Free fatty acids-sensing G protein-coupled receptors in drug targeting and therapeutics.

abstract：:The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds, and it is considered as a privileged structure. Stilbenes exemplified by resveratrol, combretastatin A-4 and pterostilbene are of significant interest for drug research and development because of their potenti...

journal_title：Current medicinal chemistry

authors： Giacomini E,Rupiani S,Guidotti L,Recanatini M,Roberti M

更新日期：2016-01-01 00:00:00

abstract：:Nitric Oxide (NO) is a signaling radical, highly diffusible pleiotropic regulator of a large set of different molecular and biological pathways, including, neurotransmission, vasodilatation and macrophagemediated responses against infections. It is produced from the amino acid L-Arginine and oxygen by the enzymatic ac...

journal_title：Current medicinal chemistry

authors： Fionda C,Abruzzese MP,Santoni A,Cippitelli M

更新日期：2016-01-01 00:00:00

abstract：:This review summarizes our knowledge of biochemical, biological and medical applications and properties of phosphinic acid compounds. Phosphinic acid compounds (phosphinates) are derivatives of phosphinic acid H2P(O)(OH). The major attention of this article is focused on applications of phosphinates of a pseudopeptide...

journal_title：Current medicinal chemistry

authors： Collinsová M,Jirácek J

更新日期：2000-06-01 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are among the most commonly used drugs worldwide. Nevertheless, their intake is frequently associated with gastrointestinal side effects, representing still an important medical and socio-economic problem. In recent years efforts focused on the development of highly select...

journal_title：Current medicinal chemistry

authors： Abdel-Tawab M,Zettl H,Schubert-Zsilavecz M

更新日期：2009-01-01 00:00:00

abstract：:Ca(2+) is a highly versatile intracellular second messenger in the central nervous system, and regulates many complicated cellular processes, including excitation, plasticity and apoptosis. Influx of Ca(2+) from the extracellular fluid is required for sustained elevation of the cytosolic Ca(2+) concentration and full ...

journal_title：Current medicinal chemistry

authors： Yagami T,Kohma H,Yamamoto Y

更新日期：2012-01-01 00:00:00

abstract：:COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...

journal_title：Current medicinal chemistry

authors： Cui J,Jia J

更新日期：2020-09-17 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：: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：:Evidence indicates that nerve gas toxins operate in ways in addition to inhibition of acetylcholine esterase. Alternative bioactivities are discussed with focus on electron transfer. The main class, including pralidoxime (2-PAM), incorporates conjugated iminium and oxime moieties that are electron affinic. Various phy...

journal_title：Current medicinal chemistry

authors： Kovacic P

更新日期：2003-12-01 00:00:00

abstract：:ATP-sensitive K(+) channels (K(ATP)channels) regulate insulin secretion by coupling intracellular metabolic changes to excitability of the plasma membrane in pancreatic beta-cells. The channels are closed when extracellular glucose levels are elevated due to enhanced feature. By contrast, cardiac-type K(ATP) channels,...

journal_title：Current medicinal chemistry

authors： Kakei M

更新日期：2003-02-01 00:00:00

abstract：:Since the beginning of the 20th century, important medicinal progress has led medical doctors to think that the end of devastating epidemics has arrived. In 1930, the discovery of sulfamides and penicillin opened a wide area of applications able to fight against bacterial infections. However, almost all antibiotics we...

journal_title：Current medicinal chemistry

authors： Salzet M

更新日期：2005-01-01 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：:Patients with peripheral arterial disease (PAD) suffer from increased cardiovascular morbidity and mortality. The ankle brachial index has been widely used as an easy tool to identify and stratify patients with PAD, however its predictive value remains limited. Higher levels of inflammatory and prothrombotic biomarker...

journal_title：Current medicinal chemistry

authors： Charakida M,Masi S,Tousoulis D

更新日期：2012-01-01 00:00:00

abstract：:Antisynthetase syndrome is a group of closely related rare diseases which clinically manifest with inflammatory myopathies, interstitial lung disease, inflammatory arthritis, skin hyperkeratosis (mechanic’s hands) and Raynaud phenomenon. The pathophysiology of antisynthetase syndrome is not entirely understood, but ge...

journal_title：Current medicinal chemistry

authors： Mirrakhimov AE

更新日期：2015-05-13 00:00:00

abstract：BACKGROUND:N-acetyl-cysteine (NAC) has shown widespread utility in different psychiatric disorders, including a beneficial role in schizophrenic patients. Although the replenishment of glutathione and the antioxidant activity of NAC have been suggested as the mechanisms that improve such a wide range of disorders, none...

journal_title：Current medicinal chemistry

authors： Martínez-Banaclocha M

更新日期：2020-01-01 00:00:00

abstract：:Drug repositioning is an important area of biomedical research. The drug repositioning studies have shifted to computational approaches. Large-scale perturbation databases, such as the Connectivity Map and the Library of Integrated Network-Based Cellular Signatures, contain a number of chemical-induced gene expression...

journal_title：Current medicinal chemistry

authors： Wang F,Lei X,Wu FX

更新日期：2020-01-01 00:00:00

abstract：BACKGROUND:Leukotrienes (LTs) constitute a bioactive group of polyunsaturated fatty acid (PUFA) metabolites molded by the enzymatic activity of lipoxygenase (LO) and have a pivotal role in inflammation and allergy. Evidence is accumulating both by in vitro cell culture experiments and animal tumor model studies in supp...

journal_title：Current medicinal chemistry

authors： Mahboubi-Rabbani M,Zarghi A

更新日期：2019-12-09 00:00:00

abstract：BACKGROUND:Serotonin reuptake inhibitors (SRIs) and cognitive-behavioral psychotherapy (CBT) are first-line treatments for obsessive-compulsive disorder (OCD). Since response is often inadequate, in recent years researchers investigated whether combining CBT and SRIs, either ab initio or sequentially, results in a grea...

journal_title：Current medicinal chemistry

authors： Albert U,Di Salvo G,Solia F,Rosso G,Maina G

更新日期：2018-01-01 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：:Essential oils constituents are a diverse family of low molecular weight organic compounds with comprehensive biological activity. According to their chemical structure, these active compounds can be divided into four major groups: terpenes, terpenoids, phenylpropenes, and "others". In addition, they may contain diver...

journal_title：Current medicinal chemistry

authors： Burčul F,Blažević I,Radan M,Politeo O

更新日期：2020-01-01 00:00:00

abstract：:Differentiation therapy of acute promyelocytic leukemia with all-trans retinoic acid represents the most successful pharmacological therapy of acute myeloid leukemia (AML). Numerous studies demonstrate that drugs that inhibit mechanistic target of rapamycin (mTOR) and activate AMP-kinase (AMPK) have beneficial effects...

journal_title：Current medicinal chemistry

authors： Visnjic D,Dembitz V,Lalic H

更新日期：2019-01-01 00:00:00

abstract：:Multitarget-directed ligands (MTDLs), an emerging and appealing drug discovery strategy, utilizing a single chemical entity to inhibit multitargets, was confirmed to be effective in reducing the likelihood of drug resistance, diminishing problems of dosing complexity, drug-drug interactions and toxicities, as well as ...

journal_title：Current medicinal chemistry

authors： Zhan P,Liu X

更新日期：2013-01-01 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：BACKGROUND:Lipids are essential components of cells that participate in metabolic and endocrine regulation and reproductive functions. The main organs where lipid regulation takes place are the liver and adipose tissue. Besides, when each tissue specific action cannot be exerted, it could lead to several endocrine-meta...

journal_title：Current medicinal chemistry

authors： Ferrer MJ,Silva AF,Abruzzese GA,Velázquez ME,Motta AB

更新日期：2021-01-06 00:00:00

abstract：:Heme is an essential molecule with contradictory biological functions. In hemoproteins such as hemoglobin and cytochromes protein-bound heme is a prosthetic group serving physiological functions as a transporter for oxygen and electrons. On the other hand free heme can have deleterious effects by generating reactive o...

journal_title：Current medicinal chemistry

authors： Wijayanti N,Katz N,Immenschuh S

更新日期：2004-04-01 00:00:00

abstract：:Osteogenic peptides are, or have potential to be, therapies for the treatment of osteoporosis, fracture repair, and repair of loosened bone implants. Human parathyroid hormone has been approved for the treatment of post-menopausal osteoporosis. Constrained analogs of PTH and the parathyroid-hormone related peptide (PT...

journal_title：Current medicinal chemistry

authors： Willick GE,Morley P,Whitfield JF

更新日期：2004-11-01 00:00:00

abstract：BACKGROUND:COVID-19 has brought the world to its knees and there is an urgent need for new strategies to identify molecules capable of fighting the pandemic. During the last few decades NMR (Nuclear Magnetic Resonance) spectroscopy has emerged as an intriguing structural biology instrument in the antiviral drug discove...

journal_title：Current medicinal chemistry

authors： Vincenzi M,Leone M

更新日期：2020-12-28 00:00:00

abstract：:The synthesis of oxacephalotin and oxacephamandol, which are more active than natural, sulfur-containing congeners, and the isolation of clavulanic acid, a potent inhibitor of beta-lactamase enzymes, directed attention of many academic and industrial laboratories the synthesis of oxygen analogues of penicillins and ce...

journal_title：Current medicinal chemistry

authors： Łysek R,Borsuk K,Furman B,Kałuza Z,Kazimierski A,Chmielewski M

更新日期：2004-07-01 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：:The purinergic receptor P2X7 is highly expressed in immune peripheral and central cells suggesting its important role in numerous diseases characterized by inflammatory processes like cancer, or neurodegenerative pathologies in relation with modulation of the immune system. Thereby, antagonization of this receptor may...

journal_title：Current medicinal chemistry

authors： Baudelet D,Lipka E,Millet R,Ghinet A

更新日期：2015-01-01 00:00:00