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Current Medicinal Chemistry

Silvia Riondino, Fiorella Guadagni, Vincenzo Formica, Patrizia Ferroni, Mario Roselli
Venous thromboembolism (VTE) is a commonly diagnosed multifactorial condition with significant morbidity and mortality, occurring in up to 20% of cancer patients. Indeed, patients with cancer are in a higher pro-thrombotic state due to alterations in their haemostatic-coagulative system, stasis and blood flow slowdown, endothelial dysfunction, vascular inflammation and platelet activation. Moreover, several cancer-dependent factors can sum up to trigger a first episode of VTE or to cause its recurrence in the course of anticoagulant treatment...
October 18, 2016: Current Medicinal Chemistry
David A Winkler
Nanoparticles are finding many applications in medicine and other field like photonics. Magnetic nanoparticles have additional advantages in medicine over non-magnetic hard nanoparticles, as their magnetic properties make them ideal for hyperthermic applications in therapy and for sensitive diagnostic imaging applications. I review the literature on computational models of the magnetic properties of nanoparticles specifically. Such models have the potential to accelerate the design of magnetic nanoparticles for medical applications...
October 18, 2016: Current Medicinal Chemistry
Ahu Gümrah Dumanlı
Cellulose is a natural linear biopolymer, which constitutes through the assembly of cellulose nanofibrils in a hierarchical order. Nanocelluloses in particular show great promise as a cost-effective advanced material for biomedical applications because of their biocompatibility, biodegradability, and low cytotoxicity. Moreover, with their chemical functionality they can be easily modified to yield useful products. While nature uses the hierarchical nanostructure of the cellulose as the load-bearing constituent in plants, a significant amount of research has been directed toward the fabrication of advanced cellulosic materials with various nanostructures and functional properties...
October 14, 2016: Current Medicinal Chemistry
Shigeo Ohba, Yuichi Hirose
Glioblastomas are the most aggressive of all gliomas and have the worst prognosis, with 5-year survival rates of less than 10%. Temozolomide (TMZ) is a DNA-methylating agent. Now that TMZ is available, the standard treatment is to resect as much of the tumor as possible without inducing unacceptable neurologic deficits, followed by treatment with radiation and TMZ. TMZ has also been used for maintenance therapy. Recently, bevacizumab, which is a monoclonal antibody to vascular endothelial growth factor, has been used for the initial treatment of glioblastomas and for the treatment of recurrent glioblastomas...
October 14, 2016: Current Medicinal Chemistry
Maria Rosaria Carratù, Anna Signorile, Domenico De Rasmo, Antonia Reale, Angelo Vacca
BACKGROUND: The serine-threonine protein phosphatase 2A (PP2A) regulates multiple cell signaling cascades and its inactivation by viral oncoproteins, mutation of specific structural subunits or upregulation of the cellular endogenous inhibitors may contribute to malignant transformation by regulating specific phosphorylation events. Pharmacological modulation of PP2A activity is becoming an attractive strategy for cancer treatment. Some compounds targeting PP2A are able to induce PP2A reactivation and subsequent cell death in several types of cancer...
October 14, 2016: Current Medicinal Chemistry
Norma Alva, Ronald Alva, Teresa Carbonell
In clinical and experimental settings, a great deal of effort is being made to protect cells and tissues against harmful conditions and to facilitate metabolic recovery following these insults. Much of the recent attention has focused on the protective role of a natural form of sugar, fructose 1,6-bisphosphate (F16bP). F16bP is a high-energy glycolytic intermediate that has been shown to exert a protective action in different cell types and tissues (including the brain, kidney, intestine, liver and heart) against various harmful conditions...
October 14, 2016: Current Medicinal Chemistry
Laura Martelli, Laurent Peyrin-Biroulet
BACKGROUND: Anti-tumor necrosis factor (anti-TNF) monoclonal antibodies have revolutionized the treatment of inflammatory bowel diseases (IBD). However, because of their complexity, their production is expensive contributing to their high price. As the patent protection of these therapies has expired in several countries, biosimilars have been developed to reduce the healthcare costs. The aim of this article is to review the literature on the safety, efficacy and immunogenicity of biosimilars in IBD...
October 14, 2016: Current Medicinal Chemistry
Jasna Jančić, Vesna Đurić, Nikola Ivančević, Blažo Nikolić, John N van den Anker, Janko Samardžić
The serine/threonine kinase mechanistic target of rapamycin (mTOR) is an important sensor of the cellular energy condition which, at the same time, represents a kind of master switch between anabolic and catabolic cellular processes. Tuberous sclerosis complex (TSC) is a genetic disease which is considered to be a prototype of a dysregulated mTOR signaling pathway. The dysregulated mTOR pathway in TSC leads to characteristic structural and physiologic abnormalities in multiple organs. In this review we focus on the pharmacological properties of mTOR inhibitors and clinical investigations of mTOR inhibitors for two important neurological TSC manifestations: subependymal giant cell astrocytomas (SEGAs) and epilepsy...
October 12, 2016: Current Medicinal Chemistry
Amirhossein Sahebkar, Matteo Pirro, Željko Reiner, Arrigo Cicero, Gianna Ferretti, Mario Simental-Mendía, Luis E Simental-Mendía
BACKGROUND: Plasma homocysteine is an independent non-traditional risk factor for atherosclerotic cardiovascular disease. The impact of statin therapy on plasma homocysteine is not conclusive. OBJECTIVE: To evaluate the effect of statin therapy on plasma homocysteine concentrations in a systematic review and meta-analysis of controlled clinical trials. The secondary aim was to assess the comparative effect of statins versus fibrates on plasma homocysteine levels in head-to-head trials...
October 7, 2016: Current Medicinal Chemistry
Gennady M Verkhivker
Protein kinases are versatile molecule switches that govern functional processes in signal transduction networks and regulate fundamental biological processes of cell cycle and organism development. The continuous growth of biological information and a remarkable breath of structural, genetic, and pharmacological studies on protein kinase genes have significantly advanced our knowledge of the kinase activation, drug binding and allosteric mechanisms underlying kinase regulation and interactions in signaling cascades...
October 6, 2016: Current Medicinal Chemistry
M K Md Arshad, M F M Fathil, Subash C B Gopinath, A R Ruslinda, M Nuzaihan M N, H Y Lam, U Hashim
Cardiovascular disease (CVD) is a major threat to global health, estimated to be the cause 30 % (17.3 million in 2008) of deaths every year, and the number of deaths caused by CVD is expected to increase further, reaching 23.3 million by 2030. Hence, there is a growing demand for simpler sample extraction, rapid screening results, and intervention of the subsequent analysis in emergency units. In this paper, we reviewed CVD biomarkers in blood- and saliva-based specimens. The history of cardiac biomarkers indicates that in the beginning, cardiac troponin I (cTnI) was a widely accepted 'gold standard' marker due to its high specificity and selectivity...
October 4, 2016: Current Medicinal Chemistry
Gustavo Tadeu Volpato, Rafaianne Queiroz Moraes-Souza, Thaigra Sousa Soares, Thais Leal-Silva, Débora Cristina Damasceno
Diabetes mellitus is a syndrome of great importance that affects an increasing number of people every day. In particular, diabetes is a common and important disease during pregnancy and is marked by complications, both fetal and maternal, that increase the risks of morbidity and mortality for diabetic pregnant women and their offspring. Drugs such as insulin and hypoglycemic drugs are given to treat diabetes, but regular exercise and adequate diet have also been indicated. Furthermore, coadjutant therapies such as medicinal plants are popularly used to reduce diabetes-induced hyperglycemia, either within or outside the context of pregnancy...
October 3, 2016: Current Medicinal Chemistry
Susana Casal, Irene Rebelo
beverages, prepared in a multitude of ways around the world, are increasingly part of our daily lives. Although considered an unhealthy beverage for decades, is increasingly the headline of medical journals in association with a reduced risk for several diseases. What if this beverage could give us pleasure, while modulating mood and lowering the risk for several diseases of the modern society, including type 2 diabetes (T2D)? Based on the most recent epidemiological and research data, long-term consumption of beverages is associated with a lower risk of developing T2D in healthy individuals, probably involving multiple mechanisms, with interventions on glucose homeostasis, antioxidant activity, and inflammatory biomarkers...
October 3, 2016: Current Medicinal Chemistry
Flavia Franconi, Ilaria Campesi
Sex is one of several factors influencing pharmacological responses, but research on its effects on pharmacokinetics and pharmacodynamics, although emerging remarkably, remains poor and contains many methodological issues. In this review, the current state of knowledge about sex differences in pharmacokinetics and some hints to pharmacogenomics were evaluated. Moreover, considering that many pharmacological responses are monitored through biomarkers, the influence of sex on some biomarkers has been reported...
October 3, 2016: Current Medicinal Chemistry
Jianqiong Yang, Haiqing Liu, Linfu Li, Hai Liu, Weimei Shi, Xiaoliang Yuan, Longhuo Wu
IRE1 signaling is the most evolutionarily conserved branch in the UPR. IRE1 is an ER stress sensor and provides a structure-based platform for the unfolded proteins docking, which causes the luminal domain conformational change and oligomerization. This self-association of IRE1 facilitates the phosphorylation of activation loop, which unlocks the auto-inhibition in the kinase domain. The activating mechanistic cascade is thus initiated to induce DFG-in conformational change and movement of αC-helix to the active site...
September 27, 2016: Current Medicinal Chemistry
Bensu Karahalil
Traditional technologies using reductionist approach are relatively insufficient to solve problems in a biological system. Rather than a reductionist approach, system biology uses a holistic and integrative approach to better figure out the whole process. Both qualitatively and quantitatively of biological system provide information about diseases, toxicities, therapies etc. Omics technologies, which system biology bring, are valuable tools for comprehensive analyses. Automated DNA sequencers enabled the sequencing of genomes; microarray and mass spectrometry analysis permit global transcriptional profiling and lead to large-scale proteomic and metabolomics analysis...
September 26, 2016: Current Medicinal Chemistry
Weichao Sun, Liling Tang
Mdm2 is a well studied oncogene and has been reported to be closely related to chemoresistance in different manners. In this article, we discuss the current knowledge of mdm2's function in drug resistance, the novel relationship between MDM2 and Akt phosphorylation, the role of Akt signaling pathway in epithelial-mesenchymal transition, and the positive correlation among MDM2, epithelial-mesenchymal transition and drug resistance. We propose a possible pathway by which MDM2 increases drug resistance through inducing epithelial-mesenchymal transition independent of p53...
September 26, 2016: Current Medicinal Chemistry
Mihad Ibrahim, Rana Sabouni, Ghaleb A Husseini
Cancer is the uncontrolled growth of cells in the body and is considered as one of the major causes of death globally. There are several cytotoxic chemotherapeutic agents used to treat cancer including methotrexate, 5-fluorouracil, cisplatin, tamoxifen, doxorubicin and others. Although billions of dollars have been spent on cancer research to develop these chemotherapies, it still remains a major illness for mankind partly due to the shortcomings of these therapies. These shortcomings include low targeting specificity, severe side effects (due to high doses) and poor pharmacokinetics...
September 26, 2016: Current Medicinal Chemistry
Mateja Prunk, Janko Kos
Proteases are involved in a variety of processes associated with tumor development and progression. Because of their integral role in extracellular matrix and basal lamina degradation they play important roles in cancer cell migration, invasion, angiogenesis and metastasis. They are also involved in cancer cell signaling, the epithelial-mesenchymal transition, the antitumor immune response, cell de-differentiation and cancer stem cell remodeling. Their involvement in pro-tumorigenic processes makes them interesting targets for anticancer therapy...
September 22, 2016: Current Medicinal Chemistry
Koen Muylaert, Martyna Jatczak, Sven Mangelinckx, Christian V Stevens
The immense amount of research on benzodiazepines resulted also in the synthesis of heterocycle-fused diazepine derivatives with potential pharmacological activity. Pyridoazepines are recognized to be active in the central nervous system and have a comparable activity to the well-known benzodiazepines. This makes the synthesis and the study of pyridodiazepines also an important research topic. This review comprises the synthesis and activity of pyridodiazepines, pyridooxazepines and pyridothiazepines. Although these structures have a great similarity with benzodiazepines, much less work has been published on their synthesis or derivatization...
September 20, 2016: Current Medicinal Chemistry
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