Regulators of serine/threonine protein phosphatases at the dawn of a clinical era?

abstract：:The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient non-steroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five struc...

journal_title：Current medicinal chemistry

authors： Dannhardt G,Laufer S

更新日期：2000-11-01 00:00:00

abstract：:Osteoporosis is a pathological loss of bone mass due to an imbalance in bone remodeling where osteoclast-mediated bone resorption exceeds osteoblast-mediated bone formation resulting in skeletal fragility and fractures. Anti-resorptive agents such as bisphosphonates and SERMs, and anabolic drugs that stimulate bone fo...

journal_title：Current medicinal chemistry

authors： Li H,Xiao Z,Quarles LD,Li W

更新日期：2020-03-30 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：:Statins are inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate-limiting enzyme of cholesterol synthesis. In recent years, statins have become the major choice of treatment for hypercholesterolemia. Emerging evidence from both animal and human studies indicates that mechanisms i...

journal_title：Current medicinal chemistry

authors： Luo JD,Chen AF

更新日期：2003-08-01 00:00:00

abstract：:The nucleotide metabolism has been targeted for many years and in various clinical settings, including cancer. The increased knowledge of certain enzymes involved in this metabolism and in associated cellular processes accumulated over the last few years, gives important information to the druggability of certain prot...

journal_title：Current medicinal chemistry

authors： Forey P,Cros-Perrial E,Dumontet C,Jordheim LP

更新日期：2020-11-25 00:00:00

abstract：:Benzamide riboside (BR) after anabolism to an analogue of NAD, was shown to inhibit the activity of NAD-dependent enzymes such as inosine 5'-monophosphate dehydrogenase (IMPDH), the rate limiting enzyme in de novo guanylate biosynthesis, and malate dehydrogenase which is involved in the citric cycle and respiratory ch...

journal_title：Current medicinal chemistry

authors： Polgar D,Gfatter S,Uhl M,Kassie F,Leisser C,Krupitza G,Grusch M

更新日期：2002-04-01 00:00:00

abstract：:Gum resin extracts of Boswellia species have been traditionally applied in folk medicine for centuries to treat various chronic inflammatory diseases, and experimental data from animal models and studies with human subjects confirmed the potential of B. spec extracts for the treatment of not only inflammation but also...

journal_title：Current medicinal chemistry

authors： Poeckel D,Werz O

更新日期：2006-01-01 00:00:00

abstract：:Inflammation is an initial response of the body to a harmful stimuli and it is achieved by the increased movement of leukocytes (especially granulocytes) from blood into injured tissues. It is required for healing wounds and infections. Despite their indispensable role in microbial killing, the inflammation reactions ...

journal_title：Current medicinal chemistry

authors： Soubhye J,Aldib I,Delporte C,Prévost M,Dufrasne F,Antwerpen PV

更新日期：2016-01-01 00:00:00

abstract：:The concept of click chemistry represented by the formation of the 1,2,3-triazole core has found wide application in drug discovery, particularly in the early discovery phases and the lead optimization process. 1,2,3-Triazoles ha ve attracted considerable attention in recent years because of their wide range of biolog...

journal_title：Current medicinal chemistry

authors： Raic-Malic S,Mescic A

更新日期：2015-01-01 00:00:00

abstract：:Cu(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) is often utilized in medicinal chemistry to make the triazole moiety as it acts as a non-classical bioisostere of the peptide bond. This useful technique can also be applied in the fragment-based assembly of molecular libraries for high-throughput screening. This mini...

journal_title：Current medicinal chemistry

authors： Fabbrizzi P,Menchi G,Guarna A,Trabocchi A

更新日期：2014-01-01 00:00:00

abstract：:It is now widely accepted that airway inflammation is the key factor underlying the pathogenesis of asthma. Inhaled corticosteroids remain the most important anti-inflammatory treatment for asthma. However, they are rather non-specific in their actions and their use raises concerns over side effects and compliance iss...

journal_title：Current medicinal chemistry

authors： Walsh GM

更新日期：2006-01-01 00:00:00

abstract：:A large number of children in the autism spectrum disorder suffer from gastrointestinal (GI) conditions, such as constipation and diarrhea. Clostridium bolteae is a part of a set of pathogens being regularly detected in the stool samples of hosts affected by GI and autism symptoms. Accompanying studies have pointed ou...

journal_title：Current medicinal chemistry

authors： Pequegnat B,Monteiro MA

更新日期：2019-01-01 00:00:00

abstract：:Non-alcoholic fatty liver disease is regarded as the hepatic manifestation of metabolic syndrome and is an important and common cause of chronic liver disease with a potential to develop end-stage liver disease. While important advances in the pathophysiology have been achieved using genetically modified and diet-indu...

journal_title：Current medicinal chemistry

authors： Chavez-Tapia NC,Rosso N,Tiribelli C

更新日期：2011-01-01 00:00:00

abstract：:This review covers recent literature from 2012-2019 concerning 170 marine natural products and their semisynthetic analogues with strong anticancer biological activities. Reports that shed light on cellular and molecular mechanisms and biological functions of these compounds, thus advancing the understanding in cancer...

journal_title：Current medicinal chemistry

authors： Matulja D,Wittine K,Malatesti N,Laclef S,Turks M,Markovic MK,Ambrožić G,Marković D

更新日期：2020-01-01 00:00:00

abstract：:The expansion of fluorescent techniques for studying the ligand-receptor interaction resulted in a burst of the novel fluorescent ligands development. The discovery of the ligand, that is of high affinity to the receptor and whose localization could be easily visualized, even on the single cell level, gave the researc...

journal_title：Current medicinal chemistry

authors： Kuder K,Kieć-Kononowicz K

更新日期：2008-01-01 00:00:00

abstract：:Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hybrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can result in compounds pres...

journal_title：Current medicinal chemistry

authors： Viegas-Junior C,Danuello A,da Silva Bolzani V,Barreiro EJ,Fraga CA

更新日期：2007-01-01 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：:The chemokine receptor, CXCR4, is a GPCR that transduces signals of its endogenous ligand, CXCL12 (stromal cell-derived factor-1, SDF-1). The CXCL12-CXCR4 system plays an important role in the migration of progenitors during embryologic development of the cardiovascular, hemopoietic, central nervous systems, etc. This...

journal_title：Current medicinal chemistry

authors： Tamamura H,Tsutsumi H,Masuno H,Fujii N

更新日期：2007-01-01 00:00:00

abstract：:The ionotropic P2X7 receptor (P2X7R) has become the focus of intense research interest for a number of reasons: i) it is a cation selective ion channel that is modulated by extracellular ATP. Upon stimulation by high concentrations of ATP it generates a non-selective membrane pore which is permeable to hydrophilic mol...

journal_title：Current medicinal chemistry

authors： Gunosewoyo H,Coster MJ,Kassiou M

更新日期：2007-01-01 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：BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...

journal_title：Current medicinal chemistry

authors： O Brien Z,Moghaddam MF

更新日期：2017-01-01 00:00:00

abstract：:The existence of functional NT/dopamine interactions in the central nervous system has been extensively documented. Among others, a possible molecular mechanism underlying the NT-induced modulation of dopamine release is a direct antagonistic NTS(1)/D(2) receptor interaction. More recently, neurochemical experiments a...

journal_title：Current medicinal chemistry

authors： Tanganelli S,Antonelli T,Tomasini MC,Beggiato S,Fuxe K,Ferraro L

更新日期：2012-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is a complex and progressive neurodegenerative disorder. The available therapy is limited to the symptomatic treatment and its efficacy remains unsatisfactory. In view of the prevalence and expected increase in the incidence of AD, the development of an effective therapy is crucial for public ...

journal_title：Current medicinal chemistry

authors： Guzior N,Wieckowska A,Panek D,Malawska B

更新日期：2015-01-01 00:00:00

abstract：:In the last decade, drug resistant invasive mycoses have become significantly more common and new antifungal drugs and ways to specifically deliver them to the fungal cell are being looked for. One of the biggest obstacles in finding such comes from the fact that fungi share essential metabolic pathways with humans. O...

journal_title：Current medicinal chemistry

authors： Walencik PK,Watly J,Rowinska-Zyrek M

更新日期：2016-01-01 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：:Photodynamic therapy (PDT) involves the administration of a photosensitizer (PS) followed by illumination with visible light, leading to generation of reactive oxygen species. The mechanisms of resistance to PDT ascribed to the PS may be shared with the general mechanisms of drug resistance, and are related to altered...

journal_title：Current medicinal chemistry

authors： Casas A,Di Venosa G,Hasan T,Al Batlle

更新日期：2011-01-01 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 glomerulonephritides are a collection of separate diseases with differing pathogeneses that collectively are common and important causes of renal disease. Effective, non-toxic immunomodulatory treatments for glomerulonephritis are lacking. This review will focus on our understanding of the role of leukocytes in im...

journal_title：Current medicinal chemistry

authors： Kitching AR,Holdsworth SR,Hickey MJ

更新日期：2008-01-01 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：:Drug-loaded nanoparticles have shown great potential in the study of carriers for disease-targeting drug delivery. Drug-loaded nanoparticles are excellent in keeping the drug in the systemic circulation for a prolonged period of time, introducing targeting molecules to improve targeting efficiency and to reduce side e...

journal_title：Current medicinal chemistry

authors： Tu Q,Zhang Y,Liu R,Wang JC,Li L,Nie N,Liu A,Wang L,Liu W,Ren L,Wang X,Wang J

更新日期：2012-01-01 00:00:00