Melanin-concentrating hormone receptor 1 antagonists: a new perspective for the pharmacologic treatment of obesity.

abstract：:The efficacy of classical and molecular therapies in cancer is hampered by the occurrence of primary (intrinsic) and secondary (acquired) refractoriness of tumours to selected therapeutic regimens. Nevertheless, the increased knowledge of the genetic, molecular and metabolic mechanisms underlying cancer results in the...

journal_title：Current medicinal chemistry

authors： Rosa R,Monteleone F,Zambrano N,Bianco R

更新日期：2014-01-01 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：: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：: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：:Balance between excitatory glutamate and inhibitory GABA neurotransmitter is essential and critical for proper development and functioning of brain. GABAergic (gamma aminobutyric acid) and glutamatergic interneurons maintain excitability, integrity and synaptic plasticity. Several evidences implicated relative loss of...

journal_title：Current medicinal chemistry

authors： Purkayastha P,Malapati A,Yogeeswari P,Sriram D

更新日期：2015-05-04 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：BACKGROUND:Many pathways regarding healthy cells and/or linked to diseases onset and progression depend on large assemblies including multi-protein complexes. Protein-protein interactions may occur through a vast array of modules known as Protein Interaction Domains (PIDs). OBJECTIVE:This review concerns with PIDs rec...

journal_title：Current medicinal chemistry

authors： Vincenzi M,Mercurio FA,Leone M

更新日期：2020-01-01 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

abstract：BACKGROUND:Diabetic nephropathy (DN) is an important diabetic microvascular complication, and it is becoming the leading cause of end-stage renal disease worldwide. Unfortunately, there are no effective therapies to treat established DN. Therefore, new therapeutic targets are urgently required. Accumulating studies ind...

journal_title：Current medicinal chemistry

authors： Yang S,Han Y,Liu J,Song P,Xu X,Zhao L,Hu C,Xiao L,Liu F,Zhang H,Sun L

更新日期：2017-01-01 00:00:00

abstract：:Endothelial cells (ECs) play a pivotal role in physiological and altered tissue neovascularization. They face multiple morphological, biochemical and functional changes during the different phases of angiogenesis, under the regulation of a great number of proangiogenic and antiangiogenic signals, including soluble and...

journal_title：Current medicinal chemistry

authors： Munaron L,Fiorio Pla A

更新日期：2009-01-01 00:00:00

abstract：:Phosphonated nucleosides represent a promising alternative in the improvement of the biological activity of nucleoside analogues in antiviral and anticancer chemotherapy. The basic concept, the chemistry, the different structural modifications and their effects on the antiviral potency will be discussed in this review...

journal_title：Current medicinal chemistry

authors： Piperno A,Chiacchio MA,Iannazzo D,Romeo R

更新日期：2006-01-01 00:00:00

abstract：:Physalia physalis is a marine cnidarian from which high molecular weight toxins with hemolytic and neurotoxic effects have been isolated. In the present work, two novel toxins, PpV9.4 and PpV19.3 were purified from P. physalis by bioactive guideline isolation. It involved two steps of column chromatography, gel filtra...

journal_title：Current medicinal chemistry

authors： Diaz-Garcia CM,Fuentes-Silva D,Sanchez-Soto C,Domínguez-Pérez D,García-Delgado N,Varela C,Mendoza-Hernández G,Rodriguez-Romero A,Castaneda O,Hiriart M

更新日期：2012-01-01 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：:Advances in combinatorial chemistry, high-throughput screening, and molecular modeling have revolutionized the process of drug discovery in the pharmaceutical industry. Drug discovery efforts for the primary protozoal parasitic diseases of the developing world, malaria, leishmaniasis, and trypanosomiasis, have also be...

journal_title：Current medicinal chemistry

authors： Werbovetz KA

更新日期：2000-08-01 00:00:00

abstract：:Ten years elapsed since the discovery by Sanofi of SR141716A the first selective CB(1) cannabinoid receptor antagonist. Shortly after, Sanofi also reported the synthesis of the first selective CB(2) cannabinoid receptor antagonist, SR144528. Since these two milestones in the cannabinoid field, many other compounds, mo...

journal_title：Current medicinal chemistry

authors： Muccioli GG,Lambert DM

更新日期：2005-01-01 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：: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：:A comprehensive outline for understanding and recommending the therapeutic use of ozone in combination with established therapy in diseases characterized by a chronic oxidative stress is currently available. The view of the absolute ozone toxicity is incorrect, because it has been based either on lung or on studies pe...

journal_title：Current medicinal chemistry

authors： Zanardi I,Borrelli E,Valacchi G,Travagli V,Bocci V

更新日期：2016-01-01 00:00:00

abstract：:Chymase stored in mast cells activates matrix metalloproteinase (MMP)-9, which may relate to the progression of sinusoidal obstruction syndrome (SOS). We investigated the preventive effect of a chymase inhibitor, TY-51469, on monocrotaline-induced SOS in hamsters. Hamsters were orally administrated with a single dose ...

journal_title：Current medicinal chemistry

authors： Masubuchi S,Komeda K,Takai S,Jin D,Tashiro K,Li ZL,Otsuki Y,Okamura H,Hayashi M,Uchiyama K

更新日期：2013-01-01 00:00:00

abstract：:Sweat is an alternative biological matrix useful to detect drugs of abuse intake. It is produced by eccrine and apocrine glands originating in the skin dermis and terminating in secretory canals that flow into the skin surface and hair follicles. Since many years it has been demonstrated that endogenous and exogenous ...

journal_title：Current medicinal chemistry

authors： De Giovanni N,Fucci N

更新日期：2013-01-01 00:00:00

abstract：:Targeted therapy has been recently highlighted due to the reduction of side effects and improvement in overall efficacy and survival to different types of cancers. Considering the approval of many monoclonal antibodies in the last twenty years, cancer treatment can be accomplished by the combination of monoclonal anti...

journal_title：Current medicinal chemistry

authors： Petrilli R,Pinheiro DP,de Cássia Evangelista de Oliveira F,Galvão GF,Marques LGA,Lopez RFV,Pessoa C,Eloy JO

更新日期：2020-05-25 00:00:00

abstract：:The cellular response to DNA damage is critical for determining whether carcinogenesis, cell death or other deleterious biological effects will ensue. Numerous cellular enzymatic mechanisms can directly repair damaged DNA, or allow tolerance of DNA lesions, and thus reduce potential harmful effects. These processes in...

journal_title：Current medicinal chemistry

authors： Lieberman HB

更新日期：2008-01-01 00:00:00

abstract：:Characterization of liver-specific autoantigens has given a fresh impetus to research in the pathogenesis of autoimmune liver diseases, viral-triggered and drug-induced autoimmunity affecting the liver. Intriguing is the fact that most of the liver-specific autoantigens are enzymes of key importance for cell's homeost...

journal_title：Current medicinal chemistry

authors： Bogdanos DP,Dalekos GN

更新日期：2008-01-01 00:00:00

abstract：:Fibroblast growth factor receptor-4 (FGFR4) is a tyrosine kinase with a range of important physiological functions. However, it is also frequently mutated in various cancers and is now generating significant interest as a potential therapeutic target. Unfortunately, biochemical characterization of its role in disease,...

journal_title：Current medicinal chemistry

authors： Ho HK,Németh G,Ng YR,Pang E,Szántai-Kis C,Zsákai L,Breza N,Greff Z,Horváth Z,Pató J,Szabadkai I,Szokol B,Baska F,Őrfî L,Ullrich A,Kéri G,Chua BT

更新日期：2013-01-01 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：: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:Post-translational modification (PTM) crosstalk is a young research field. However, there is now evidence of the extraordinary characterization of the different proteoforms and their interactions in a biological environment that PTM crosstalk studies can describe. Besides gene expression and phosphorylation ...

journal_title：Current medicinal chemistry

authors： Hernandez-Valladares M,Wangen R,Berven FS,Guldbrandsen A

更新日期：2019-01-01 00:00:00

abstract：:Semicarbazide-sensitive amine-oxidase (SSAO) is present in various human tissues and in plasma. Oxidative deamination of short-chain aliphatic amines is catalyzed by this enzyme to afford the corresponding aldehydes, ammonia and hydrogen peroxide. Methylamine and aminoacetone have been recognized to be physiological s...

journal_title：Current medicinal chemistry

authors： Mátyus P,Dajka-Halász B,Földi A,Haider N,Barlocco D,Magyar K

更新日期：2004-05-01 00:00:00

abstract：:Over the years, natural products have shown success as antidiabetics in in vitro, in vivo studies and clinical trials. Because natural product-derived drugs are more affordable and effective with fewer side-effects compared to conventional therapies, pharmaceutical research is increasingly leaning towards the discover...

journal_title：Current medicinal chemistry

authors： Alam F,Islam MA,Kamal MA,Gan SH

更新日期：2018-01-01 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