Phosphodiesterase 10 Inhibitors - Novel Perspectives for Psychiatric and Neurodegenerative Drug Discovery.

abstract：:Vitamin D has been known for a long time as a major factor involved in the calcium- phosphate balance and homeostasis, along with parathyroid hormone (PTH). While vitamin D effects on calcium and phosphate are fully known, recent studies attempted to link vitamin D status and cardiovascular diseases. The involvement o...

journal_title：Current medicinal chemistry

authors： Santoro D,Pellicanò V,Cernaro V,Lacava V,Lacquaniti A,Atteritano M,Buemi M

更新日期：2016-01-01 00:00:00

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00

abstract：:The oxime formation reaction of therapeutical progestogen (levonorgestrel, levonorgestrel acetate, norethisterone), androgen (methyltestosterone, testosterone phenylpropionate) and anabolic (nortestosterone phenylpropionate) Delta(4)-3-ketosteroids has been investigated. The ketosteroid-hydroxylamine reaction was moni...

journal_title：Current medicinal chemistry

authors： Szentesi A,Gergely A,Horváth P,Mahó S,Mátyus P,Szász G

更新日期：2001-09-01 00:00:00

abstract：BACKGROUND:The therapeutic properties of cannabinoids are well-known since ancient years. Growing evidence exist on endocannabinoid system (ECS) modulation related with human tumorigenesis. OBJECTIVE:Taking into account the substantial role of ECS on immune cell regulation, the present review is aimed to summarize the...

journal_title：Current medicinal chemistry

authors： Giaginis C,Lakiotaki E,Korkolopoulou P,Konstantopoulos K,Patsouris E,Theocharis S

更新日期：2016-01-01 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：:Irinotecan, a camptothecin analogue, is a prodrug which requires bioactivation to form the active metabolite SN-38. SN-38 acts as a DNA topoisomerase I poison. Irinotecan has been widely used in the treatment of metastatic colorectal cancer, small cell lung cancer and several other solid tumors. However, large inter-p...

journal_title：Current medicinal chemistry

authors： Ma MK,McLeod HL

更新日期：2003-01-01 00:00:00

abstract：:Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...

journal_title：Current medicinal chemistry

authors： Eros D,Kövesdi I,Orfi L,Takács-Novák K,Acsády G,Kéri G

更新日期：2002-10-01 00:00:00

abstract：:Signalling lipids are known to control a wide array of cellular processes, including cell proliferation, apoptosis, migration, and energy metabolism. Fatty acids and their derivatives, eicosanoids, phosphoinositides, sphingolipids, some cannabinoid-like molecules bind and activate nuclear receptors, including peroxiso...

journal_title：Current medicinal chemistry

authors： Fidaleo M,Fanelli F,Ceru MP,Moreno S

更新日期：2014-01-01 00:00:00

abstract：:Nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF) belong to the protein family of neurotrophins. They both display profound neuromodulatory functions and are essentially involved in the survival and homeostatic maintenance of central and peripheral neurons during development and adulthood. Moreove...

journal_title：Current medicinal chemistry

authors： Schulte-Herbrüggen O,Braun A,Rochlitzer S,Jockers-Scherübl MC,Hellweg R

更新日期：2007-01-01 00:00:00

abstract：BACKGROUND:Glioma is a heterogeneous, highly complicated central nervous system (CNS) tumor with uncertain mechanism of initiation and progression, resulting in an unfavorable outcome. An extended network of cytokines is recognized as a major regulator of glioma pathogenesis, either promoting or inhibiting glioma progr...

journal_title：Current medicinal chemistry

authors： Kosmopoulos M,Christofides A,Drekolias D,Zavras PD,Gargalionis AN,Piperi C

更新日期：2018-01-01 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：: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：BACKGROUND:With global increase in elderly population, modern societies must find strategies to reduce the consequences of aging process; thereby decreasing the incidence of age-related neurodegenerative diseases. Oxidative stress and recently inflammation, have been pointed out as the leading causes of brain aging. Th...

journal_title：Current medicinal chemistry

authors： Sarubbo F,Moranta D,Asensio VJ,Miralles A,Esteban S

更新日期：2017-01-01 00:00:00

abstract：:The biological relevance of sulfur containing carbohydrates is gaining substantial attention. Thus the new developments, especially in the synthetic and medicinal chemistry of thio-sugars are critically important for carbohydrate drug design. New studies of biological processes including biosynthetic reactions and enz...

journal_title：Current medicinal chemistry

authors： Witczak ZJ

更新日期：1999-02-01 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：: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：:Leukoaraiosis (LA), one of the most frequent causes of cognitive disturbances, is presumed to involve vascular demyelinization and cerebral small-vessel diseases. Although it has been suggested that the development of LA is associated with cerebral circulatory disturbances, the pathomechanism of this circulatory probl...

journal_title：Current medicinal chemistry

authors： Szolnoki Z

更新日期：2007-01-01 00:00:00

abstract：:Breast cancer is an example of a solid tumour which is well treated in the early stages of disease by surgical excision, but once metastatic spread has occurred, medical therapies (chemotherapy and radiotherapy) are highly toxic, expensive and palliative. It is known that certain tumours exhibit specific patterns of m...

journal_title：Current medicinal chemistry

authors： Dowsland MH,Harvey JR,Lennard TW,Kirby JA,Ali S

更新日期：2003-04-01 00:00:00

abstract：:Metabolomics is playing an increasingly important role in plant science. It aims at the comprehensive analysis of the plant metabolome which consists both of primary and secondary metabolites. The goal of metabolomics is ultimately to identify and quantify this wide array of small molecules in biological samples. This...

journal_title：Current medicinal chemistry

authors： Wolfender JL,Rudaz S,Choi YH,Kim HK

更新日期：2013-01-01 00:00:00

abstract：:HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) nowadays represent most promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT). They have a unique antiviral potency, high specificity and low cytotoxicity. However, to a great extent, the efficacy of HIV-1 NNRTIs is compounde...

journal_title：Current medicinal chemistry

authors： Chen X,Zhan P,Li D,De Clercq E,Liu X

更新日期：2011-01-01 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：BACKGROUND:We report herein the synthesis of a novel dicationic boron dipyrromethene derivative (compound 3) which is symmetrically substituted with two trimethylammonium styryl groups. METHODS:The antibacterial photodynamic activity of compound 3 was determined against sixteen methicillin-resistant Staphylococcus aur...

journal_title：Current medicinal chemistry

authors： Dharmaratne P,Yu L,Wong RC,Chan BC,Lau KM,Wang B,Lau CB,Fung KP,Ng DK,Ip M

更新日期：2020-12-07 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：:Several lines of defense maintain the surface integrity of the delicate airway epithelium which is regularly subjected to severe trauma. These defense mechanisms include protection by the mucus layer, rapid repair by restitution (cell migration) and regeneration via proliferation and differentiation. Luminal surveilla...

journal_title：Current medicinal chemistry

authors： Hoffmann W

更新日期：2007-01-01 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：BACKGROUND:Stimuli-responsive carriers are a class of drug delivery systems which can change their physicochemical properties and/or structural conformations in response to specific stimuli. Although passive and active drug targeting has proved to reduce the side effects to normal cells, controlled intracellular drug r...

journal_title：Current medicinal chemistry

authors： Sheng Y,Hu J,Shi J,Lee LJ

更新日期：2019-01-01 00:00:00

abstract：:Epinephrine and Norepinephrine, typically released during stress bind to nine different adrenoceptors (AR) which classically control the cardiovascular and respiratory systems. New targets were described for the many agonists and antagonists developed for these AR, as the central nervous system. During the last three ...

journal_title：Current medicinal chemistry

authors： Lüthy IA,Bruzzone A,Piñero CP,Castillo LF,Chiesa IJ,Vázquez SM,Sarappa MG

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:In view of many current mosquito-borne diseases there is a need for the design of novel repellents. OBJECTIVE:The objective of this article is to review the results of the researches carried out by the authors in the computer-assisted design of novel mosquito repellents. METHODS:Two methods in the computat...

journal_title：Current medicinal chemistry

authors： Basak SC,Bhattacharjee AK

更新日期：2020-01-01 00:00:00

abstract：:Thalidomide (N-alpha-phthalimidoglutarimide) was used widely as a hypnotic/sedative agent in the late 1950s and the early 1960s, but had to be withdrawn from the market because of its severe teratogenicity. In spite of this, there has been a resurgence of interest in the drug in recent years due to its potential usefu...

journal_title：Current medicinal chemistry

authors： Hashimoto Y

更新日期：1998-06-01 00:00:00

abstract：:Melatonin, a tryptophan-derived neurohormone found in animals, plants, and microbes, participates in various biological and physiological functions. Among other properties, numerous in vitro or in vivo studies have reported its therapeutic potential against many parasites, bacteria and viruses. In this concern, melato...

journal_title：Current medicinal chemistry

authors： Elmahallawy EK,Luque JO,Aloweidi AS,Gutiérrez-Fernández J,Sampedro-Martínez A,Rodriguez-Granger J,Kaki A,Agil A

更新日期：2015-01-01 00:00:00