Identification of enzyme inhibitors using combinatorial libraries.

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：: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：:Functioning of G protein-coupled receptors (GPCRs) is tightly linked to the membrane environment, but a molecular level understanding of the modulation of GPCR by membrane lipids is not available. However, specific receptor-lipid interactions as well as unspecific effects mediated by the bulk properties of the membran...

journal_title：Current medicinal chemistry

authors： Sadiq SK,Guixa-Gonzalez R,Dainese E,Pastor M,De Fabritiis G,Selent J

更新日期：2013-01-01 00:00:00

abstract：:Diabetic nephropathy (DN) is a major complication of diabetes and the leading cause of end-stage renal disease (ESRD). Approximately, one third of diabetic patients develop diabetic nephropathy. As diabetes and its associated metabolic diseases are becoming epidemic, DN is emerging as a major health threat to humans. ...

journal_title：Current medicinal chemistry

authors： Lin X,Tao L,Tang D

更新日期：2013-01-01 00:00:00

abstract：:Lipoxygenases (LOXs) are non-heme iron containing dioxygenases involved in the oxygenation of polyunsaturated fatty acids (PUFAs) such as arachidonic acid (AA). Depending on the position of insertion of oxygen, LOXs are classified into 5-, 8-, 9-, 12- and 15-LOX. Among these, 5-LOX is the most predominant isoform asso...

journal_title：Current medicinal chemistry

authors： Aparoy P,Reddy KK,Reddanna P

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Smac mimetics (also known as IAP antagonist) are a new class of targeted drugs having a goal to suppress the IAPs, reestablishing the apoptotic pathways and inducing cancer cell death. Therefore, development of Smac mimetics was considered an attractive strategy for the development of new anticancer drugs. L...

journal_title：Current medicinal chemistry

authors： Ali R,Singh S,Haq W

更新日期：2018-01-01 00:00:00

abstract：:Tuberculosis (TB) is the leading cause of mortality due to a single infectious agent. The currently used combination drug regimens produce cure rates that exceed 95%, given good patient adherence during the multiple months treatment period. However the recent surge in HIV infections and the synergy between HIV and TB ...

journal_title：Current medicinal chemistry

authors： Budha NR,Lee RE,Meibohm B

更新日期：2008-01-01 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：:Cholecystokinin (CCK) is an important neuro-intestinal peptide hormone produced by the enteroendocrine I-cells in the upper part of small intestine. Protein- and fat-enriched food plays an important role in triggering CCK secretion from the intestine. Carbohydrates stimulate only small amounts of CCK release. The CCK-...

journal_title：Current medicinal chemistry

authors： Wang HH,Portincasa P,Wang DQ

更新日期：2019-01-01 00:00:00

abstract：:Among naturally occurring isoflavones, soy isoflavones are an important class with various biological activities. Due to their phytoestrogenic structure, their effects on the brain are profound thus making the neurobiological effects of these compounds an active area of research. One such compound is daidzein, which h...

journal_title：Current medicinal chemistry

authors： Ahmed T,Javed S,Tariq A,Budzyńska B,D'Onofrio G,Daglia M,Nabavi SF,Nabavi SM

更新日期：2017-01-01 00:00:00

abstract：:This investigation aims to evaluate strategies for an efficient selection of bioactive compounds from the multitude and biodiversity of the plant kingdom. Statistics prove natural products (NPs) as a source leading most consistently to successful development of new drugs. However, there are several reasons why the int...

journal_title：Current medicinal chemistry

authors： Rollinger JM,Langer T,Stuppner H

更新日期：2006-01-01 00:00:00

abstract：:The story of antimalarials as antinflammatory drugs dates back several centuries. Chinin, the extract of the Cinchona bark, has been exploited since the 18th century for its antimalarial and antifebrile properties. Later, during the Second World War, the broad use of antimalarials allowed arguing their antirheumatic e...

journal_title：Current medicinal chemistry

authors： Piscianz E,Cuzzoni E,Sharma R,Tesser A,Sapra P,Tommasini A

更新日期：2018-01-01 00:00:00

abstract：:Amyloid beta peptide (Aβ) is recognised as a main feature of Alzheimer's disease (AD). Increasing evidence suggests that small soluble oligomers of Aβ are the toxic form of the peptide and may instigate AD. Different factors including some key residues within Aβ molecule, the cell membrane, prion protein and metals pl...

journal_title：Current medicinal chemistry

authors： Jamasbi E,Wade JD,Separovic F,Hossain MA

更新日期：2016-01-01 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：:Symmetry plays a crucial role in a variety of biological processes. For instance, many protein receptors, upon activation, dimerize to its active form and subsequently produce its biological action. Hence, there is a renewal of curiosity for the synthesis of dimeric molecules (or bivalent ligands) capable, not only to...

journal_title：Current medicinal chemistry

authors： Bérubé G

更新日期：2006-01-01 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：:The kidney has numerous complex interactions with the heart, including shared risk factors (e.g., hypertension, dyslipidemia, etc.) and mutual amplification of morbidity and mortality. Both cardiovascular diseases and chronic kidney disease (CKD) may cause various alterations in cardiovascular system, metabolic homeos...

journal_title：Current medicinal chemistry

authors： Potpara TS,Jokic V,Dagres N,Marin F,Prostran MS,Blomstrom-Lundqvist C,Lip GY

更新日期：2016-01-01 00:00:00

abstract：:Onychomycosis (fungal nail infections) is very common worldwide but is fortunately not often lethal. Several powerful drugs have been introduced into clinical practice in recent years, but these infections remain difficult to cure primarily due to the difficulty of penetration of drug to the site of the infection in t...

journal_title：Current medicinal chemistry

authors： Basha A,Basha F,Ali SK,Hanson PR,Oakley BR,Hajovsky H,Mitscher LA

更新日期：2016-05-27 00:00:00

abstract：:Diabetes mellitus (DM) is characterized by hyperglycemia, resulting from defects in insulin secretion, insulin action or both. There are several factors such as hyperlipidemia and oxidative stress (OS), namely the production of reactive oxygen/nitrogen species (ROS/RNS), that actively contribute to the development and...

journal_title：Current medicinal chemistry

authors： Sousa A,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-05-24 00:00:00

abstract：:The utilization of graphene-based nanomaterials combined with magnetic nanoparticles offers key benefits in the modern biomedicine. In this minireview, we focus on the most recent advances in hybrids of magnetic graphene derivatives for biomedical applications. We initially analyze the several methodologies employed f...

journal_title：Current medicinal chemistry

authors： Alegret N,Criado A,Prato M

更新日期：2017-01-01 00:00:00

abstract：: ...

journal_title：Current medicinal chemistry

authors： Biava PM,Nicolini A

更新日期：2019-01-01 00:00:00

abstract：:Apoptotic cell death has been reported in human oocytes and preimplantation embryos under in vivo and in vitro conditions. BCL-2 family proteins comprise both anti- and pro-apoptotic members, which are likely to play a key role in controlling oocyte and early embryo survival. However, very limited data are available o...

journal_title：Current medicinal chemistry

authors： Boumela I,Assou S,Haouzi D,Déchaud H,Aït-Ahmed O,Hamamah S

更新日期：2014-01-01 00:00:00

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：:To date, many scientific attempts have been directed towards the development of experimental models for the identification of neuronal mechanisms evoking cardiovascular and hemodynamic dysfunctions. The spontaneously hypertensive rat (SHR), a genetic model of essential hypertension, has become a valuable rodent for th...

journal_title：Current medicinal chemistry

authors： Giusi G,Alò R,Avolio E,Zizza M,Facciolo RM,Talani G,Biggio G,Sanna E,Canonaco M

更新日期：2012-01-01 00:00:00

abstract：:The use of antisense oligonucleotides as therapeutic agents has generated considerable enthusiasm in the research and medical community. Antisense oligonucleotides as therapeutic agents were proposed as far back as in the 1970s when the antisense strategy was initially developed. Nonetheless, it has taken almost a qua...

journal_title：Current medicinal chemistry

authors： Aboul-Fadl T

更新日期：2005-01-01 00:00:00

abstract：:Cancer is the world's second leading cause of death after heart diseases, and involves abnormal cell growth at a primary site and the potential to spread to other parts of the body. Tumors are highly heterogeneous and consist of subgroups of cells with distinct characteristics. Of these, the cancer stem cells (CSC) ni...

journal_title：Current medicinal chemistry

authors： Vizetto-Duarte C,Branco PC,Custódio L

更新日期：2020-03-20 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：:Reversible phosphorylation is a key mechanism for regulating the biological activity of many human proteins that affect a diverse array of cellular processes, including protein-protein interactions, gene transcription, cell-cycle progression and apoptosis. Once viewed as simple house keeping enzymes, recent studies ha...

journal_title：Current medicinal chemistry

authors： Honkanen RE,Golden T

更新日期：2002-11-01 00:00:00

abstract：:Cardiovascular pathologies in the French are not prevalent despite high dietary saturated fat consumption. This is commonly referred to as the "French Paradox" attributing its anti-lipidemic effects to moderate consumption of red wine. Resveratrol, a phytoalexin found in red wine, is currently the focus of intense res...

journal_title：Current medicinal chemistry

authors： Raval AP,Lin HW,Dave KR,Defazio RA,Della Morte D,Kim EJ,Perez-Pinzon MA

更新日期：2008-01-01 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