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：:Nature as a source of inspiration has been shown to have a great beneficial impact on the development of new computational methodologies. In this scenario, analyses of the interactions between a protein target and a ligand can be simulated by biologically inspired algorithms (BIAs). These algorithms mimic biological s...

journal_title：Current medicinal chemistry

authors： Heberlé G,de Azevedo WF Jr

更新日期：2011-01-01 00:00:00

abstract：:Natural products are regarded as vital key source of lead compounds for drug discovery due to their structural diversity and broad array of biological activities. Phenylpropanoid sucrose esters are naturally occurring compounds isolated from various plants and are structurally characterized by a sucrose core connected...

journal_title：Current medicinal chemistry

authors： Panda P,Appalashetti M,Judeh ZM

更新日期：2011-01-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are a large family of calcium-dependent zinc- containing endopeptidases, which are responsible for the tissue remodeling and degradation of the extracellular matrix (ECM), including collagens, elastins, gelatin, matrix glycoproteins, and proteoglycan. The inappropriate expression of th...

journal_title：Current medicinal chemistry

authors： Yadav RK,Gupta SP,Sharma PK,Patil VM

更新日期：2011-01-01 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：:We apply noval techniques, the Scaling Index Method (SIM), which reveals local topology of the structure, and the Minkowski Functionals (MF), which provide four global topological characteristics, to assess strength of the trabecular network of the human bone. We compare capabilities of these methods with the standard...

journal_title：Current medicinal chemistry

authors： Sidorenko I,Monetti R,Bauer J,Mueller D,Rummeny E,Eckstein F,Matsuura M,Lochmueller EM,Zysset P,Raeth C

更新日期：2011-01-01 00:00:00

abstract：:Borderline Personality Disorder (BPD) is a common disorder in psychiatric practice and drugs are widely used in its treatment, targeting symptom clusters, such as affective dysregulation, impulsive-behavioural dyscontrol, and cognitive-perceptual symptoms. In last period, a growing number of studies on pharmacological...

journal_title：Current medicinal chemistry

authors： Bellino S,Rinaldi C,Bozzatello P,Bogetto F

更新日期：2011-01-01 00:00:00

abstract：:Deregulation of kinase function has been implicated in several important diseases, including cancer, neurological and metabolic disorders. Because of their key role in causing disease, kinases have become one of the most intensively pursued classes of drug targets. To date, several monoclonal antibodies (mAbs) and sma...

journal_title：Current medicinal chemistry

authors： Cerchia L,de Franciscis V

更新日期：2011-01-01 00:00:00

abstract：:The neuropeptide substance P (SP) shows a widespread distribution in both the central and peripheral nervous systems and it is known that after binding to the neurokinin-1 (NK-1) receptors, SP regulates many biological functions in the central nervous system such as emotional behaviour, stress, depression, anxiety, em...

journal_title：Current medicinal chemistry

authors： Muñoz M,Coveñas R

更新日期：2011-01-01 00:00:00

abstract：:There is increasing evidence that statins, inhibitors of 3-hydroxyl-3-methylglutaryl coenzyme A reductase, can effectively be used not only in the treatment of hypercholesterolemia, but also in other human disorders; indeed, statins have strong anti-inflammatory and immunomodulatory effects, so that they can influence...

journal_title：Current medicinal chemistry

authors： Poggi A,Zocchi MR

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：:The Pim (provirus insertion site of Moloney murine leukemia virus) family of serine/threonine protein kinases possesses the fundamental characteristics critical for the biology of eukaryotes, in particular, survival and malignant transformation of cells. The members of this protein family (Pim-1 to Pim-3) are aberrant...

journal_title：Current medicinal chemistry

authors： Anizon F,Shtil AA,Danilenko VN,Moreau P

更新日期：2010-01-01 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：:Fulvestrant is a novel endocrine therapy for breast cancer, with a unique structure and mode of action. It binds competitively to the oestrogen receptor (ER), with high affinity, and downregulates ER by functional blockade and increased turnover. Fulvestrant has reached the clinic via extensive pre-clinical and clinic...

journal_title：Current medicinal chemistry

authors： Johnston SJ,Cheung KL

更新日期：2010-01-01 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：: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：:A BRAF somatic mutation at residue 600 of the BRAF protein (BRAFV600E) is highly prevalent in papillary thyroid carcinomas (PTC). This mutation occurs in approximately 44% (from 29% to 83%) of PTC depending on the different studies. BRAFV600E is almost always found in PTC with a papillary or a mixed follicular/papilla...

journal_title：Current medicinal chemistry

authors： Lassalle S,Hofman V,Ilie M,Butori C,Bozec A,Santini J,Vielh P,Hofman P

更新日期：2010-01-01 00:00:00

abstract：:Four different types of small RNAs functionally associated with gene silencing have been discovered in animals including small interfering RNAs (siRNAs), microRNAs (miRNAs), and Piwi-interacting RNAs (piRNAs). Experimental evidence suggests that miRNAs regulate the expression of more than 30% of protein-coding genes. ...

journal_title：Current medicinal chemistry

authors： Shah AA,Leidinger P,Blin N,Meese E

更新日期：2010-01-01 00:00:00

abstract：:Fabry disease (FD) is an X-linked glycosphingolipid storage disorder caused by deficient activity of the lysosomal enzyme alpha-galactosidase A. This leads to a progressive accumulation of globotriaosylceramide (Gb3) in the lysosomes of different cells and tissues, causing principally ventricular hypertrophy, renal fa...

journal_title：Current medicinal chemistry

authors： Caballero L,Climent V,Hernández-Romero D,Quintanilla MA,de la Morena G,Marín F

更新日期：2010-01-01 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：:This review focuses on the development of nanoparticle systems for antimicrobial drug delivery. Numerous antimicrobial drugs have been prescribed to kill or inhibit the growth of microbes such as bacteria, fungi and viruses. Even though the therapeutic efficacy of these drugs has been well established, inefficient del...

journal_title：Current medicinal chemistry

authors： Zhang L,Pornpattananangku D,Hu CM,Huang CM

更新日期：2010-01-01 00:00:00

abstract：:Glucocorticoids (GC) play a fundamental role in controlling physiologic homeostasis and, when present in excess, can have a detrimental impact on glucose control, blood pressure and lipid levels. The oxidoreductase 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) mainly catalyzes the intracellular regeneration...

journal_title：Current medicinal chemistry

authors： Ge R,Huang Y,Liang G,Li X

更新日期：2010-01-01 00:00:00

abstract：:During this past decade, science and engineering have seen a rapid increase in interest for nanoscale materials with dimensions less than 100 nm, which lie in the intermediate state between atoms and bulk (solid) materials. Their attributes are significantly altered relative to the corresponding bulk materials as they...

journal_title：Current medicinal chemistry

authors： Banerjee R,Katsenovich Y,Lagos L,McIintosh M,Zhang X,Li CZ

更新日期：2010-01-01 00:00:00

abstract：:Various human tumors preferentially metastasize by lymphatic route and lymphovascular invasion predicts lymph node metastasis. In this review article, we will summarize recent literature data concerning lymphangiogenesis, focusing on tumor lymphangiogenesis. In detail, we try to answer some important questions related...

journal_title：Current medicinal chemistry

authors： Raica M,Ribatti D

更新日期：2010-01-01 00:00:00

abstract：:Osteoporosis is characterized by reduced bone mass and structural deterioration of bone tissue leading to enhanced bone fragility and a consequent increase in fracture risk. Bone loss further increases in postmenopausal women when the ovaries stop making estrogens. Women undergoing treatment for osteoporosis require l...

journal_title：Current medicinal chemistry

authors： Bitto A,Polito F,Squadrito F,Marini H,D'Anna R,Irrera N,Minutoli L,Granese R,Altavilla D

更新日期：2010-01-01 00:00:00

abstract：:The role of MRI in the armory of diagnostic modalities for the medicine of the forthcoming years largely depends on how chemistry will provide advanced tools to meet the medical needs. This review aims at outlining the most innovative approaches that have been undertaken in the recent history of MRI contrast agents fo...

journal_title：Current medicinal chemistry

authors： Terreno E,Dastrù W,Delli Castelli D,Gianolio E,Geninatti Crich S,Longo D,Aime S

更新日期：2010-01-01 00:00:00

abstract：:Molecular recognition and ligand binding involving proteins underlie the most important life processes within the cell, such as substrate transport, catalysis, signal transmission, receptor trafficking, gene regulation, switching on and off of biochemical pathways. Despite recent successes in predicting the structures...

journal_title：Current medicinal chemistry

authors： Morra G,Genoni A,Neves MA,Merz KM Jr,Colombo G

更新日期：2010-01-01 00:00:00

abstract：:Receptor-binding peptides have attracted an enormous interest in targeting molecules for the development of tumour specific radiopharmaceutical compounds. The overexpression of many receptors on human tumour makes such peptide-ligands attractive agents for diagnostic imaging and therapy of cancers. The use of solid-ph...

journal_title：Current medicinal chemistry

authors： Bolzati C,Refosco F,Marchiani A,Ruzza P

更新日期：2010-01-01 00:00:00

abstract：:gamma-Amino butyric acid is an extremely important inhibitory neurotransmitter in the mammalian central nervous system and is essential for the overall balance between neuronal excitation and inhibition. It is well documented that GABA deficiency is associated with several important neurological disorders such as Hunt...

journal_title：Current medicinal chemistry

authors： Gajcy K,Lochyński S,Librowski T

更新日期：2010-01-01 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：:Protein C is a vitamin K-dependent anticoagulant serine protease zymogen in plasma which upon activation by the thrombin-thrombomodulin complex down-regulates the coagulation cascade by degrading cofactors Va and VIIIa by limited proteolysis. In addition to its anticoagulant function, activated protein C (APC) also bi...

journal_title：Current medicinal chemistry

authors： Rezaie AR

更新日期：2010-01-01 00:00:00

abstract：:Adenosine is an important autocoid, exerting its physiological effects on the human body by activation of four different G-protein-coupled-receptors (GPCRs) classified as A(1), A(2A), A(2B), and A(3). These receptors are coupled to secondary messenger systems including adenylate cyclase, inositol phosphate metabolism,...

journal_title：Current medicinal chemistry

authors： Romagnoli R,Baraldi PG,Tabrizi MA,Gessi S,Borea PA,Merighi S

更新日期：2010-01-01 00:00:00

abstract：:The human body is composed of 60 trillion cells, which have their origin in a fertilized egg. During development, the potential of a cell or tissue can be achieved by environmental manipulation. Then, what molecular determinants underlie or accompany the potential of the cells? To obtain a broader understanding of the...

journal_title：Current medicinal chemistry

authors： Toyoda M,Hamatani T,Okada H,Matsumoto K,Saito H,Umezawa A

更新日期：2010-01-01 00:00:00

abstract：:Ornithine transcarbamylase (OTC; EC 2.1.3.3) is a one-carbon-unit transferring enzyme that synthesizes citrulline using ornithine and carbamoylphosphate as substrates. It is involved in the metabolic transformation of arginine and proline, and it participates in the urea cycle in vertebrates and in the formation of pu...

journal_title：Current medicinal chemistry

authors： Díaz-Muñoz M,Hernández-Muñoz R

更新日期：2010-01-01 00:00:00

abstract：:Cellular signaling is regulated by several biochemical reactions, whose dynamics depends on changes in the fluxes of specific ligands through the containment barriers that are the biological membranes. The regulation of this complex dynamic equilibrium is mainly due to the activity of border proteins, that must be abl...

journal_title：Current medicinal chemistry

authors： Dainese E,Oddi S,Maccarrone M

更新日期：2010-01-01 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：:Novel molecular genetic approaches, at genome-scale in different species allowed characterizing genes that have undergone recent selection. The interest in this research field is not limited to the natural curiosity about our evolutionary past, but it is also to identify novel susceptibility genes for neuropsychiatic ...

journal_title：Current medicinal chemistry

authors： Moalic JM,Le Strat Y,Lepagnol-Bestel AM,Ramoz N,Loe-Mie Y,Maussion G,Gorwood P,Simonneau M

更新日期：2010-01-01 00:00:00

abstract：:Although the assortment of antifungal drugs is broad, the most commonly used agents have major drawbacks. Toxicity, serious side effects or the emergence of drug resistance are amongst them. New drugs and drug candidates under clinical trials do not guarantee better pharmacological parameters. These new medicines may ...

journal_title：Current medicinal chemistry

authors： Musiol R,Serda M,Hensel-Bielowka S,Polanski J

更新日期：2010-01-01 00:00:00

abstract：:The importance of organometallics can be noticed by their presence in all life organisms. The most known natural organometallic molecule is vitamin B12, a porphyrin containing a cobalt atom, useful for several enzymatic transformations. Based on the remarkable properties of this class of compounds, a new area of medic...

journal_title：Current medicinal chemistry

authors： Chavain N,Biot C

更新日期：2010-01-01 00:00:00

abstract：:Polyphenolic molecules produced by higher plants in response to biotic and abiotic stresses exert numerous effects on tumorigenic cell transformation, and on tumor cells in vitro and in vivo, and may interact with conventional anti-tumor therapies. In the present review, we collected and critically discussed data on: ...

journal_title：Current medicinal chemistry

authors： Korkina LG,De Luca C,Kostyuk VA,Pastore S

更新日期：2009-01-01 00:00:00