inosine 5'-monophosphate dehydrogenase (IMPDH) catalyzes the first committed step of guanosine 5'-monophosphate (GMP) biosynthesis, and thus regulates the guanine nucleotide pool, which in turn governs proliferation. Human IMPDHs are validated targets for immunosuppressive, antiviral and anticancer drugs, but as yet m...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711795590129
更新日期:2011-01-01 00:00:00
abstract::Fungal phytotoxins are natural secondary metabolites produced by plant pathogenic fungi during host-pathogen interactions. They have received considerable particular attention for elucidating disease etiology, and consequently to design strategies for disease control. Due to wide differences in their chemical structur...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170426152331
更新日期:2018-01-01 00:00:00
abstract::Sarcopenia, or age-related muscle decline, occurs in most organisms and burdens both human health and the healthcare system. As our population ages, additional options for treating sarcopenia are needed. Mitochondrial dysfunction is implicated in the onset of sarcopenia, so therapies directed at improving mitochondria...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867324666170801095850
更新日期:2018-01-01 00:00:00
abstract::For more than 20 years there has been increasing interest in the development of novel therapies to raise levels of high-density lipoprotein cholesterol (HDL-C). However, well publicized failures of recent clinical trials of agents that raise HDL-C levels have stimulated considerable controversy with regard to the pote...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867321666140414104130
更新日期:2014-01-01 00:00:00
abstract::The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse effects. Thus, entirely new interventions, addressing the underlying...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867325666181001112226
更新日期:2020-01-01 00:00:00
abstract::It is well-recognized that the majority of cancer-related deaths is attributed to metastasis, which can arise from virtually any type of tumor. Metastasis is a complex multistep process wherein cancer cells must break away from the primary tumor, intravasate into the circulatory or lymphatic systems, extravasate, prol...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867325666180522090842
更新日期:2019-01-01 00:00:00