2-Arylbenzothiazole as a privileged scaffold in drug discovery.

abstract：:Migraine is a common disabling neurological disorder which is characterised by a recurring headache associated with a variety of sensory and autonomic symptoms. The pathophysiology of migraine remains not entirely understood, although many mechanisms involving the central and peripheral nervous system are now becoming...

journal_title：Current medicinal chemistry

authors： Cevoli S,Favoni V,Cortelli P

更新日期：2019-01-01 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：:Histone Deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell cycle arrest in cancer cells. Recently, their use has been clinically validated in cancer patients resulting in the approval b...

journal_title：Current medicinal chemistry

authors： Cappellacci L,Perinelli DR,Maggi F,Grifantini M,Petrelli R

更新日期：2020-01-01 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：: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：:Sarcopenia, or age-related muscle decline, occurs in most organisms and burdens both human health and the healthcare system. As our population ages, additional options for treating sarcopenia are needed. Mitochondrial dysfunction is implicated in the onset of sarcopenia, so therapies directed at improving mitochondria...

journal_title：Current medicinal chemistry

authors： Waltz TB,Fivenson EM,Morevati M,Li C,Becker KG,Bohr VA,Fang EF

更新日期：2018-01-01 00:00:00

abstract：:Virtual screening is an important means for lead compound discovery. The scoring function is the key to selecting hit compounds. Many scoring functions are currently available; however, there are no all-purpose scoring functions because different scoring functions tend to have conflicting results. Recently, neural net...

journal_title：Current medicinal chemistry

authors： Shan W,Li X,Yao H,Lin K

更新日期：2020-05-26 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：:A challenging question in biology is how cells control their shape and volume. The relative abundance of organelles can be radically modified to comply with a new task, an example being the massive development of the endoplasmic reticulum (ER) in Ig-secreting plasma cells. The ER is the site where secretory proteins a...

journal_title：Current medicinal chemistry

authors： Otsu M,Sitia R

更新日期：2007-01-01 00:00:00

abstract：:More than five decades since the Discovery of Penicillin, the chemistry and biological activity of b-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial i...

journal_title：Current medicinal chemistry

authors： Kidwai M,Sapra P,Bhushan KR

更新日期：1999-03-01 00:00:00

abstract：:The fibrinolytic system includes a broad spectrum of proteolytic enzymes with physiological and pathophysiological functions in several processes, such as haemostatic balance, tissue remodeling, tumor invasion, angiogenesis and reproduction. The main enzyme of the plasminogen activator system is plasmin, which is resp...

journal_title：Current medicinal chemistry

authors： Zorio E,Gilabert-Estellés J,España F,Ramón LA,Cosín R,Estellés A

更新日期：2008-01-01 00:00:00

abstract：:Obesity and metabolic syndrome represent major public health problems, and are the biggest preventable causes of death worldwide. Obesity is the leading risk factor for type 2 diabetes mellitus (T2DM), cardiovascular diseases and non-alcoholic fatty liver disease. Obesity-associated insulin resistance, which is charac...

journal_title：Current medicinal chemistry

authors： Panzhinskiy E,Ren J,Nair S

更新日期：2013-01-01 00:00:00

abstract：:Paediatric Acquired ImmunoDeficiency Syndrome (AIDS) is a life-threatening and infectious disease in which the Human Immunodeficiency Virus (HIV) is mainly transmitted through Mother-To- Child Transmission (MTCT) during pregnancy, labour and delivery, or breastfeeding. This review provides an overview of the distinct ...

journal_title：Current medicinal chemistry

authors： Melo R,Lemos A,Preto AJ,Bueschbell B,Matos-Filipe P,Barreto C,Almeida JG,Silva RDM,Correia JDG,Moreira IS

更新日期：2020-01-01 00:00:00

abstract：:Photodynamic therapy (PDT) is a novel medical technique involving three key components: light, a photosensitizer molecule and molecular oxygen, which are essential to achieve the therapeutic effect. There has been great interest in the use of PDT in the treatment of many cancers and skin disorders. Upon irradiation wi...

journal_title：Current medicinal chemistry

authors： Skupin-Mrugalska P,Sobotta L,Kucinska M,Murias M,Mielcarek J,Düzgüneş N

更新日期：2014-01-01 00:00:00

abstract：:Mast cells are best known as central effector cells in IgE-mediated type I allergic diseases including asthma and hay fever. An increasing amount of evidence, however, has demonstrated that mast cells are sentinel cells playing a critical role in host defense against invading microbes. Mast cells are located immediate...

journal_title：Current medicinal chemistry

authors： Matsuguchi T

更新日期：2012-01-01 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：:Perceiving a pharmacophore is the first essential step towards understanding the interaction between a receptor and a ligand. Once a pharmacophore is established, a beneficial use of it is 3D database searching to retrieve novel compounds that would match the pharmacophore, without necessarily duplicating the topologi...

journal_title：Current medicinal chemistry

authors： Kurogi Y,Güner OF

更新日期：2001-07-01 00:00:00

abstract：:Protein tyrosine phosphatases (PTPs) are crucial regulators for numerous biological processes in nature. The dysfunction and overexpression of many PTP members have been demonstrated to cause fatal human diseases such as cancers, diabetes, obesity, neurodegenerative diseases and autoimmune disorders. In the past decad...

journal_title：Current medicinal chemistry

authors： He XP,Xie J,Tang Y,Li J,Chen GR

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：:Chronic Obstructive Pulmonary Disease (COPD) is a progressive respiratory disorder characterized by irreversible chronic inflammation and airflow obstruction. It affects more than 64 million patients worldwide and it is predicted to become the third cause of death in the industrialized world by 2030. Currently availab...

journal_title：Current medicinal chemistry

authors： Pirozzi F,Ren K,Murabito A,Ghigo A

更新日期：2019-01-01 00:00:00

abstract：:Selenium is an essential trace element. It is, however toxic at concentration little above which is required for health. Selenium is incorporated into proteins as selenocysteine, the 21(st) amino acid. Selenoproteins are found in bacteria, archaea and eukaryotes. Biochemical and physicochemical properties of selenium ...

journal_title：Current medicinal chemistry

authors： Soriano-Garcia M

更新日期：2004-06-01 00:00:00

abstract：:The deposition of β-amyloid (Aβ) plaques in the parenchymal and cortical brain is accepted as the main pathological hallmark of Alzheimer's disease (AD). According to the amyloid cascade hypothesis, the Aβ deposition in the brain appears to be a good diagnostic biomarker for AD and may also be a good predictive biomar...

journal_title：Current medicinal chemistry

authors： Cui M

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:The genus Achillea L. is rich in bioactive sesquiterpenes and flavonoids; most of the studied species exhibit several biological activities and are used as emmenagogue, wound healing and analgesic agents. Some species are also used in local folklore medicine. OBJECTIVE:Following a literature survey, we disc...

journal_title：Current medicinal chemistry

authors： Papakosta K,Grafakou ME,Barda C,Kostopoulos IV,Tsitsilonis O,Skaltsa H

更新日期：2020-01-01 00:00:00

abstract：:Plant foods are not only a main source of nutrients, but they are also rich in physiologically bioactive bionutrients or phytochemicals. Consumption of fruit and vegetables is associated with a decreased risk of pathological status, including cancer. Reactive oxygen species play a key role in the genesis and developme...

journal_title：Current medicinal chemistry

authors： Matés JM,Segura JA,Alonso FJ,Márquez J

更新日期：2011-01-01 00:00:00

abstract：:The market, sales and regulatory approval of new human medicines, during the past few years, indicates increasing number and share of new biologics and emergence of new multibillion dollar molecules. The global sale of monoclonal antibodies in 2006 were $20.6 billion. Remicade had annual sales gain of $1 billion durin...

journal_title：Current medicinal chemistry

authors： Maggon K

更新日期：2007-01-01 00:00:00

abstract：:Gene expression, both tissue specific or inducible, is controlled at the level of transcription by various transcription factors interacting with specific sequences of DNA. Anticancer drugs and other potential therapeutic agents alter interactions of regulatory proteins with DNA by a variety of different mechanisms. T...

journal_title：Current medicinal chemistry

authors： Gniazdowski M,Denny WA,Nelson SM,Czyz M

更新日期：2003-06-01 00:00:00

abstract：BACKGROUND:Monocyte chemoattractant protein-1 (MCP-1) is a member of the CC chemokine family that plays a key role in the inflammatory process. It has been broadly studied in the aspect of its role in obesity and diabetes related diseases. MCP-1 causes the infiltration of macrophages into obese adipose tissue via bindi...

journal_title：Current medicinal chemistry

authors： Czemplik M,Kulma A,Wang YF,Szopa J

更新日期：2017-01-01 00:00:00

abstract：:In the course of studying human mucin MUC1, the attitude towards this molecule has been changing time and again. Initially, the list of presumable functions of MUC1 was restricted to protecting and lubricating epithelium. To date, it is assumed to play an important role in cell signaling as well as in all stages of on...

journal_title：Current medicinal chemistry

authors： Syrkina MS,Vassetzky YS,Rubtsov MA

更新日期：2019-01-01 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：: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