Targeting the Folate Receptor: Improving Efficacy in Inorganic Medicinal Chemistry.

abstract：:Glucagon-like peptide-1 (GLP-1) is an insulinotropic hormone secreted from endocrine cells in the gut mucosa in response to meal ingestion. It is an important incretin hormone; mice with a null mutation in the GLP-1 receptor gene develop glucose intolerance. In addition, it inhibits gastrointestinal secretion and moti...

journal_title：Current medicinal chemistry

authors： Holst JJ

更新日期：1999-11-01 00:00:00

abstract：:Resistance to quinolones and fluoroquinolones has been increasingly reported among human and veterinary isolates during the last three decades related to their wide clinical use. Until recently, the mechanisms of resistance to quinolones in Enterobacteriaceae were believed to be only chromosome-encoded, i.e. related t...

journal_title：Current medicinal chemistry

authors： Cattoir V,Nordmann P

更新日期：2009-01-01 00:00:00

abstract：:Nitric oxide (NO) is a diatomic free radical produced from L-arginine by constitutive and inducible nitric oxide synthase (cNOS and iNOS) in numerous mammalian cells and tissues. Nitric oxide (NO), superoxide (O2-) and their reaction product peroxynitrite (ONOO-) may be generated in excess during the host response aga...

journal_title：Current medicinal chemistry

authors： Conforti F,Menichini F

更新日期：2011-01-01 00:00:00

abstract：:Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This mini...

journal_title：Current medicinal chemistry

authors： Fabbrizzi P,Menchi G,Guarna A,Trabocchi A

更新日期：2014-01-01 00:00:00

abstract：:Chagas disease is an infectious tropical disease included within the group of neglected tropical diseases. Though historically endemic to Latin America, it has lately spread to high-income countries due to human migration. At present, there are only two available drugs, nifurtimox and benznidazole, approved for this t...

journal_title：Current medicinal chemistry

authors： Bellera CL,Alberca LN,Sbaraglini ML,Talevi A

更新日期：2020-01-01 00:00:00

abstract：:During past two decades, plant-derived bioactive compounds have been reported as novel therapeutic agents for prevention and/or mitigation of different human diseases such as cancer, inflammation, cardiovascular and neurodegenerative diseases. Hesperidin is known as one of the most common and bioactive constituents of...

journal_title：Current medicinal chemistry

authors： Ahmadi A,Shadboorestan A,Nabavi SF,Setzer WN,Nabavi SM

更新日期：2015-01-01 00:00:00

abstract：:Farnesylthiosalisylic acid (FTS) is a potent non-toxic anticancer drug that targets oncogenic and pathologically activated Ras. The mechanism of action of FTS is well understood. It interferes with the binding of activated Ras proteins to their escort chaperons and with Ras tethering to the plasma membrane. This agent...

journal_title：Current medicinal chemistry

authors： Mor A,Aizman E,Chapman J,Kloog Y

更新日期：2013-01-01 00:00:00

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...

journal_title：Current medicinal chemistry

authors： Yu S,Zhao G

更新日期：2012-01-01 00:00:00

abstract：:The aminocoumarin antibiotics novobiocin, clorobiocin and coumermycin A(1) are produced by different Streptomyces strains and are potent inhibitors of DNA gyrase. The biosynthetic gene clusters of all three antibiotics have been cloned and sequenced, and the function of most genes contained therein has been elucidated...

journal_title：Current medicinal chemistry

authors： Li SM,Heide L

更新日期：2005-01-01 00:00:00

abstract：:Drug repositioning is an important area of biomedical research. The drug repositioning studies have shifted to computational approaches. Large-scale perturbation databases, such as the Connectivity Map and the Library of Integrated Network-Based Cellular Signatures, contain a number of chemical-induced gene expression...

journal_title：Current medicinal chemistry

authors： Wang F,Lei X,Wu FX

更新日期：2020-01-01 00:00:00

abstract：:There is evidence that hyperglycemia results in the generation of reactive oxygen species, leading to oxidative stress in various tissues, including vascular system. An important link between oxidative stress, inflammatory response and insulin activity is now well established. The ability of antioxidants to protect ag...

journal_title：Current medicinal chemistry

authors： Nicolle E,Souard F,Faure P,Boumendjel A

更新日期：2011-01-01 00:00:00

abstract：:Over the last centuries, there were many important discoveries in medicine that were crucial for gaining a better understanding of several physiological processes. Molecular modelling techniques are powerful tools that have been successfully used to analyse and interface medicinal chemistry studies with electrochemica...

journal_title：Current medicinal chemistry

authors： Almeida MO,Maltarollo VG,de Toledo RA,Shim H,Santos MC,Honorio KM

更新日期：2014-01-01 00:00:00

abstract：:The clinical treatment of multifactorial pathologies (e.g. cancer, Alzheimer's disease, psychiatric disorders), is still a major challenge. Many researches have been published dealing with the design of multiple ligands, able to act at the same time towards several targets relevant for a given pathology. In the presen...

journal_title：Current medicinal chemistry

authors： Costantino L,Barlocco D

更新日期：2012-01-01 00:00:00

abstract：:Small interfering RNA (siRNA) constitutes an excellent way of knocking down genes. However, it requires the use of delivery systems to reach the target cells, especially to neuronal cells. Dendrimers are one of the most widely used synthetic nanocarriers for siRNA delivery. However, due to the complexity of the dendri...

journal_title：Current medicinal chemistry

authors： Pavan GM,Monteagudo S,Guerra J,Carrión B,Ocaña V,Rodríguez-Lopez J,Danani A,Pérez-Martínez FC,Ceña V

更新日期：2012-01-01 00:00:00

abstract：:Dendritic cells (DCs) play a central role in the establishment of tolerance/immunity, because they activate naïve T cells (TCs). Therefore, the pharmacological modulation of DCs has become a major field of interest in immunology. A large body of literature has arisen from the studies of DC biology during immunosuppres...

journal_title：Current medicinal chemistry

authors： Schlichting CL,Schareck WD,Nickel T,Weis M

更新日期：2005-01-01 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

authors： Wauthier V,Verbeeck RK,Calderon PB

更新日期：2007-01-01 00:00:00

abstract：:Metabolomics is playing an increasingly important role in plant science. It aims at the comprehensive analysis of the plant metabolome which consists both of primary and secondary metabolites. The goal of metabolomics is ultimately to identify and quantify this wide array of small molecules in biological samples. This...

journal_title：Current medicinal chemistry

authors： Wolfender JL,Rudaz S,Choi YH,Kim HK

更新日期：2013-01-01 00:00:00

abstract：:The non-steroidal anti-inflammatory drugs (NSAIDs) are diverse group of compounds used for the treatment of inflammation, since the introduction of acetylsalicylic acid in 1899. Traditional (first generation) NSAIDs exert antiinflammatory, analgesic, and antipyretic effects through the blockade of prostaglandin synthe...

journal_title：Current medicinal chemistry

authors： Chakraborti AK,Garg SK,Kumar R,Motiwala HF,Jadhavar PS

更新日期：2010-01-01 00:00:00

abstract：:Whilst knowledge of basic biology, diagnosis and prognosis of glioblastoma (GB - WHO grade IV) are steadily improving, advancements of therapy are discouragingly slow, with the only significant novelty during last ten years represented by introduction of temozolomide in chemotherapy. In order to analyze the current st...

journal_title：Current medicinal chemistry

authors： Frosina G

更新日期：2015-01-01 00:00:00

abstract：:Advanced enteropancreatic (EP) neuroendocrine tumors (NETs) can be treated with several different therapies, including chemotherapy, biotherapy, and locoregional treatments. Over the last few decades, impressive progress has been made in the biotherapy field. Three main druggable molecular targets have been studied an...

journal_title：Current medicinal chemistry

authors： Fazio N,Scarpa A,Falconi M

更新日期：2014-01-01 00:00:00

abstract：:The bryostatins, powerful protein kinase C (PKC) agonists, are a family of complex macrolactone natural products. They are originally isolated from the marine bryozoan Bugula neritina. So far tweenty bryostatins have been obtained naturally and exhibit a remarkable range of biological activities, including antineoplas...

journal_title：Current medicinal chemistry

authors： Ruan BF,Zhu HL

更新日期：2012-01-01 00:00:00

abstract：:Although the understanding the pathophysiology of atherogenesis and atherosclerosis progression has been one of the major goals of cardiovascular research during the last decades, the precise mechanisms underlying plaque destabilization are still unknown. The disruption of the plaque and the thrombosis in the lumen th...

journal_title：Current medicinal chemistry

authors： Cominacini L,Garbin U,Mozzini C,Stranieri C,Pasini A,Solani E,Tinelli IA,Pasini AF

更新日期：2015-01-01 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：: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

authors： Sui M,Zhang H,Fan W

更新日期：2011-01-01 00:00:00

abstract：:Inosine monophosphate dehydrogenase (IMPDH) catalyzes the conversion of IMP to XMP with the concomitant reduction of NAD to NADH. This reaction is the rate-limiting step in guanine nucleotide biosynthesis. IMPDH is a proven target for immunosuppressive, anticancer and antiviral chemotherapy, and may also be a target f...

journal_title：Current medicinal chemistry

authors： Hedstrom L

更新日期：1999-07-01 00:00:00

abstract：:Photodynamic therapy (PDT) is a novel medical technique involving three key components: light, a photosensitizer molecule and molecular oxygen, which are essential to achieve the therapeutic effect. There has been great interest in the use of PDT in the treatment of many cancers and skin disorders. Upon irradiation wi...

journal_title：Current medicinal chemistry

authors： Skupin-Mrugalska P,Sobotta L,Kucinska M,Murias M,Mielcarek J,Düzgüneş N

更新日期：2014-01-01 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

authors： Vincenzi M,Leone M

更新日期：2020-12-28 00:00:00

abstract：:The hemostatic system comprises platelet aggregation, coagulation and fibrinolysis also termed primary, secondary and tertiary hemostasis. From the platelet transcriptome 6000 mRNA species and represent receptors, ion channels, signalling molecules, kinases, phosphatases, and structural, metabolic and regulatory prote...

journal_title：Current medicinal chemistry

authors： Stassen JM,Arnout J,Deckmyn H

更新日期：2004-09-01 00:00:00

abstract：:Sulfonyl group-containing compounds constitute an important class of therapeutical agents in medicinal chemistry presumably because of the tense chemical structure and functionality of the sulfonyl, which could not only form hydrogen bonding interactions with active site residues of biological targets but also, as inc...

journal_title：Current medicinal chemistry

authors： Chen X,Hussain S,Parveen S,Zhang S,Yang Y,Zhu C

更新日期：2012-01-01 00:00:00

abstract：:Protein p53 is a key player in mitochondrial mediated apoptotic cell death and excess p53 activity has been implicated in many disease states such athrosclerosis, diabetes, osteoarthritis, Alzheimer's disease, Parkinson's disease, Huntington's disease, AIDS, P. falciparum and S. typhimurium infections. Thus, chemical ...

journal_title：Current medicinal chemistry

authors： Nayak SK,Panesar PS,Kumar H

更新日期：2009-01-01 00:00:00