Biosynthesis of bacterial aromatic polyketides.

abstract：:Inflammation is a complex phenomenon necessary in human defense mechanisms but also involved in the development of some human diseases. The discovery of cyclooxygenase-2 (COX- 2) improved the pharmacology of nonsteroidal anti-inflammatory drugs (NSAID) giving a clear mechanism for prostaglandin regulation in vivo and ...

journal_title：Current topics in medicinal chemistry

authors： Rayar AM,Lagarde N,Ferroud C,Zagury JF,Montes M,Sylla-Iyarreta Veitia M

更新日期：2017-01-01 00:00:00

abstract：:Dementia is an increasing health problem in older aged populations worldwide. Age-related changes in the brain can be observed decades before the first symptoms of cognitive decline appear. Cognitive impairment has chronic inflammatory components, which can be enhanced by systemic immune activation. There exist mutual...

journal_title：Current topics in medicinal chemistry

authors： Leblhuber F,Steiner K,Geisler S,Fuchs D,Gostner JM

更新日期：2020-01-01 00:00:00

abstract：:The vesicular acetylcholine transporter (VAChT) is a glycoprotein responsible for the accumulation of acetylcholine into pre-synaptic vesicules of cholinergic neurons. Cholinergic innervation has been shown to be decreased at the earlier stages of Alzheimer's disease (AD). Thus, the expression of VAChT has been correl...

journal_title：Current topics in medicinal chemistry

authors： Giboureau N,Som IM,Boucher-Arnold A,Guilloteau D,Kassiou M

更新日期：2010-01-01 00:00:00

abstract：:Choline kinase (CK) is a homodimeric enzyme that catalyses the transfer of the ATP γ-phosphate to choline, generating phosphocholine and ADP in the presence of magnesium. Several isoforms of CK are present in humans but only the HsCKα has been associated with cancer and validated as a drug target to treat this disease...

journal_title：Current topics in medicinal chemistry

authors： Serran-Aguilera L,Nuti R,López-Cara LC,Ríos-Marco P,Carrasco MP,Marco C,Entrena A,Macchiarulo A,Hurtado-Guerrero R

更新日期：2014-01-01 00:00:00

abstract：:The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...

journal_title：Current topics in medicinal chemistry

authors： Thai KM,Ngo TD,Tran TD,Le MT

更新日期：2013-01-01 00:00:00

abstract：:The genetics of Alzheimer's disease (AD) implies that restoring non-pathological levels or ratios of different amyloid-beta (Abeta) peptide species in the brain could prevent the onset or delay the progression of this neurodegenerative disease. In particular, a selective reduction of the longer Abeta(1-42) peptide whi...

journal_title：Current topics in medicinal chemistry

authors： Beher D

更新日期：2008-01-01 00:00:00

abstract：:Pronucleotides represent a promising alternative to improve the biological activity of nucleoside analogues against different viral diseases. The basic idea is to achieve nucleotide delivery into cells, bypassing limitations with intracellular formation of nucleotides from their nucleoside precursors. The cycloSal-con...

journal_title：Current topics in medicinal chemistry

authors： Meiera C,Renzea J,Ducho C,Balzarini J

更新日期：2002-10-01 00:00:00

abstract：:Salbutamol forms an important and widely administered β2 agonist prescribed in the symptomatic treatment of bronchial asthma. Unfortunately, a subset of patients show refractoriness to it owing to ADRB2 gene variant (rs 1800888). The variant substitutes Thr to Ile at the position 164 in the β2 adrenergic receptor lead...

journal_title：Current topics in medicinal chemistry

authors： Bandaru S,Tiwari G,Akka J,Marri VK,Alvala M,Gutlapalli VR,Nayarisseri A,Mundluru HP

更新日期：2015-01-01 00:00:00

abstract：:Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....

journal_title：Current topics in medicinal chemistry

authors： Casazza V,Rossi F,Rizzi M

更新日期：2011-01-01 00:00:00

abstract：:With the global aging population, Alzheimer's disease, Parkinson's disease and mild cognition impairment are increasing in prevalence. The success of rapamycin as an agent to extend lifespan in various organisms, including mice, brings hope that chronic mTOR inhibition could also refrain age-related neurodegeneration....

journal_title：Current topics in medicinal chemistry

authors： Jahrling JB,Laberge RM

更新日期：2015-01-01 00:00:00

abstract：:The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally α-amino acids with one or more stereogenic centers due to st...

journal_title：Current topics in medicinal chemistry

authors： Vogensen SB,Greenwood JR,Bunch L,Clausen RP

更新日期：2011-01-01 00:00:00

abstract：:Dipeptidyl peptidase-IV (DPP-IV) (EC 3.4.14.5) is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structu...

journal_title：Current topics in medicinal chemistry

authors： Smelcerovic A,Miljkovic F,Kolarevic A,Lazarevic J,Djordjevic A,Kocic G,Anderluh M

更新日期：2015-01-01 00:00:00

abstract：:Bacterial infections constitute an always growing health problem worldwide. The resistance to antibiotics of an increasing number of bacterial pathogens necessitates a permanent search for new molecules with different mechanisms of action. Histidine biosynthesis is an ancient pathway found in bacteria, archaebacteria,...

journal_title：Current topics in medicinal chemistry

authors： Monti SM,De Simone G,D'Ambrosio K

更新日期：2016-01-01 00:00:00

abstract：:Urinary protein biomarkers and metabolomic markers have been leveraged to detect acute Drug Induced Kidney Injury (DIKI) in rats; however, the utility of these indicators to enable early detection of DIKI in canine models has not been well documented. Therefore, we evaluated temporal changes in biomarkers and metaboli...

journal_title：Current topics in medicinal chemistry

authors： Wagoner MP,Yang Y,McDuffie JE,Klapczynski M,Buck W,Cheatham L,Eisinger D,Sace F,Lynch KM,Sonee M,Ma JY,Chen Y,Marshall K,Damour M,Stephen L,Dragan YP,Fikes J,Snook S,Kinter LB

更新日期：2017-01-01 00:00:00

abstract：:PLA2 enzyme catalyses the hydrolysis of cellular phospholipids at the sn-2 position to liberate arachidonic acid and lysophospholipid to generate a family of pro-inflammatory eicosanoids and platelet activating factor. The generation of pro-inflammatory eicosanoids involves a series of free radical intermediates with ...

journal_title：Current topics in medicinal chemistry

authors： Nanda BL,Nataraju A,Rajesh R,Rangappa KS,Shekar MA,Vishwanath BS

更新日期：2007-01-01 00:00:00

abstract：:Most drug discovery programs today originate by selection of 'hit' molecules resulting from assays against large compound screening libraries. The chemical space in which these hits reside has implications for its biological activity in vivo and likelihood of progression to a drug candidate. We have created a database...

journal_title：Current topics in medicinal chemistry

authors： Zuegg J,Cooper MA

更新日期：2012-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Scotti MT,Muratov EN,González-Díaz H

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Neuraminidase inhibitors (NAIs) are the only class of antivirals in clinical use against influenza virus approved worldwide. However, approximately 1-3% of circulating strains present resistance mutations to oseltamivir (OST), the most used NAI. Therefore, it is important to catalogue new molecules to inhibi...

journal_title：Current topics in medicinal chemistry

authors： de Freitas CS,Rocha MEN,Sacramento CQ,Marttorelli A,Ferreira AC,Rocha N,de Oliveira AC,de Oliveira Gomes AM,Dos Santos PS,da Silva EO,da Costa JP,de Lima Moreira D,Bozza PT,Silva JL,Barroso SPC,Souza TML

更新日期：2020-01-01 00:00:00

abstract：:An intensive research effort during the last 25 years has generated an impressive number of alkaloids isolated from marine ascidians, which remain unique among marine invertebrates in that they overwhelmingly produce this kind of metabolites. The present review is focused on some major groups of ascidians' bioactive a...

journal_title：Current topics in medicinal chemistry

authors： Menna M

更新日期：2014-01-01 00:00:00

abstract：:G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited f...

journal_title：Current topics in medicinal chemistry

authors： Kontoyianni M

更新日期：2016-01-01 00:00:00

abstract：:Despite the tremendous progress in the field of drug designing, discovering a new drug molecule is still a challenging task. Drug discovery and development is a costly, time consuming and complex process that requires millions of dollar and 10-15 years to bring new drug molecules in the market. This huge investment an...

journal_title：Current topics in medicinal chemistry

authors： Singla D,Dhanda SK,Chauhan JS,Bhardwaj A,Brahmachari SK,Open Source Drug Discovery Consortium.,Raghava GP

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND:Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to...

journal_title：Current topics in medicinal chemistry

authors： Francisco CS,Javarini CL,de S Barcelos I,Morais PAB,de Paula H,de S Borges W,Neto ÁC,Lacerda V

更新日期：2020-01-01 00:00:00

abstract：:The Human Genome Project and the explosion of high-throughput data have transformed the areas of molecular and personalized medicine, which are producing a wide range of studies and experimental results and providing new insights for developing medical applications. Research in many interdisciplinary fields is resulti...

journal_title：Current topics in medicinal chemistry

authors： de la Iglesia D,García-Remesal M,de la Calle G,Kulikowski C,Sanz F,Maojo V

更新日期：2013-01-01 00:00:00

abstract：:Chagas disease and African sleeping sickness are trypanosomal infections that represent important public health problems in Latin America and Africa, respectively. The restriction of these diseases to the poorer parts of the world has meant that they have been largely neglected and limited progress has been made in th...

journal_title：Current topics in medicinal chemistry

authors： Wilkinson SR,Bot C,Kelly JM,Hall BS

更新日期：2011-01-01 00:00:00

abstract：:This article focuses on the GDNF family of neurotrophic factors as a potential new class of therapeutics for neuropathic pain, with a particular emphasis on the ligands, artemin and GDNF. In vivo activity of the ligands, expression of ligands and receptors after peripheral nerve injury, and modulation of nerve injury-...

journal_title：Current topics in medicinal chemistry

authors： Sah DW,Ossipov MH,Rossomando A,Silvian L,Porreca F

更新日期：2005-01-01 00:00:00

abstract：:Cyclic peptide scaffolds are key components of signal transduction pathways in both prokaryotic and eukaryotic organisms since they act as chemical messengers that activate or inhibit specific cognate receptors. In prokaryotic organisms these peptides are utilized in non-essential pathways, such as quorum sensing, tha...

journal_title：Current topics in medicinal chemistry

authors： Mull RW,Harrington A,Sanchez LA,Tal-Gan Y

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:The impact of fungal infections on human health has increased considerably within a past few decades. Although drugs with antifungal properties are available, but they are less effective and are associated with side effects. OBJECTIVE AND METHOD:To screen the bacterial isolates from Sesamum indicum and to i...

journal_title：Current topics in medicinal chemistry

authors： Chaudhary R,Balhara M,Jangir D,Dangi M,Dangi M,Khatri S,Chhillar AK

更新日期：2018-01-01 00:00:00

abstract：:Safety and biocompatibility assessment of biomaterials are themes of constant concern as advanced materials enter the market as well as products manufactured by new techniques emerge. Within this context, this review provides an up-to-date approach on current methods for the characterization and safety assessment of b...

journal_title：Current topics in medicinal chemistry

authors： Oliveira JPR,Melendez-Ortiz HI,Bucio E,Alves PT,Lima MIS,Goulart LR,Mathor MB,Varca GHC,Lugao AB

更新日期：2018-01-01 00:00:00

abstract：: ...

journal_title：Current topics in medicinal chemistry

authors： Nayarisseri A,Hood EA

更新日期：2018-01-01 00:00:00

abstract：:Research over the years has gradually and sequentially highlighted contributory role of hypothalamic- based kisspeptin-signaling axis as a major positive modulator of the neuroendocrinological reproductive axis in mammals. However, a series of landmark studies provided convincing evidence of role of this signaling in ...

journal_title：Current topics in medicinal chemistry

authors： Jabeen S,Qureshi MZ,Javed Z,Iqbal MJ,Ismail M,Farooqi AA

更新日期：2016-01-01 00:00:00