The potential impacts of tylophora alkaloids and their derivatives in modulating inflammation, viral infections, and cancer.
Abstract Cancer chemotherapies or antitumor agents mainly remain the backbone of current treatment based on killing the rapidly dividing cancer cell such as tylophora alkaloids and their analogues which have also demonstrated anticancer potential through diverse biological pathways including regulation of the immune system. The introduction of durable clinically effective monoclonal antibodies, however, unmasked a new era of cancer immunotherapies. Therefore, the understanding of cancer pathogenesis will provide new possible treatment options, including cancer immunotherapy and targeted agents. Combining cytotoxic...
Source: Current Medicinal Chemistry - July 26, 2018 Category: Chemistry Authors: Bach DH, Lee SK Tags: Curr Med Chem Source Type: research

Current highlights about the safety of inorganic nanomaterials in healthcare.
Abstract In recent years inorganic materials are largely present in products intended to health care. Literature gives many examples of inorganic materials used in many health care products, mainly in pharmaceutical field. Silver, zinc oxide, titanium oxide, iron oxide, gold, mesoporous silica, hydrotalcite-like compound and nanoclays are the most common inorganic materials used in nanosized form for different applications in health field. Generally, these materials are employed to realize formulations for systemic use, often with the aim to perform a specific targeting to the pathological site. The nanometric dim...
Source: Current Medicinal Chemistry - July 23, 2018 Category: Chemistry Authors: Perioli L, Pagano C, Ceccarini MR Tags: Curr Med Chem Source Type: research

Potassium Channels: A Big Family, Many Different Targets, Great Pharmacological Opportunities.
PMID: 30014793 [PubMed - in process] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 19, 2018 Category: Chemistry Authors: Martelli A Tags: Curr Med Chem Source Type: research

Pancreatic Cancer Chemoprevention: Challenges and Opportunities.
PMID: 30014794 [PubMed - in process] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 19, 2018 Category: Chemistry Authors: Mohammed A, Rao CV Tags: Curr Med Chem Source Type: research

Perspectives on Rational Drug Design and Therapy for Pediatric Precision Medicine.
PMID: 30014795 [PubMed - in process] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 19, 2018 Category: Chemistry Authors: Stocco G Tags: Curr Med Chem Source Type: research

Synthetic Peptide Libraries. From random mixtures to in vivo testing.
Abstract Combinatorially generated molecular repertoires have been largely used to identify novel bioactive compounds. Ever more sophisticated technological solutions have been proposed to simplify and speed up such process, expanding the chemical diversity space and increasing the prospect to select new molecular entities with specific and potent activities against targets of therapeutic relevance. In this context, random mixtures of oligomeric peptides were originally used and since more than 25 years they represent a continuous source of bioactive molecules with potencies ranging from the subnM to microM concen...
Source: Current Medicinal Chemistry - July 15, 2018 Category: Chemistry Authors: Sandomenico A, Caporale A, Doti N, Cross S, Cruciani G, Chambery A, De Falco S, Ruvo M Tags: Curr Med Chem Source Type: research

The role of matrix Gla protein (MGP) in vascular calcification.
Abstract Matrix Gla protein (MGP) is a vitamin K-dependent protein, which is synthesized in bone and many further mesenchymal cells, which is also highly expressed by vascular smooth 1muscle cells (VSMCs) and chondrocytes. Numerous studies have confirmed that MGP acts as a calcification-inhibitor although the mechanism of action is still not fully understood. The modulation of tissue calcification by MGP is potentially regulated in several ways including direct inhibition of calcium-phosphate precipitation, the formation of matrix vesicles (MVs), the formation of apoptotic bodies (ABs), and trans-differentiation o...
Source: Current Medicinal Chemistry - July 15, 2018 Category: Chemistry Authors: Bjorklund G, Svanberg E, Dadar M, Card DJ, Chirumbolo S, Harrington DJ, Aaseth J Tags: Curr Med Chem Source Type: research

Methodological aspects of phytosterol measurements in biological samples.
Abstract Phytosterol measurement has gained a lot of interest during the last two decades after foods and supplements with added 4-desmethyl phytosterols were recognized and used as effective and safe non-pharmacologic hypocholesterolemic agents, and also after the mechanisms of intestinal absorption and hepatic excretion of sterols were unraveled. In addition, the wide use of serum phytosterols as biomarkers of cholesterol absorption has increased the interest in their measurement. In this review the basic methods are discussed without going into details in the practical operations. The analysis includes first li...
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Gylling H, Simonen P, Kaipiainen L, Wester I Tags: Curr Med Chem Source Type: research

Drug Repurposing in the Development of Anticancer Agents.
CONCLUSION: Drugs could have many off-target effects, and can be intelligently repurposed if the off-target effects can be employed for therapeutic purposes. In cancer, due to the heterogeneity of the disease, often targets are quite diverse, hence a number of already known drugs that interfere with these targets could be deployed or repurposed with appropriate research and development. PMID: 30009698 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Olgen S, Kotra L Tags: Curr Med Chem Source Type: research

The role of adipokines in the establishment and progression of head and neck neoplasms.
Abstract Adipokines constitute a family of protein factors secreted by white adipose tissue (WAT), that regulate the functions of WAT and other sites. Leptin, adiponectin, resistin, are the main adipokines present in serum and saliva, targeting several tissues and organs, including vessels, muscles, liver and pancreas. Besides body mass regulation, adipokines affect glucose homeostasis, inflammation, angiogenesis, cell proliferation and apoptosis, and other crucial cell procedures. Their involvement in tumor formation and growth is well established and deregulation of adipokine and adipokine receptors' expression ...
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Tzanavari T, Tasoulas J, Vakaki C, Mihailidou C, Tsourouflis G, Theocharis S Tags: Curr Med Chem Source Type: research

Quercetin and its Natural Sources in Wound Healing Management.
Abstract Giving a glance to the report Wound Care Market by Product up-to-date at 2017, we can see that wound care market is expected to reach USD 22.01 billion by 2022 from USD 18.35 billion at a CAGR of 3.7%. Numerous are the factors driving the growth of this market, including the increasing prevalence of chronic wounds and acute wounds, increasing aged population, rising R&D activities and advancement in the field of wound care research. Advanced wound management products are accounted for the largest market share in 2017. These evidences meaning that the wound care research represents a Clinical Emergency...
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Polera N, Badolato M, Perri F, Carullo G, Aiello F Tags: Curr Med Chem Source Type: research

Calcium Channel Blockers in Restoration of Endothelial Function: Systematic Review and Meta-Analysis of Randomized Controlled Trials.
CONCLUSION: CCB improved EF to a more prominent extent only if paralleled to TD, while inversely; ACEI and ARB were more effective in augmenting FMD. PMID: 30009701 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Radenkovic M, Stojanovic M, Prostran M Tags: Curr Med Chem Source Type: research

Antimicrobial Peptides: Amphibian Host Defense Peptides.
Abstract Antimicrobial peptides (AMPs) are one of the most common components of the innate immune system that protect multicellular organisms against microbial invasion. The vast majority of AMPs are isolated from the frog skin. Anuran (frogs and toads) skin contains abundant AMPs that can be developed therapeutically. Such peptides are a unique but diverse group of molecules. In general, more than 50% of the amino acid residues form the hydrophobic part of the molecule. Normally, there are no conserved structural motifs responsible for activity, although the vast majority of the AMPs are cationic due to the prese...
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Patocka J, Nepovimova E, Klimova B, Wu Q, Kuca K Tags: Curr Med Chem Source Type: research

Cysteine-Targeted Irreversible Inhibitors of Tyrosine Kinases and Key Interactions.
Abstract Tyrosine kinases are a subgroup of the larger class of protein kinases that transfer phosphate groups from ATP to various amino acid residues. By phosphorylating the tyrosine residues, the tyrosine kinases are responsible for the activation of various proteins through signal transduction cascades, which serves as a ubiquitous mechanism of cell signaling. The frequent success of many tyrosine kinase inhibitors (TKIs) in clinical success and disease-causing mutations in protein kinases suggests that a large number of kinases may represent therapeutically relevant targets. To date, most of the clinical and p...
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Hu C, Dong X Tags: Curr Med Chem Source Type: research

C-cinnamoyl glycosides: an emerging "tail" for the development of selective carbonic anhydrase inhibitors.
This article will review the latest developments in the synthesis and biological activity of these C-glycosides. PMID: 30009704 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 13, 2018 Category: Chemistry Authors: Martinez H, Riafrecha L, Colinas PA Tags: Curr Med Chem Source Type: research

Use of plant sterol and stanol fortified foods in clinical practice.
Abstract Plant sterols and stanols (PS) are natural, non-nutritive molecules that play a structural role in plant membranes similar to that of cholesterol in animal membranes and abound in seeds and derived oils. PS exert their physical effect of interference with micellar solubilization of cholesterol within the intestinal lumen and are marginally absorbed by enterocytes, with negiglible increases in circulating levels. The physiological role of PS in plants and their natural origin and non-systemic action, together with their cholesterol-lowering effect, make them an attractive option as non-pharmacological agen...
Source: Current Medicinal Chemistry - July 8, 2018 Category: Chemistry Authors: Cofan M, Ros E Tags: Curr Med Chem Source Type: research

Sitosterolemia: diagnosis, metabolic and hematological abnormalities, cardiovascular disease and management.
Abstract Sitosterolemia is a recessive inherited metabolic disorder of unknown prevalence, characterized by increased levels of plasma plant sterols. It is caused by 28 and 31 variants in ABCG5 and ABCG8 genes, respectively, and is characterized by a predisposition to hyperabsorption and accumulation of toxic levels of plant sterols in plasma. Its clinical picture is extremely heterogeneous. The main clinical features are tendinous and cutaneous xanthomas, arthritis or arthralgia, premature cardiovascular disease and atherosclerosis. These characteristics are shared with familial hypercholesterolemia (FH), making ...
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Bastida JM, Giros ML, Benito R, Janusz K, Hernandez-Rivas JM, Gonzalez-Porras JR Tags: Curr Med Chem Source Type: research

The Mechanisms behind the Biological Activity of Flavonoids.
Abstract Flavonoids are phenolic compounds widely distributed in the human diet. Their intake has been associated with a decreased risk of different diseases such as cancer, immune dysfunction or coronary heart disease. However, the knowledge about the mechanisms behind their in vivo activity is limited and still under discussion. For years, their bioactivity was associated with the direct antioxidant and radical scavenging properties of phenolic compounds, but nowadays this assumption is unlikely to explain their putative health effects, or at least to be the only explanation for them. New hypotheses about possib...
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Gonzalez-Paramas AM, Ayuda-Duran B, Martinez S, Gonzalez-Manzano S, Santos-Buelga C Tags: Curr Med Chem Source Type: research

Epigenetic metalloenzymes.
Abstract Epigenetics control the expression of genes and is responsible for the cellular phenotypes. The fundamental basis of these mechanisms involves in part the post-translational modifications (PTMs) of DNA and proteins, in particular the nuclear histones. DNA can be methylated or demethylated on cytosine. Histones are marked by several modifications including acetylation and/or methylation, and of particular importance are the covalent modifications of lysine. It exists a balance between addition and removal of these PTMs, leading to three groups of enzymes involved in these processes: the writers adding mark...
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Blanquart C, Linot C, Cartron PF, Tomaselli D, Mai A, Bertrand P Tags: Curr Med Chem Source Type: research

Porous Inorganic and Hybrid Systems for Drug Delivery: Future Promise in Combatting Drug Resistance and Translation to Botanical Applications.
CONCLUSION: The findings of this review confirm the importance of studying and utilizing porous particles for therapeutic delivery. Moreover, we show that the properties of porous particles that make them promising for medicinal drug delivery also make them promising candidates for agro-industrial applications. PMID: 29984645 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Guo J, Mattos BD, Tardy BL, Moody VM, Xiao G, Ejima H, Cui J, Liang K, Richardson JJ Tags: Curr Med Chem Source Type: research

Focusing on the influenza virus polymerase complex: recent progress in drug discovery and assay development.
Abstract Influenza viruses are severe human pathogens that pose persistent threat to public health. Each year more people die of influenza virus infection than that of breast cancer. Due to the limited efficacy associated with current influenza vaccines, as well as emerging drug resistance from small molecule antiviral drugs, there is a clear need to develop new antivirals with novel mechanisms of action. The influenza virus polymerase complex has become a promising target for the development of the next-generation of antivirals for several reasons. Firstly, the influenza virus polymerase, which forms a heterotrim...
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Zhang J, Hu Y, Musharrafieh RG, Yin H, Wang J Tags: Curr Med Chem Source Type: research

The impact of phytosterols on the healthy and diseased brain.
Abstract The central nervous system (CNS) is the most cholesterol-rich organ in mammals. Cholesterol homeostasis is essential for proper brain functioning and dysregulation of cholesterol metabolism can lead to neurological problems. Multiple sclerosis (MS) and Alzheimer's disease (AD) are examples of neurological diseases that are characterized by a disturbed cholesterol metabolism. Phytosterols (PS) are plant-derived components that structurally and functionally resemble cholesterol. PS are known for their cholesterol-lowering properties. Due to their ability to reach the brain, researchers have started to inves...
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Dierckx T, Bogie JFJ, Hendriks JA Tags: Curr Med Chem Source Type: research

Recent Drug-Repurposing-Driven Advances in the Discovery of Novel Antibiotics.
Abstract Drug repurposing is a safe and successful pathway to speed up the novel drug discovery and development processes compared with de novo drug discovery approaches. Drug repurposing uses FDA-approved drugs and drugs that failed in clinical trials, which have detailed information of potential toxicity, formulation, and pharmacology. Technical advancements in the informatics, genomics, and biological sciences account for the major success of drug repurposing in identifying secondary indications of existing drugs. Drug repurposing is playing a vital role in filling the gap in the discovery of potential antibiot...
Source: Current Medicinal Chemistry - July 5, 2018 Category: Chemistry Authors: Konreddy AK, Rani GU, Lee K, Choi Y Tags: Curr Med Chem Source Type: research

Could flavonoids compete with synthetic azoles in diminishing Candida albicans infections?
Abstract Flavonoids are polyphenolic compounds with already confirmed various health benefits. This review will shed light on flavonoids as potential antifungals in Candida albicans infections. C. albicans is opportunistic pathogen able to cause serious health issues due to numerous virulence factors amplifying its pathogenicity. One of the most important virulence factors is Candida ability to form biofilms which are highly resistant to treatment with antifungal drugs; making diminishing of this pathogen even more challenging. This review will focus on current knowledge on individual flavonoid compounds potential...
Source: Current Medicinal Chemistry - June 29, 2018 Category: Chemistry Authors: Smiljkovic M, Kostic M, Stojkovic D, Glamoclija J, Sokovic M Tags: Curr Med Chem Source Type: research

Impact of natural dietary agents on multiple myeloma prevention and treatment: molecular insights and potential for clinical translation.
Abstract Chemoprevention is based on the use of non-toxic, pharmacologically active agents to prevent tumor progression. In this regard, natural dietary agents have been described by the most recent literature as promising tools for controlling onset and progression of malignancies. Extensive research has been so far performed to shed light on the effects of natural products on tumor growth and survival, disclosing the most relevant signal transduction pathways targeted by such compounds. Overall, anti-inflammatory, anti-oxidant and cytotoxic effects of dietary agents on tumor cells are supported either by results...
Source: Current Medicinal Chemistry - June 29, 2018 Category: Chemistry Authors: Raimondi L, De Luca A, Giavaresi G, Barone A, Tagliaferri P, Tassone P, Amodio N Tags: Curr Med Chem Source Type: research

Development and Application of Computational Methods in Phage Display Technology.
CONCLUSION: The current bioinformatics archives, methods and tools reviewed here have benefitted the biopanning community. To develop better or new computational tools, some promising directions are also discussed. PMID: 29956612 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 29, 2018 Category: Chemistry Authors: He B, Derda R, Dzisoo AM, Huang J Tags: Curr Med Chem Source Type: research

Cancer-associated cachexia, reactive oxygen species, and nutrition therapy.
Abstract Cancer-related cachexia (CAC) is a syndrome occurring in many cancer patients, with a detrimental effect on their survival. Recent reports have outlined that the syndrome may be partly explained by the deleterious and pro-inflammatory action of reactive oxygen species (ROS). This review focuses on nutrients that theoretically could counteract the oxidative stress in tumor cells, fundamentally due to their antioxidant activity. The preclinical and clinical results obtained with the nutritional elements selenium, melatonin, taurine, carnosine, coenzyme Q10 (ubiquinone), and omega-3 polyunsaturated fatty aci...
Source: Current Medicinal Chemistry - June 29, 2018 Category: Chemistry Authors: Bjorklund G, Razi MD, Aaseth J, Chirumbolo S, Pen JJ Tags: Curr Med Chem Source Type: research

Latest Updates in Dengue Fever Therapeutics: Natural, Marine, and Synthetic Drugs.
Abstract In this paper, we review the history of Dengue, the mechanism of infection, the molecular characteristics and components of Dengue, the mechanism of entry to the target cells, cyclization of the genome and replication process, as well as translation of the proteins for virus assembly. The major emphasis of this work is on natural products and plant extracts, which were used for as palliative or adjuvant treatment of Dengue. This review article also summarizes latest findings in regards to the marine products as effective drugs to target different symptoms of Dengue. Furthermore, an update on synthetic dru...
Source: Current Medicinal Chemistry - June 29, 2018 Category: Chemistry Authors: Hosseini S, Munoz-Soto RB, Oliva-Ramirez J, Vazquez-Villegas P, Aghamohammadi N, Rodriguez-Garcia A, Martinez-Chapa SO Tags: Curr Med Chem Source Type: research

Electrophysiological characteristics of the migraine brain: current knowledge and perspectives.
Abstract BACKGROUND: Despite pain being its most prominent feature, migraine is primarily a disorder of sensory processing. Electrophysiology-based research in the field has consistently developed over the last fifty years. OBJECTIVE: To summarize the current knowledge on the electrophysiological characteristics of the migraine brain, and discuss perspectives. METHODS: We critically reviewed the literature on the topic to present and discuss articles selected on the basis of their significance and/or novelty. Results Physiologic fluctuations within time, between-subject differences, and methodological is...
Source: Current Medicinal Chemistry - June 27, 2018 Category: Chemistry Authors: Marucco E, Lisicki M, Magis D Tags: Curr Med Chem Source Type: research

State of the Art on Carbonic Anhydrase Modulators for Biomedical Purposes.
Abstract The current review is intended to highlight recent advances in the search of new and effective modulators of the metalloenzymes Carbonic Anhydrases (CAs, EC 4.2.1.1) expressed in (h) humans. CAs reversibly catalyze the CO2 hydration reaction, which is of crucial importance in the regulation of a plethora of fundamental processes at cellular level as well as in complex organisms. The first section of this review will be dedicated to compounds acting as activators of the hCAs (CAAs) and their promising effects on central nervous system affecting pathologies mainly characterized from memory and learning impa...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Bozdag M, Altamimi ASA, Vullo D, Supuran CT, Carta F Tags: Curr Med Chem Source Type: research

Photo-triggered drug delivery systems for neuron-related applications.
Abstract The development of materials, chemistry and genetics have created a great number of systems for delivering antibiotics, neuropeptides or other drugs to neurons in neuroscience research, and have also provided important and powerful tools in neuron-related applications. Although these drug delivery systems can facilitate the advancement of neuroscience studies, there are still limited applications due to various drawbacks, such as difficulty in controlling delivery molecules or drugs to the target region, and trouble of releasing them in predictable manners. The combination of optics and drug delivery syst...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Li W, Lin J, Wang T, Huang P Tags: Curr Med Chem Source Type: research

Circulating Biomarkers In Migraine. New Opportunities For Precision Medicine.
Conclusion The characterization of migraine specific biomarkers would be fundamental in a perspective of precision medicine, enabling risk assessment and tailored treatments. However, speculating on the clinical validity of migraine biomarkers may be premature and controlled clinical trials are presently needed to investigate both the diagnostic and therapeutic value of these biomarkers in migraine. PMID: 29932027 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Ferroni P, Barbanti P, Spila A, Fratangeli F, Aurilia C, Fofi L, Egeo G, Guadagni F Tags: Curr Med Chem Source Type: research

Pharmacokinetic and pharmacogenetic markers of irinotecan toxicity.
CONCLUSIONS: The findings of this review confirm the importance of considering individual patient characteristics to select IRI doses. Currently, the most straightforward approach for IRI dose individualization is UGT1A1 genotyping. However, this strategy is sub-optimal due to several other genetic and environmental contributions to the variable pharmacokinetics of IRI and its active metabolite. The use of dried blood spot sampling could allow the clinical application of complex sampling for the clinical use of limited sampling and population pharmacokinetic models for IRI doses individualization. PMID: 29932028 [PubM...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Hahn RZ, Antunes MV, Verza SG, Perassolo MS, Suyenaga ES, Schwartsmann G, Linden R Tags: Curr Med Chem Source Type: research

Phytosterols and inflammation.
Abstract Besides the well-characterized effect of foods and supplements enriched with plant sterols/stanols on serum LDL-C concentrations, evidence is now emerging that phytosterols exert beneficial effects on non-lipid variables such as inflammatory and oxidative stress markers, coagulation parameters and endothelial function. This makes sterols and stanols an attractive alternative for dietary interventions in cardiovascular disease prevention, particularly in populations at low or medium risk. This review aims to summarize the current knowledge derived from experimental studies and human data on the anti-inflam...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Vilahur G, Ben-Aicha S, Diaz E, Badimon L, Padro T Tags: Curr Med Chem Source Type: research

Energy Metabolism Impairment in Migraine.
Abstract Migraine is a common disabling neurological disorder which is characterised by recurring headache associated with a variety of sensory and autonomic symptoms. The pathophysiology of migraine remains not entirely understood, although many mechanisms involving the central and peripheral nervous system are now becoming clear. In particular, it is widely accepted that migraine is associated with energy metabolic impairment of the brain. The purpose of this review is to present an update overview of the energy metabolism involvement in the migraine pathophysiology. Several biochemical, morphological and magnet...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Cevoli S, Favoni V, Cortelli P Tags: Curr Med Chem Source Type: research

Rational drug design approach of receptor tyrosine kinase type III inhibitors.
Abstract Rational drug design is accomplished through the complementary use of structural biology and computational biology of biological macromolecules involved in disease pathology. Most of the known theoretical approaches for drug design are based on knowledge of the biological targets to which the drug binds. This approach can be used to design drug molecules that restore the balance of the signaling pathway by inhibiting or stimulating biological targets by molecular modeling procedures as well as by molecular dynamics simulations. Type III receptor tyrosine kinase affects most of the fundamental cellular pro...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Kim E, Kim C Tags: Curr Med Chem Source Type: research

Liver Radioembolization: An Analysis of Parameters that Influence the Catheter-Based Particle-Delivery via CFD.
Abstract Radioembolization (RE) is a valuable treatment for liver cancer. It consists of administering radioactive microspheres via an intra-arterially placed catheter with the aim of lodging these microspheres, which are driven by the bloodstream, in the tumoral bed. Even though it is a safe treatment, some radiation-induced complications may arise. In trying to detect or solve the possible incidences that cause nontarget irradiation, simulating the particle-hemodynamics in hepatic arteries during RE via computational fluid dynamics (CFD) tools has become a valuable approach. This paper reviews the parameters tha...
Source: Current Medicinal Chemistry - June 22, 2018 Category: Chemistry Authors: Aramburo J, Anton R, Rivas A, Ramos JC, Sangro B, Bilbao JI Tags: Curr Med Chem Source Type: research

An Overview of the Loading Efficacy of Cationic Lipids with Milk Proteins:A Potential Application for Lipid Delivery.
Abstract In this review, the loading efficacies of helper and cationic lipids cholesterol (CHOL), 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), dioctadecyldimethyl-ammoniumbromide (DDAB) and dioleoylphosphatidylethanolamine (DOPE) with milk β-lactoglobulin, α-casein and β-casein were compared in aqueous solution at physiological conditions. Structural analysis showed that lipids bind milk proteins via hydrophilic, hydrophobic and H-bonding contacts with DOTAP and DDAB forming more stable protein conjugates. Loading efficacy was 30-50% and enhanced with cationic lipids. Lipid conjugation altered...
Source: Current Medicinal Chemistry - June 8, 2018 Category: Chemistry Authors: Chanphai P, Bourassa P, Tajmir-Riahi HA Tags: Curr Med Chem Source Type: research

A Chemical Approach to Overcome Tyrosine Kinase Inhibitors Resistance : Learning from Chronic Myeloid Leukemia.
CONCLUSION: The aim of this review is to furnish an overview and a methodological guideline for the approach and the overcoming of TKIs Resistances. PMID: 29874990 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 6, 2018 Category: Chemistry Authors: Zanforlin E, Zagotto G, Ribaudo G Tags: Curr Med Chem Source Type: research

Phytosterols in cancer: From molecular mechanisms to preventive and therapeutic potentials.
Abstract Cancer is the second leading cause of death worldwide. Compelling evidence supports the hypothesis that the manipulation of dietary components, including plant compounds termed phytochemicals, demonstrates certain important health benefits in humans, including those in cancer. In fact, beyond their well-known cardiovascular applications, phytosterols may also possess anticancer properties, as has been demonstrated by several studies. Although the mechanism of action by which phytosterols (and derivatives) may prevent cancer development is still under investigation, data from multiple experimental studies ...
Source: Current Medicinal Chemistry - June 6, 2018 Category: Chemistry Authors: Blanco-Vaca F, Cedo L, Julve J Tags: Curr Med Chem Source Type: research

Dual Inhibitors as a New Challenge for Cancer Multidrug Resistance Treatment.
CONCLUSION: These findings bring into focus rational anticancer strategies with dual-targeting agents. Most evaluated synthetic and natural drugs showed a great potential in chemosensitization. Further steps in this direction are needed for the optimization of anticancer treatment. PMID: 29874992 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 6, 2018 Category: Chemistry Authors: Stankovic T, Dinic J, Podolski-Renic A, Musso L, Buric SS, Dallavalle S, Pesic M Tags: Curr Med Chem Source Type: research

Emerging Technologies for Cancer Research: towards Personalized Medicine with Microfluidic Platforms and 3D Tumor Models.
Abstract In the present review, we describe three hot topics in cancer research such as circulating tumor cells, exosomes, and 3D environment models. The first section is dedicated to microfluidic platforms for detecting circulating tumor cells, including both affinity-based methods that take advantage of antibodies and aptamers, and "label-free" approaches, exploiting cancer cells physical features and, more recently, abnormal cancer metabolism. In the second section, we briefly describe biology of exosomes and their role in cancer, as well as conventional techniques for their isolation and innovative m...
Source: Current Medicinal Chemistry - June 5, 2018 Category: Chemistry Authors: Turetta M, Ben FD, Brisotto G, Biscontin E, Bulfoni M, Cesselli D, Colombatti A, Scoles G, Gigli G, Del Mercato LL Tags: Curr Med Chem Source Type: research

Ionic Liquid-Like Pharmaceutical Ingredients and Applications of Ionic Liquids in Medicinal Chemistry: Development, Status and Prospects.
CONCLUSION: This review placed emphasis on chemical structures of ILs and their structure-activity relationships in a specific manner, leading to meaningful and valuable related information to some related fields and thus promotes further development and application of various ILs for medicinal chemistry. The deep exploration for key scientific problems is the driving force to propel their theoretical breakthrough and industrial production. PMID: 29874988 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 5, 2018 Category: Chemistry Authors: Tang J, Song H, Feng X, Yohannes A, Yao S Tags: Curr Med Chem Source Type: research

The promising role of plant tannins as bioactive antidiabetic agents.
CONCLUSION: Hence, according to findings of the present review, tannins could be useful for prevention and management of diabetes mellitus and its associated complications and these natural products could be promising compounds for the discovery of new hypoglycemic agents. PMID: 29874989 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 5, 2018 Category: Chemistry Authors: Ajebli M, Eddouks M Tags: Curr Med Chem Source Type: research

The LDL-Receptor and its molecular properties: From theory to novel biochemical and pharmacological approaches in reducing LDL-cholesterol.
Conclusion LDL-R and its molecular properties are involved in lipid homeostasis, so potentially sets the therapeutic goals in cardiovascular patients, which is usually debated. Further research is needed in order to fully understand its properties, as well as to find the potential pharmacological interventions that could be beneficial in cholesterol homeostasis and various morbidities in order to reach the most appropriate therapeutic goal. PMID: 29865996 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - June 3, 2018 Category: Chemistry Authors: Petroglou D, Kanellos I, Savopoulos C, Kaiafa G, Chrysochoou A, Skantzis P, Daios S, Hatzitolios AI, Giannoglou G Tags: Curr Med Chem Source Type: research

Promising alternative therapeutics for oral candidiasis.
CONCLUSION: The findings of this review confirm the importance and the urgency of the development of efficacious therapies for oral candidal infections. PMID: 29852856 [PubMed - as supplied by publisher] (Source: Current Medicinal Chemistry)
Source: Current Medicinal Chemistry - May 31, 2018 Category: Chemistry Authors: Rodrigues CF, Rodrigues ME, Henriques MCR Tags: Curr Med Chem Source Type: research

Coating Matters: Review on Colloidal Stability of Nanoparticles with Biocompatible Coatings in Biological Media, Living Cells and Organisms.
Abstract Within the last two decades, the field of nanomedicine has not developed as successfully as has widely been hoped for. The main reason for this is the immense complexity of the biological systems, including the physico-chemical properties of the biological fluids as well as the biochemistry and the physiology of living systems. The nanoparticles' physico-chemical properties are also highly important. These differ profoundly from those of freshly synthesized particles when applied in biological/living systems as recent research in this field reveals. The physico-chemical properties of nanoparticles are pre...
Source: Current Medicinal Chemistry - May 31, 2018 Category: Chemistry Authors: Schubert J, Chanana M Tags: Curr Med Chem Source Type: research

Modulation of Immuno-biome during radio-sensitization of tumors by glycolytic inhibitors.
Abstract The tumor microenvironment (TME) comprising of stroma and various components of the immune system forms a pro-tumorigenic cocoon around the tumor cells where reprogramming of the metabolism manifesting in Warburg phenotype (enhanced aerobic glycolysis) occurs in tumor as well as non-tumor cells. This reprogramming plays a significant role in suppressing the immune attack on the tumor cells leading to cancer cell survival, proliferation and resistance to therapies. Therefore, there is a considerable interest in developing therapeutic strategies involving metabolic modifiers to improve the efficacy of thera...
Source: Current Medicinal Chemistry - May 31, 2018 Category: Chemistry Authors: Gupta S, Dwarakanath B Tags: Curr Med Chem Source Type: research

Pharmacological Management of Chronic Obstructive Lung Disease (COPD). Focus on Mutations.
CONCLUSIONS: Findings from "omics" trials should be used to learn more about biologic targeted drugs, and to select more specific drugs matching patient's distinctive molecular profile. Specific markers of inflammation such as percentage of eosinophils are important in determining sensitivity/resistance to corticosteroids. Specific gene variations (Single nucleotide polymorphisms: SNPs) may influence drug sensitivity or resistance. Clinicians working in a real-world need to have a suitable interpretation of molecular results together with a treatment guidance and recommendations. Far more translational research i...
Source: Current Medicinal Chemistry - May 31, 2018 Category: Chemistry Authors: Russo P, Lococco F, Kisialiou A, Prinzi G, Lamonaca P, Cardaci V, Fini M Tags: Curr Med Chem Source Type: research

Genome wide approaches to identify protein-DNA interactions.
CONCLUSION: ChIP-chip, ChIP-seq, and ChIP-exo have been the major techniques to study genome-wide in vivo protein-DNA interaction. Due to the rapid development of next-generation sequencing technology, array-based ChIP-chip is deprecated and ChIP-seq has become the most widely used technique to identify transcription factor binding sites in genome-wide. The newly developed ChIP-exo further improves the spatial resolution to single nucleotide. Numerous tools have been developed to analyze ChIP-chip, ChIP-seq and ChIP-exo data. However, different programs may employ different mechanisms or underlying algorithms thus each wil...
Source: Current Medicinal Chemistry - May 29, 2018 Category: Chemistry Authors: Ma T, Ye Z, Wang L Tags: Curr Med Chem Source Type: research