Strategies for efficient lead structure discovery from natural products.

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：:Mitochondria are cytoplasmic double-membraned organelles that are involved in a myriad of key cellular regulatory processes. The loss of mitochondrial function is related to the pathogenesis of several human diseases. Over the last decades, an increasing number of studies have shown that dietary polyphenols can regula...

journal_title：Current medicinal chemistry

authors： Teixeira J,Chavarria D,Borges F,Wojtczak L,Wieckowski MR,Karkucinska-Wieckowska A,Oliveira PJ

更新日期：2019-01-01 00:00:00

abstract：:The study of iron chelators as anti-tumor agents is still in its infancy. Iron is important for cellular proliferation and this is demonstrated by observations that iron-depletion results in cell cycle arrest and also apoptosis. In addition, many iron chelators are known to inhibit ribonucleotide reductase, the iron-c...

journal_title：Current medicinal chemistry

authors： Yu Y,Gutierrez E,Kovacevic Z,Saletta F,Obeidy P,Suryo Rahmanto Y,Richardson DR

更新日期：2012-01-01 00:00:00

abstract：:The blood-brain barrier (BBB) impedes the influx of intravascular compounds from the blood to the brain. The elements composing the BBB are endothelial cells, pericytes and the end-feet of astrocytes. Among them, the endothelial cell barrier line is the most critical for preventing toxic substances from entering the b...

journal_title：Current medicinal chemistry

authors： Ueno M

更新日期：2007-01-01 00:00:00

abstract：:Hyperlipidemia is characterized by abnormally increased plasma of any or all lipids and /or lipoproteins and is a confirmed risk factor for the formation of atherosclerosis. Inflammation plays a crucial role in the formation and progression of atherosclerosis and consequently on cardiovascular diseases. Nowadays, the ...

journal_title：Current medicinal chemistry

authors： Papapanagiotou A,Siasos G,Kassi E,Gargalionis AN,Papavassiliou AG

更新日期：2015-01-01 00:00:00

abstract：:With the recent market approval of Pitolisant (Wakix®), the interest in clinical application for novel multifunctional histamine H3 receptor antagonists has clearly increased. Several combinations of different H3R pharmacophores with pharmacophoric elements of other G-protein coupled receptors, transporters or enzymes...

journal_title：Current medicinal chemistry

authors： Szczepańska K,Kuder KJ,Kieć-Kononowicz K

更新日期：2020-08-05 00:00:00

abstract：:A dramatical decline in human male reproductive function has been reported for the past 20 years. Many recent epidemiological, clinical and experimental findings suggest that the reproductive dysfunction could result from prenatal and neonatal chemical compound exposure. Even if numerous studies argue for a relationsh...

journal_title：Current medicinal chemistry

authors： Gilleron J,Malassiné A,Carette D,Segretain D,Pointis G

更新日期：2011-01-01 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

authors： Rochais C,Rault S,Dallemagne P

更新日期：2010-01-01 00:00:00

abstract：:T helper (Th) cells belong to the adaptive immune system and provide an effective and antigen-specific means of host protection. Th17 cells are a subset of Th cells, characterized by the production of the inflammatory cytokines interleukin (IL)-17A (IL-17A) and IL-17F, which bind to a receptor complex comprised of IL-...

journal_title：Current medicinal chemistry

authors： Ghali JR,Holdsworth SR,Kitching AR

更新日期：2015-01-01 00:00:00

abstract：:In their structural multiplicity and in the extent to which they occur in nature the derivatives of benzofuran are significantly lesser than the isoelectronic analogue indoles. However, these heterocyclic compounds show a variety of pharmacological properties, and change of their structure offers a high degree of dive...

journal_title：Current medicinal chemistry

authors： De Luca L,Nieddu G,Porcheddu A,Giacomelli G

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:Immunomodulation is one of the significant therapeutic strategies. It includes both stimulation and suppression of the immune system by a variety of substances called immunomodulators, designed to regulate the immune response of the organism against infections of varying etiology. An example of such a substa...

journal_title：Current medicinal chemistry

authors： Siebert A,Gensicka-Kowalewska M,Cholewinski G,Dzierzbicka K

更新日期：2017-11-17 00:00:00

abstract：:Kit is a growth factor receptor of the type III tyrosine kinase family, whose gain-of-function mutations have been identified as driving causes of different kinds of tumours. It thus represents a viable drug target, and the development of Kit inhibitors has been shown to be a promising therapeutic concept. This review...

journal_title：Current medicinal chemistry

authors： Sartini S,Dario B,Morelli M,Da Settimo F,La Motta C

更新日期：2011-01-01 00:00:00

abstract：:Modification of cysteine (Cys) residues in proteins, due to (i) the participation of the thiol moiety of this amino acid in oxido-reductions reactions; (ii) its ability to strongly coordinate transition metal ions; or (iii) its nucleophilic nature and facile reaction with electrophiles, may be of critical importance f...

journal_title：Current medicinal chemistry

authors： Scozzafava A,Casini A,Supuran CT

更新日期：2002-06-01 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

authors： Poggi A,Catellani S,Fenoglio D,Borsellino G,Battistini L,Zocchi MR

更新日期：2007-01-01 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：:Mast cells are potent effectors playing a key role in IgE-associated hypersensitivity reactions, allergic disorders, inflammation and protective immune responses. Mast cell development in vivo occurs mainly in non-hematopoietic microenvironments and increased mast cell numbers can be seen in various inflammatory disea...

journal_title：Current medicinal chemistry

authors： Hu ZQ,Zhao WH,Shimamura T

更新日期：2007-01-01 00:00:00

abstract：:Glycosaminoglycans, highly charged polycarboxylated, polysulfated polysaccharides, are an important class of therapeutic agents and investigational drug candidates. Heparin has been widely used as a clinical anticoagulant for over 60 years. Low molecular weight heparins have begun to displace heparin and recently a sy...

journal_title：Current medicinal chemistry

authors： Karst NA,Linhardt RJ

更新日期：2003-10-01 00:00:00

abstract：:The transport of organic and inorganic molecules, along with inorganic ions across the plasma membrane results in chemical fluxes that reflect the cellular function in healthy and diseased states. Measurement of these chemical fluxes enables the characterization of protein function and transporter stoichiometry, chara...

journal_title：Current medicinal chemistry

authors： Messerli MA,Sarkar A

更新日期：2019-05-06 00:00:00

abstract：:From the discovery of Endothelial Progenitor Cells (EPC), these bone marrowderived precursors have been placed as crucial mediators of the endothelial repair. Accordingly, altered levels and function of EPC have been found in different scenarios of CV risk. Despite the fact that EPC exhibit important characteristics w...

journal_title：Current medicinal chemistry

authors： Rodríguez-Carrio J,López P,Suárez A

更新日期：2018-01-01 00:00:00

abstract：:Rapid innovations in nanomedicine have increased the likelihood that engineered nanomaterials will eventually come in contact with humans and the environment. The advent of nanotechnology has created strong interest in many fields such as biomedical sciences and engineering field. Central to any significant advances i...

journal_title：Current medicinal chemistry

authors： Subbiah R,Veerapandian M,Yun KS

更新日期：2010-01-01 00:00:00

abstract：:The COVID-19 pandemic has had catastrophic Global effects on financial markets, jobs and peoples' lives. Future prevention/therapy of COVID-19 will rely heavily on vaccine development and attempts to repurpose drugs previously used for other microbial diseases. Little attention, however, has been paid to possible diff...

journal_title：Current medicinal chemistry

authors： Ratcliffe NA,Castro HC,Paixão IC,Mello CB

更新日期：2020-10-27 00:00:00

abstract：:Akuammiline alkaloids are a family of monoterpene indole alkaloids of renewed medicinal interest. These bases act as ligands for a heterogeneous group of molecular targets and, consequently, display a wide variety of pharmacological activities. For example, pseudoakuammigine (2) exhibits opioid activity in vivo, echit...

journal_title：Current medicinal chemistry

authors： Ramírez A,García-Rubio S

更新日期：2003-09-01 00:00:00

abstract：:Normal somatic stem cells (SC) are naturally resistant to chemotherapeutic agents due to their expression of various membrane transporter molecules (such as MDR-1), detoxifying enzymes and DNA repair proteins. In addition, they also have a slow rate of cell turnover and therefore escape from chemotherapeutic agents th...

journal_title：Current medicinal chemistry

authors： Gangemi R,Paleari L,Orengo AM,Cesario A,Chessa L,Ferrini S,Russo P

更新日期：2009-01-01 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

authors： Iles RA

更新日期：2008-01-01 00:00:00

abstract：:Artificial intelligence methods, in particular, machine learning, has been playing a pivotal role in drug development, from structural design to clinical trial. This approach is harnessing the impact of computer-aided drug discovery thanks to large available data sets for drug candidates and its new and complex manner...

journal_title：Current medicinal chemistry

authors： Musella S,Verna G,Fasano A,Di Micco S

更新日期：2020-11-11 00:00:00

abstract：:The discovery of anandamide as an endogenous ligand for the cannabinoid receptors has led to a resurgence of interest in the fatty acid amides. However, N-palmitoylethanolamine (PEA), a shorter and fully saturated analogue of anandamide, has been known since the fifties. This endogenous compound is a member of the N-a...

journal_title：Current medicinal chemistry

authors： Lambert DM,Vandevoorde S,Jonsson KO,Fowler CJ

更新日期：2002-03-01 00:00:00

abstract：:Inflammation plays a critical role in the atherosclerotic process in various vascular beds, starting from endothelial dysfunction and counting all stages of plaque development. The significant contribution of inflammation in the initiation and progression of atherosclerosis has been documented over many years but its ...

journal_title：Current medicinal chemistry

authors： Vavuranakis M,Kariori M,Vrachatis D,Siasos G,Kalogeras K,Bei E,Moldovan C,Lavda M,Aznaouridis K,Oikonomou E,Tousoulis D

更新日期：2015-01-01 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

authors： Sheng Y,Hu J,Shi J,Lee LJ

更新日期：2019-01-01 00:00:00

abstract：:Coumarins are of many different structures. They constitute an important class of pharmacological agents possessing a range of different physiological activities including anti-cancer, anti-oxidant, anti- inflammation, anti-HIV, anti-coagulant, anti-bacterial, analgesic and comparative immune-modulation. Recently, cou...

journal_title：Current medicinal chemistry

authors： Wu L,Wang X,Xu W,Farzaneh F,Xu R

更新日期：2009-01-01 00:00:00

abstract：:Reactive oxygen species (ROS) are widely believed to cause or aggravate several human pathologies such as neurodegenerative diseases, cancer, stroke and many other ailments. Antioxidants are assumed to counteract the harmful effects of ROS and therefore prevent or treat oxidative stress-related diseases. In this repor...

journal_title：Current medicinal chemistry

authors： Firuzi O,Miri R,Tavakkoli M,Saso L

更新日期：2011-01-01 00:00:00