Natural and synthetic naphthoquinones active against Trypanosoma cruzi: an initial step towards new drugs for Chagas disease.

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

authors： Crocenzi FA,Mottino AD,Roma MG

更新日期：2004-02-01 00:00:00

abstract：BACKGROUND:Monocyte chemoattractant protein-1 (MCP-1) is a member of the CC chemokine family that plays a key role in the inflammatory process. It has been broadly studied in the aspect of its role in obesity and diabetes related diseases. MCP-1 causes the infiltration of macrophages into obese adipose tissue via bindi...

journal_title：Current medicinal chemistry

authors： Czemplik M,Kulma A,Wang YF,Szopa J

更新日期：2017-01-01 00:00:00

abstract：:Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) infection has been a global challenge. The complicated forms of the Coronavirus Disease 2019 (COVID-19) can evolve to multiple-organ failure, including several coagulopathies related to a sudden worsening of respiratory status. This article aimed to review s...

journal_title：Current medicinal chemistry

authors： Pena ALB,Oliveira RA,Severo RG,Simões E Silva AC

更新日期：2020-10-05 00:00:00

abstract：:In recent years there has been a growing interest in computer-based screening. One of the driving forces has been the increased efficiency of protein crystallography leading to the real possibility of using structure-based design as a significant contributor to the discovery of novel ligands. In 1957 after 22 years of...

journal_title：Current medicinal chemistry

authors： Glen RC,Allen SC

更新日期：2003-05-01 00:00:00

abstract：:Obesity and metabolic syndrome represent major public health problems, and are the biggest preventable causes of death worldwide. Obesity is the leading risk factor for type 2 diabetes mellitus (T2DM), cardiovascular diseases and non-alcoholic fatty liver disease. Obesity-associated insulin resistance, which is charac...

journal_title：Current medicinal chemistry

authors： Panzhinskiy E,Ren J,Nair S

更新日期：2013-01-01 00:00:00

abstract：:Prothymosin alpha (ProTα) is a highly acidic polypeptide, ubiquitously expressed in almost all mammalian cells and tissues and consisting of 109 amino acids in humans. ProTα is known to act both, intracellularly, as an anti-apoptotic and proliferation mediator, and extracellularly, as a biologic response modifier medi...

journal_title：Current medicinal chemistry

authors： Karachaliou CE,Kalbacher H,Voelter W,Tsitsilonis OE,Livaniou E

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Steroid hormones belong to a group of low-molecular weight compounds which are responsible for maintenance of various body functions, thus, their accurate assessment is crucial for evaluation of biosynthetic defects. The development of reliable methods allowing disease diagnosis is essential to improve early...

journal_title：Current medicinal chemistry

authors： Kotłowska A,Szefer P

更新日期：2019-01-01 00:00:00

abstract：:Dimerization and oligomerization of G protein-coupled receptors (GPCRs), proposed almost 30 years ago, have crucial relevance for drug design. Indeed, formation of GPCR oligomers may affect the diversity and performance by which extracellular signals are transferred to G proteins in the process of receptor transductio...

journal_title：Current medicinal chemistry

authors： Kaczor AA,Selent J

更新日期：2011-01-01 00:00:00

abstract：:Acyclic nucleoside analogues bearing phosphonomethoxy residues in the side chain (ANP) attract much attention due to a very beneficial combination of biological properties. Intensive work of organic chemists during the last two decades resulted in a large panel of new compounds that were evaluated as potential antivir...

journal_title：Current medicinal chemistry

authors： Khandazhinskaya A,Yasko M,Shirokova E

更新日期：2006-01-01 00:00:00

abstract：:Both zinc and copper are essential minerals that are required for various cellular functions. Although these metals are essential, they can be toxic at excess amounts, especially in certain genetic disorders. Zinc and copper homeostasis results from a coordinated regulation by different proteins involved in uptake, ex...

journal_title：Current medicinal chemistry

authors： Cai L,Li XK,Song Y,Cherian MG

更新日期：2005-01-01 00:00:00

abstract：:Bicarbonate (HCO₃⁻) membrane transport systems are crucial players in the physiology of several tissues. The molecular basis of HCO₃⁻ membrane transport is of major physiological relevance since this ion is involved in the establishment of intracellular and extracellular ionic composition, osmolariy and pH. The membra...

journal_title：Current medicinal chemistry

authors： Bernardino RL,Jesus TT,Martins AD,Sousa M,Barros A,Cavaco JE,Socorro S,Alves MG,Oliveira PF

更新日期：2013-01-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are zinc-endopeptidases responsible for degradation of the extracellular matrix (ECM) components including basement membrane collagen, interstitial collagen, fibronectin, and various proteoglycans, during normal remodeling and repair processes. The turnover and remodeling of ECM must b...

journal_title：Current medicinal chemistry

authors： Oikonomidi S,Kostikas K,Tsilioni I,Tanou K,Gourgoulianis KI,Kiropoulos TS

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:Since Signal Transducer and Activator of Transcription 3 (STAT3) is a transcription factor which plays an important role in multiple aspects of cancer, including progression and migration, and it is constitutively activated in various human tumors, STAT3 inhibition has emerged as a validated strategy for the...

journal_title：Current medicinal chemistry

authors： Gelain A,Mori M,Meneghetti F,Villa S

更新日期：2019-01-01 00:00:00

abstract：:Developing suitable medicines for genetic diseases requires a detailed understanding of not only the pathways that cause the disease, but also the identification of the genetic components involved in disease manifestation. This article focuses on the complexities associated with ocular ciliopathies - a class of debili...

journal_title：Current medicinal chemistry

authors： Shivanna M,Anand M,Chakrabarti S,Khanna H

更新日期：2019-01-01 00:00:00

abstract：:Multitarget-directed ligands (MTDLs), an emerging and appealing drug discovery strategy, utilizing a single chemical entity to inhibit multitargets, was confirmed to be effective in reducing the likelihood of drug resistance, diminishing problems of dosing complexity, drug-drug interactions and toxicities, as well as ...

journal_title：Current medicinal chemistry

authors： Zhan P,Liu X

更新日期：2013-01-01 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

authors： Tu Q,Zhang Y,Liu R,Wang JC,Li L,Nie N,Liu A,Wang L,Liu W,Ren L,Wang X,Wang J

更新日期：2012-01-01 00:00:00

abstract：:ATP-sensitive K(+) channels (K(ATP)channels) regulate insulin secretion by coupling intracellular metabolic changes to excitability of the plasma membrane in pancreatic beta-cells. The channels are closed when extracellular glucose levels are elevated due to enhanced feature. By contrast, cardiac-type K(ATP) channels,...

journal_title：Current medicinal chemistry

authors： Kakei M

更新日期：2003-02-01 00:00:00

abstract：:Tumor necrosis factor (TNF) is a cytokine with well known anticancer properties and is being utilized as anticancer agent for the treatment of patients with locally advanced solid tumors. However, TNF role in cancer biology is debated. In fact, in spite of the wealth of evidence supporting its antitumor activity, the ...

journal_title：Current medicinal chemistry

authors： Bertazza L,Mocellin S

更新日期：2010-01-01 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

authors： Arévalo ÁST,Erices JI,Uribe DA,Howden J,Niechi I,Muñoz S,Martín RS,Monrás CAQ

更新日期：2017-01-01 00:00:00

abstract：:Dose-limiting toxicity to healthy tissues is among the major hurdles in anticancer treatment along with intrinsic or acquired multi-drug resistance. Development of small molecule inhibitors (SMI) specific for antiapoptotic Bcl-2 proteins is a novel approach in a way that these antagonists are aimed to interfere with s...

journal_title：Current medicinal chemistry

authors： Bodur C,Basaga H

更新日期：2012-01-01 00:00:00

abstract：:Differentiation therapy of acute promyelocytic leukemia with all-trans retinoic acid represents the most successful pharmacological therapy of acute myeloid leukemia (AML). Numerous studies demonstrate that drugs that inhibit mechanistic target of rapamycin (mTOR) and activate AMP-kinase (AMPK) have beneficial effects...

journal_title：Current medicinal chemistry

authors： Visnjic D,Dembitz V,Lalic H

更新日期：2019-01-01 00:00:00

abstract：AIMS:Salvianolic acid B (Sal B), one of the most active components of Danshen extracts, has beneficial roles in the prevention and treatment of cardiovascular diseases. However, the precise mechanism by which Sal B exerts its effects on vascular cells is unclear. We aimed to elucidate the effects of Sal B on vascular c...

journal_title：Current medicinal chemistry

authors： Lee HJ,Seo M,Lee EJ

更新日期：2014-01-01 00:00:00

abstract：:Synthetic compounds with a tri- and tetra-substituted imidazole scaffold are known as selective inhibitors of the p38 mitogen-activated protein (MAP) kinase responsible for proinflammatory cytokine release. The scope is to review the literature describing their design, synthesis and activity studies. To date a great p...

journal_title：Current medicinal chemistry

authors： Scior T,Domeyer DM,Cuanalo-Contreras K,Laufer SA

更新日期：2011-01-01 00:00:00

abstract：:The inhibition of protein degradation through the ubiquitin-proteasome pathway is a recently developed approach to cancer treatment which extends the range of cellular targets for chemotherapy. This therapeutic strategy is very interesting since the proteasomes carry out the regulated degradation of unnecessary or dam...

journal_title：Current medicinal chemistry

authors： Gilardini A,Marmiroli P,Cavaletti G

更新日期：2008-01-01 00:00:00

abstract：:The need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...

journal_title：Current medicinal chemistry

authors： Catafau AM,Bullich S

更新日期：2013-01-01 00:00:00

abstract：:Diabetic nephropathy (DN) is a major complication of diabetes and the leading cause of end-stage renal disease (ESRD). Approximately, one third of diabetic patients develop diabetic nephropathy. As diabetes and its associated metabolic diseases are becoming epidemic, DN is emerging as a major health threat to humans. ...

journal_title：Current medicinal chemistry

authors： Lin X,Tao L,Tang D

更新日期：2013-01-01 00:00:00

abstract：:Bioactivation of xenobiotics can, in certain circumstances, result in the formation of reactive electrophilic species. These reactive metabolites may covalently modify proteins and macromolecules and it has been suggested that protein modification is a key initial step in provoking idiosyncratic adverse drug reactions...

journal_title：Current medicinal chemistry

authors： Edwards PJ,Sturino C

更新日期：2011-01-01 00:00:00

abstract：:Ambient level of gamma -aminobutyric acid (GABA), the major inhibitory neurotransmitter of the brain is mediated by neuronal and glial GABA transporters (GATs), members of the sodium and chloride ion-dependent solute carrier family. The neuronal GABA transporter subtype (GAT-1) has already been proven to be the target...

journal_title：Current medicinal chemistry

authors： Kardos J,Palló A,Bencsura A,Simon A

更新日期：2010-01-01 00:00:00

abstract：:In the last decade much attention has been paid to the development of metabolically non-reversible dimeric or hybrid compounds, which combine two structural units of one or two lead compounds of interest for the treatment of Alzheimer's disease. As a consequence of their capability to simultaneously interact with two ...

journal_title：Current medicinal chemistry

authors： Muñoz-Torrero D,Camps P

更新日期：2006-01-01 00:00:00

abstract：:This review summarizes our knowledge of biochemical, biological and medical applications and properties of phosphinic acid compounds. Phosphinic acid compounds (phosphinates) are derivatives of phosphinic acid H2P(O)(OH). The major attention of this article is focused on applications of phosphinates of a pseudopeptide...

journal_title：Current medicinal chemistry

authors： Collinsová M,Jirácek J

更新日期：2000-06-01 00:00:00