Assessing structure, function and druggability of major inhibitory neurotransmitter gamma-aminobutyrate symporter subtypes.

abstract：:Breakdown of glucose under physiological conditions gives rise to glucose degradation products (GDPs). GDPs are also formed during heat sterilization of glucose-containing peritoneal dialysis fluids (PD-fluids). In PD-fluids GDPs have been shown in many different in vitro assays to be responsible for adverse effects s...

journal_title：Current medicinal chemistry

authors： Ortiz A,Wieslander A,Linden T,Santamaria B,Sanz A,Justo P,Sanchez-Niño MD,Benito A,Kjellstrand P

更新日期：2006-01-01 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：: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

authors： Bjørklund G,Dadar M,Aaseth J,Chirumbolo S

更新日期：2020-01-01 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:The incidence of pancreatic cancer (PC) is rising in parallel with the deaths caused by this malignant disease largely due to limited improvement in current treatment strategies. In spite of aggressive PC research, for the past three decades, there has been no significant improvement in the five-year surviva...

journal_title：Current medicinal chemistry

authors： Mohammed A,Janakiram NB,Madka V,Li M,Asch AS,Rao CV

更新日期：2018-01-01 00:00:00

abstract：:Glutamate carboxypeptidase II (GCPII) and its splice variants, paralogs and human homologs represent a family of proteins with diverse tissue distribution, cellular localization and largely unknown function which have been explored only recently. While GCPII itself has been thoroughly studied from different perspectiv...

journal_title：Current medicinal chemistry

authors： Hlouchová K,Navrátil V,Tykvart J,Sácha P,Konvalinka J

更新日期：2012-01-01 00:00:00

abstract：:Flavonoids are natural plant-derived polyphenolic compounds with various biological properties particularly in the cardiovascular system, including antiatherogenic, antioxidant, vasodilation, antihypertensive, and antiplatelet activities. These biological properties have been evaluated in several experimental and clin...

journal_title：Current medicinal chemistry

authors： Almeida Rezende B,Pereira AC,Cortes SF,Lemos VS

更新日期：2016-01-01 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

authors： Dash A,Das T,Knapp FFR

更新日期：2020-01-01 00:00:00

abstract：:Cervical spondylotic myelopathy (CSM) is a very common and debilitating disease; however, its underlying pathocellular process remains uncertain. Attempts have been made to reproduce CSM in experimental animal models in order to deepen the knowledge on the molecular pathobiology of this disease. The up-to-date observa...

journal_title：Current medicinal chemistry

authors： Karadimas SK,Gialeli CH,Klironomos G,Tzanakakis GN,Panagiotopoulos E,Karamanos NK,Gatzounis G

更新日期：2010-01-01 00:00:00

abstract：:Potent enzyme inhibitors have long been recognized as powerful tools for assessing the physiological roles of enzymes and have led to the therapeutic drugs able to modulate their activities in vivo. However, to be valuable tools such inhibitors should be selective so that they do not interfere with other members of th...

journal_title：Current medicinal chemistry

authors： Batra S,Srinivasan T,Rastogi SK,Kundu B

更新日期：2002-02-01 00:00:00

abstract：:G protein-coupled receptor (GPCR) (also known as seven-transmembrane domain receptor) superfamily represents the largest protein family in the human genome. These receptors respond to various physiological ligands such as photons, odors, pheromones, hormones, ions, and small molecules including amines, amino acids to ...

journal_title：Current medicinal chemistry

authors： Yonezawa T,Kurata R,Yoshida K,Murayama MA,Cui X,Hasegawa A

更新日期：2013-01-01 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：: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：: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

authors： Curtin M,Glaser K

更新日期：2003-11-01 00:00:00

abstract：:DNA mutation is a very important step in carcinogenesis and elevated levels of oxidative DNA damage have been monitored in a variety of tumors. The discovery of the role of free radicals in cancer has led to a new medical approach. Minimizing oxidative damage may be a significant advance in the prevention or treatment...

journal_title：Current medicinal chemistry

authors： Tekiner-Gulbas B,Westwell AD,Suzen S

更新日期：2013-01-01 00:00:00

abstract：:The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming t...

journal_title：Current medicinal chemistry

authors： Kalász H,Antal I

更新日期：2006-01-01 00:00:00

abstract：:It is well accepted that inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, is one of high risk factors for colorectal cancer (CRC). This supports the notion that inflammation plays a key role in cancer development. Epidemiologic studies have shown that vitamin D (Vit D) deficiency is ...

journal_title：Current medicinal chemistry

authors： Luan Z,Ma Y,Xin Y,Qian J,Wang H

更新日期：2017-01-01 00:00:00

abstract：:Natural products from symbiotic or commensal associations between marine invertebrate and microbial organisms show exceptional promise as pharmaceuticals in many therapeutic areas. An economic and sustainable global market supply due to difficulty of synthesis is cited as the main obstacle for exploitation of these ot...

journal_title：Current medicinal chemistry

authors： Dunlap WC,Jaspars M,Hranueli D,Battershill CN,Perić-Concha N,Zucko J,Wright SH,Long PF

更新日期：2006-01-01 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：:Chagas disease is one of the most important endemic diseases in Latin America, caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, nifurtimox and benznidazole, are toxic and present severe side effects. The need of effective drugs, without adverse effects, has stimulated the search for new c...

journal_title：Current medicinal chemistry

authors： Salas CO,Faúndez M,Morello A,Maya JD,Tapia RA

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:The phosphodiesterase 10 (PDE10) family, identified in 1999, is mainly expressed in the brain, particularly in the striatum, within the medium spiny neurons, nucleus accumbens, and olfactory tubercle. Inhibitors of PDE10 (PDE10-Is) are a conceptually rational subject for medicinal chemistry with potential us...

journal_title：Current medicinal chemistry

authors： Zagorska A,Partyka A,Bucki A,Gawalskax A,Czopek A,Pawlowski M

更新日期：2018-01-01 00:00:00

abstract：:Transglutaminases (TGases) are enzymes which catalyze the cross linking of a glutaminyl residue of a protein/peptide substrate to a lysyl residue of a protein/peptide co-substrate with the formation of an N-gamma-(epsilon-L-glutamyl)-L-lysine [GGEL] cross link (isopeptidic bond) and the concomitant release of ammonia....

journal_title：Current medicinal chemistry

authors： Martin A,Romito G,Pepe I,De Vivo G,Merola MR,Limatola A,Gentile V

更新日期：2006-01-01 00:00:00

abstract：:The present paper summarizes the possible roles of frequent and unfavourable genetic variants in cerebrovascular disorders, such as stroke and leukoaraiosis. It also approaches the topic theoretically from functional and mathematical points of view, which can help make the accumulating data on genetic variants more un...

journal_title：Current medicinal chemistry

authors： Szolnoki Z

更新日期：2009-01-01 00:00:00

abstract：:Platinum complex-based chemotherapy is one of the major treatment options of many malignancies. Although severe side effects occur, and only a limited spectrum of tumors can be cured, Pt compounds are used in every second therapy scheme. Thus, many different drug design strategies have been employed for improving the ...

journal_title：Current medicinal chemistry

authors： Hartinger CG,Nazarov AA,Ashraf SM,Dyson PJ,Keppler BK

更新日期：2008-01-01 00:00:00

abstract：:The evidence seems to be growing in favor of the stem cell theory of cancer with the emergence of studies demonstrating the parallel mechanisms of self renewing pathways in stem cells and particular subsets of cancer cells. The finding of leukemia stem cells and subsequently breast cancer stem cells (BCSC) further sup...

journal_title：Current medicinal chemistry

authors： Nahas GR,Patel SA,Bliss SA,Rameshwar P

更新日期：2012-01-01 00:00:00

abstract：:Enteroviruses are members of picornavirus family which causes diverse and severe diseases in humans and animals. Clinical manifestations of enterovirus infections include fever, hand, foot, and mouth disease, and herpangina. Enteroviruses also cause potentially severe and life-threatening infections such as meningitis...

journal_title：Current medicinal chemistry

authors： Li C,Wang H,Shih SR,Chen TC,Li ML

更新日期：2007-01-01 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：:Recent results using animal models of inflammatory skin conditions have shown that blockers of the voltage-gated potassium channel, Kv1.3 hold great promise for clinical utility. Kv1.3 blockers act as immunosuppressants by modulating the various subsets of inflammatory T and B cells involved in autoimmune disorders. W...

journal_title：Current medicinal chemistry

authors： Nguyen W,Howard BL,Neale DS,Thompson PE,White PJ,Wulff H,Manallack DT

更新日期：2010-01-01 00:00:00

abstract：:MicroRNAs (miRNAs) translationally repressing their target messenger RNAs due to their gene-regulatory functions play an important but not unexpected role in a tumour development. More surprising are the findings that levels of various miRNAs are well correlated with presence of specific tumours and formation of metas...

journal_title：Current medicinal chemistry

authors： Pekarik V,Gumulec J,Masarik M,Kizek R,Adam V

更新日期：2013-01-01 00:00:00

abstract：:Anticancer drugs are often nonselective antiproliferative agents (cytotoxins) that preferentially kill dividing cells by attacking their DNA at some level. The lack of selectivity results in significant toxicity to noncancerous proliferating cells. These toxicities along with drug resistance exhibited by the solid tum...

journal_title：Current medicinal chemistry

authors： Singh Y,Palombo M,Sinko PJ

更新日期：2008-01-01 00:00:00