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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/27924727/metabolomics-of-healthy-berry-fruits
#1
Gilda D Urso, Sonia Piacente, Cosimo Pizza, Paola Montoro
The consumption of berry-type fruits has become very popular in recent years because of their positive effects on human health. Berries are in fact widely known for their health-promoting benefits, including prevention of chronic disease, cardiovascular disease and cancer. Berries are a rich source of bioactive metabolites, such as vitamins, minerals, and phenolic compounds, mainly anthocyanins. Numerous in vitro and in vivo studies recognized the health effects of berries and their function as bioactive modulators of various cell functions associated with oxidative stress...
December 5, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27919217/drug-delivery-nanoparticles-in-treating-chemoresistant-tumor-cells
#2
Giuseppina Barrera, Martina Daga, Benedetta Ferrara, Chiara Dianzani, Stefania Pizzimenti, Monica Argenziano, Roberta Cavalli, Francesco Trotta
Intrinsic or acquired chemoresistance represents the main obstacle to the successful treatment of cancer patients. Several mechanisms are involved in multidrug resistance: decreased uptake of hydrophilic drugs, increase of energy dependent efflux, alteration of the redox state, alteration of apoptotic pathways, and modification of the tumor microenvironment. In recent years, several types of nanoparticles have been developed to overcome these obstacles and improve the accumulation and release of drugs at the pathological site...
December 5, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27919216/topoisomerase-ii-inhibitors-and-poisons-and-the-influence-of-cell-cycle-checkpoints
#3
Nicholas D Arcy, Brian Gabrielli
Interactions between the decatenation checkpoint and Topoisomerase II (TopoII) are vital for maintaining integrity of the genome. Agents that target this enzyme have been in clinical use in cancer therapy for over 30 years with great success. The types of compounds that have been developed to target TopoII are broadly divided into poisons and catalytic inhibitors. The TopoII poisons are in clinical use as anti-cancer therapies, although in common to most chemotherapeutic agents, they display considerable normal tissue toxicity...
December 5, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27919215/current-strategies-in-modification-of-plga-based-gene-delivery-system
#4
Mohammad Ramezani, Mahboubeh Ebrahimian, Maryam Hashemi
The successful gene therapy has been limited by safe and efficient delivery of nucleic acid to the target cells. Poly (d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) are able to deliver drugs and gene efficiently. This formulation has several advantages in comparison with other formulations including improvement of solubility, stability, controlling of degradation and release of the entrapped agents. For application of PLGA as gene carrier, there exist many challenges. PLGA nanoparticles could protect the encapsulated DNA from in vivo degradation but the DNA release is slowl and their negative charge acts as a barrier to DNA incorporation and delivery...
December 5, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27915991/control-of-inflammatory-bowel-disease-and-colorectal-cancer-by-synthetic-vitamin-d-receptor-ligands
#5
Ichiro Takada, Makoto Makishima
Vitamin D deficiency and insufficiency are associated with an increased risk of cancer, autoimmune disease, inflammation, infection, cardiovascular disease and metabolic disease, as well as bone and mineral disorders. The vitamin D receptor (VDR), a member of the nuclear receptor superfamily, is a receptor for the active form of vitamin D, 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3], and mediates vitamin D regulation of specific target gene expression. The secondary bile acid lithocholic acid, which is produced by intestinal bacteria, is another natural VDR ligand...
December 2, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27915990/possible-molecular-mechanisms-by-which-vitamin-d-prevents-inflammatory-bowel-disease-and-colitis-associated-colorectal-cancer
#6
Zijian Luan, Yiming Ma, Yu Xin, Jiaming Qian, Hongying Wang
It is well accepted that inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, is one of high risk factors for colorectal cancer (CRC). This supports the notion that inflammation plays a key role in cancer development. Epidemiologic studies have shown that vitamin D (Vit D) deficiency is associated with IBD and various types of cancer including colorectal cancer. Clinical trials and mouse models have shown that Vit D is beneficial in preventing or ameliorating inflammation and carcinogenesis...
December 2, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27915989/new-insights-into-vitamin-d-and-autophagy-in-inflammatory-bowel-diseases
#7
Hyun-Woo Suh, Jin Kyung Kim, Tae Sung Kim, Eun-Kyeong Jo
Vitamin D exerts an anti-inflammatory effect in both health and disease. The importance of vitamin D in protection against various inflammatory and metabolic diseases, including inflammatory bowel diseases (IBDs), has been discussed. Considerable data indicate a role for vitamin D in the activation of autophagy, an intracellular renewal system that maintains homeostasis by eliminating large protein aggregates and damaged organelles. Recent studies have demonstrated an intricate interplay between autophagy and the regulation of inflammation, suggesting that autophagy-modulating agents could be used to treat IBDs...
December 2, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27915988/vitamin-d-vdr-probiotics-and-gastrointestinal-diseases
#8
Mei Shang, Jun Sun
Vitamin D is an important factor in regulating inflammation, immune responses, and carcinoma inhibition via action of its receptor, vitamin D receptor (VDR). Recent studies have demonstrated the role of vitamin D/VDR in regulating host-bacterial interactions. Probiotics are beneficial bacteria with the power of supporting or favoring life on the host. In the current review, we will discuss the recent progress on the roles of vitamin D/VDR in gut microbiome and inflammation. We will summarize evidence of probiotics in modulating vitamin D/VDR and balancing gut microbiota in health and gastrointestinal diseases...
December 2, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27915987/sex-differences-in-alcohol-use-disorder
#9
Roberta Agabio, Claudia Pisanu, Gian Luigi Gessa, Flavia Franconi
BACKGROUND: Alcohol use disorder (AUD) is a common and disabling mental disorder associated with a significant burden of medical consequences and high socioeconomic costs. Although a growing number of studies support the existence of sex differences in several aspects of alcohol consumption and AUD, the majority of investigations have been conducted in men. OBJECTIVE: This article was aimed at reviewing sex differences in AUD, focusing on epidemiology, neurobiology, pharmacokinetics, susceptibility to medical consequences, and treatment...
December 1, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27897116/the-molecular-mechanisms-and-the-role-of-hnrnp-k-protein-post-translational-modification-in-dna-damage-repair
#10
Jing Lu, Feng-Hou Gao
DNA damage repair is a kind of cellular self-protection mechanism that some relevant proteins are activated when DNA damage response happens in order to maintain the intracellular function stability and structure integrity. Post-translational modifications (PTMs) of proteins can rapidly confers to them more complicated structure and sophisticated function by covalently combining with different small molecules with target proteins, which in turn plays an important regulatory role in DNA damage repair. It was reported that heterogeneous nuclear ribonucleoprotein K (hnRNP K) could be involved in DNA damage repair process under the regulation of its many post-translational modifications, including methylation, ubiquitination, sumoylation and phosphorylation...
November 29, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27897115/cysteinet-dysregulation-in-muscular-dystrophies-a-pathogenic-network-susceptible-to-therapy
#11
Marcos Arturo Martínez-Banaclocha
BACKGROUND: Muscular dystrophies are inherited disorders characterized by progressive skeletal muscle degeneration without curative therapy. The specific defective protein in each type of muscular dystrophy has been associated with different deleterious factors that contribute to the progression of the disease. Among these factors, the impairment of calcium homeostasis, the ubiquitin-proteasome dysfunction, and the oxidative damage of cellular macromolecules seem to be of central importance...
November 29, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27897114/ureas-applications-in-drug-design-and-development
#12
Ajit Dhananjay Jagtap, Nagendra Bharatrao Kondekar, Amit A Sadani, Ji-Wang Chern
The unique hydrogen binding capabilities of ureas make them an important functional group to make drug-target interactions and thus incorporated in small molecules displaying broad range of bioactivities. The related research and numerous excellent achievements of ureas applicability in drug design for the modulation of selectivity, stability, toxicity and pharmacokinetic profile of lead molecules have become active topic. This review aims to provide insights in to the significance of urea in drug design by summarizing successful studies of various urea derivatives as modulators biological targets (viz...
November 29, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27897117/enantiomeric-resolution-of-rs-naproxen-and-application-of-s-naproxen-in-the-direct-and-indirect-enantioseparation-of-racemic-compounds-by-liquid-chromatography-a-review
#13
Sonika Batra, Ravi Bhushan
(S)-Naproxen (Npx), an α-aryl propionic acid derivative, belongs to class of Non-Steroidal Anti-Inflammatory Drugs and is easily available in pure (S)-form. (S)-Npx has been used as a chiral selector for chromatographic separation of a variety of racemates, using both direct and indirect methods, and has been found to be useful and successful as a basic chiral moiety. This review article describes methods for enantioseparation of (RS)-Npx, development of chiral stationary phases based on (S)-Npx and preparation of novel chiral derivatizing reagents synthesized from (S)-Npx along with their application for enantioseparation of several pharmaceutically important racemates...
November 28, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27881070/pregnancy-specific-%C3%AE-1-glycoproteins-combined-biomarker-roles-structure-function-relationships-and-implications-for-drug-design
#14
Nurbubu T Moldogazieva, Innokenty M Mokhosoev, Alexander A Terentiev
BACKGROUND: Pregnancy specific β1-glycoproteins (PSGs) have long been recognized as trophoblast quality and embryo viability markers. However, biological roles of PSGs remain obscure, and structure/function relationships to other feto-placental proteins as well as implications for drug design have not been reviewed. This review summarizes and discusses advances in 45-year studies of PSGs with focus on the latest achievements and the challenges for future investigations. METHODS: Literature search was performed to review the majority of recent PSG studies with emphasis on usage of high-throughput integrated proteomic profiling technologies, systems biology and bioinformatics approaches that enhance novel biomarker and drug target discovery as well as protein structure/activity analysis...
November 22, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27881069/anti-influenza-virus-effects-of-catechins-a-molecular-and-clinical-review
#15
Kazuke Ide, Yohei Kawasaki, Koji Kawakami, Hiroshi Yamada
Influenza infection and associated epidemics represent a serious public health problem. Several preventive and curative measures exist against its spread including vaccination and therapeutic agents such as neuraminidase inhibitors (e.g., oseltamivir, zanamivir, as well as peramivir and laninamivir, which are licensed in several countries) and adamantanes (e.g., amantadine and rimantadine). However, neuraminidase inhibitor- and adamantane-resistant viruses have been detected, whereas vaccines exhibit strain-specific effects and are limited in supply...
November 22, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27881068/neuron-microglia-interactions-in-motor-neuron-degeneration-the-inflammatory-hypothesis-in-amyotrophic-lateral-sclerosis-revisited
#16
Manuel J Rodríguez, Nicole Mahy
Research into the pathogenesis of amyotrophic lateral sclerosis (ALS) has obtained notable gene discoveries, although, to date, only progress with regard to treatment has been very modest. Currently ALS is considered a multifactorial disease that presents diverse clinical presentations, ranging from a monogenic inherited disease to an autoimmune pathology, and develops with misfolded protein aggregation and neuroinflammation. An important factor related to ALS pathogenesis is the microglial activation associated with degenerative motor neurons...
November 22, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27881067/emerging-nanocarriers-based-approaches-to-diagnose-and-reduce-vascular-inflammation-in-atherosclerosis
#17
Manuela Calin, Ileana Manduteanu
Exploitation of nanotechnology advances in the cardiovascular medicine has led to new approaches for diagnosis and therapy of vascular inflammation associated to cardiovascular diseases. Innovative nanoparticles targeted to the main players in the arterial wall inflammation in atherosclerosis (i.e. inflammatory molecules, immune or resident cells) have been already developed to diagnose and/or reduce excessive vascular inflammation and is eagerly awaited that promising preclinical and early clinical results to boost the approval of the first nanocarrier in this field...
November 22, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27881066/new-insights-emerging-from-recent-investigations-on-human-group-ii-pyridoxal-5-phosphate-decarboxylases
#18
Alessandro Paiardini, Giorgio Giardina, Giada Rossignoli, Carla Borri Voltattorni, Mariarita Bertoldi
Aromatic amino acid, cysteine sulfinic acid, glutamate and histidine decarboxylases, belonging to group II of pyridoxal 5'-phosphate-dependent enzymes, catalyze the synthesis of dopamine/serotonin, hypotaurine, ϒ-aminobutyric acid and histamine, respectively. Considering that these reaction's products are all essential bioactive molecules, group II decarboxylases have been long studied from an evolutionary, biochemical and pharmacological standpoint. Despite the fact that they all belong to a common fold-type, during evolution each decarboxylase has evolved unique structural elements responsible for its substrate specificity...
November 22, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27881065/lipids-at-the-cross-road-of-autoimmunity-in-multiple-sclerosis
#19
Marcella Reale, Silvia Sánchez-Ramón
Multiple sclerosis (MS) is a chronic autoimmune disease that affects the central nervous system (CNS) characterized by demyelination and neurodegeneration, driven by a Th17/Th1-immune response, which afflicts mainly young women. Although MS causes are not completely known, it is notorious that the disease is characterized by an extended focal degradation of the myelin sheath, with ulterior axon and neuronal damage. Lipid molecules play a main dual role in MS, both as target molecules of myelin destruction and as mediators of inflammation...
November 22, 2016: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/27903218/structure-activity-relationship-studies-of-new-marine-anticancer-agents-and-their-synthetic-analogues
#20
Sergey N Fedorov, Valentin A Stonik, Friedemann Honecker, Sergey Dyshlovoy
This review addresses in depth recent structure-activity relationship (SAR) studies of new marine compounds and their synthetic analogues with potential or established anticancer activity, published in 2015.
November 21, 2016: Current Medicinal Chemistry
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