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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/28440185/a-therapeutic-potential-of-animal-%C3%AE-hairpin-antimicrobial-peptides
#1
Tatiana V Ovchinnikova, Pavel V Panteleev, Sergey V Balandin, Vadim T Ivanov
Endogenous antimicrobial peptides (AMPs) are evolutionary ancient molecular factors of innate immunity that play the key role in host defense. Because of the low resistance rate, AMPs have caught extensive attention as possible alternatives to conventional antibiotics. Over the last years, it has become evident that biological functions of AMPs are beyond direct killing of microbial cells. This review focuses on a relatively small family of animal host defense peptides with the β-hairpin structure stabilized by disulfide bridges...
April 24, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28425862/the-impact-of-il-17-in-atherosclerosis
#2
Xinjie Lu
Atherosclerosis is a chronic vascular disease in which atherosclerotic plaques develop in the arterial wall. It is believed that inflammation plays a major role in atherosclerotic formation and progression. Thus, atherosclerosis can be considered as an inflammatory disease of the arterial vessel. Mouse model demonstrated that T and B cell deficiency reduces the atherosclerotic burden in the formation of an atherosclerotic lesion. CD4+ T helper cells (Th), such as Th1 cells known being the major CD4+ T cell subtype found in mouse models of atherogenesis, increase plaque formation caused by oxLDL...
April 19, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413964/sex-genetic-interaction-in-the-risk-for-cerebrovascular-disease
#3
Donatella Pastore, Francesca Pacifici, Barbara Capuani, Raffaele Palmirotta, Chuanhui Dong, Andrea Coppola, Pasquale Abete, Mario Roselli, Paolo Sbraccia, Fiorella Guadagni, Davide Lauro, Tatjana Rundek, David Della-Morte
Cerebrovascular disease (CeVD) is one of the major cause of death and a leading cause of disability worldwide. CeVD is a complex and multifactorial disease caused by the interaction of environment and genetic factors. Women have lower CeVD incidence than men until an advanced age, when the incidence of CeVD rises dramatically in women. Therefore, sex has been validated as an important risk factor in the etiology of CeVD, especially ischemic stroke. Although the importance of sex steroids have been heavily studied in the mechanism of neuronal injury, the experimental and clinical data suggest that hormones do not fully account for male versus female CeVD patterns...
April 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413965/small-molecule-drugs-and-targeted-therapy-for-melanoma-current-strategies-and-future-directions
#4
Carmen Cerchia, Antonio Lavecchia
Malignant melanoma is the most aggressive and life-threatening skin cancer. Melanoma develops in melanocytes and is characterized by a very high tendency to spread to other parts of the body. Its pathogenesis depends on DNA mutations leading to the activation of oncogenes or to the inactivation of suppressor genes. The identification of misregulations in intracellular signal transduction pathways has provided an opportunity for development of mutation-specific inhibitors, which specifically target the mutated signaling cascades...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413963/overview-of-cantharidin-and-its-analogues
#5
Guofang Wang, Jian Dong, Liping Deng
Canthiridin has significant anti-cancer effects and only limited use due to its toxicity. In spite of some side effects such as hematochezia and tenesmus, cantharidin can efficiently inhibit various tumor cell lines, therefore, its importance can never be overemphasized. Several of its analogues show functions similar to cantharidin without high toxicity. In order to utilize cantharidin to treat cancer, some viable methods are found to reduce its side effects. Since cantharidin can inhibit the activity of protein phosphatases, new researches for the inhibition of protein phosphatases have been implemented...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413962/neurochemical-markers-in-the-mammalian-brain-structure-roles-in-synaptic-communication-and-pharmacological-relevance
#6
Christopher L Rees, Charise M White, Giorgio A Ascoli
BACKGROUND: Knowledge of molecular marker (typically protein or mRNA) expression in neural systems can provide insight to the chemical blueprint of signal processing and transmission, assist in tracking developmental or pathological progressions, and yield key information regarding potential medicinal targets. These markers are particularly relevant in the mammalian brain in light of its unsurpassed cellular diversity. Accordingly, molecular expression profiling is rapidly becoming a major approach to classify neuron types...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413961/incretins-and-lipid-metabolism
#7
Vasilis Tsimihodimos, Moses S Elisaf
Backgound: Recent findings indicate that incretin hormones and incretin-based therapies may affect the metabolism of lipoproteins, although the corresponding mechanisms are not clearly defined. OBJECTIVE: To summarize the available data on the mechanisms linking incretins with the characteristics of serum lipoproteins and discuss the clinical implications of these relationships. METHODS: PubMed was searched using the terms "incretins", "GLP-1", "GIP" and "lipids", "dyslipidemia", "triglycerides", "apolipoprotein B48"...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413960/circulating-ace2-in-cardiovascular-and-kidney-diseases
#8
Lidia Anguiano Gómez, Marta Riera Oliva, Julio Pascual Santos, María José Soler
Angiotensin converting enzyme(ACE) 2 is a homologue of ACE that catalyzes the conversion of Angiotensin(Ang) II into Ang1-7, which induces vasodilation, anti-fibrotic, anti-proliferative and anti-inflammatory effects. Given that ACE2 counterbalances the effects of Ang II, it has been proposed as a biomarker in kidney disease patients. Circulating ACE2 has been studied in human and experimental studies under physiological and pathological conditions and different techniques have been assessed to determine its enzymatic activity...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413959/chemopreventive-properties-of-tolfenamic-acid-a-mechanistic-review
#9
David Feldman, Elizabeth Leahy, Seong-Ho Lee
Tolfenamic acid is one of the conventional non-steroidal anti-inflammatory drugs (NSAIDs) commonly used for the treatment of inflammation, migraines and pain. There has been a growing body of experimental evidence that tolfenamic acid possesses anti-cancer activity. However, in order to develop a therapeutic strategy using tolfenamic acid for the treatment of cancer, further research is required to highlight reliable cellular and molecular mechanisms of anti-cancer properties. Tolfenamic acid has been shown to alter the expression of several genes that represent cancer hallmarks including apoptosis, growth arrest, angiogenesis and metastasis...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413958/anti-fatigue-effects-of-active-ingredients-from-traditional-chinese-medicine-a-review
#10
Si-Si Zhou, Jian-Guo Jiang
Fatigue, a phenomenon which is believed to be caused by body exercise, can lead to the failure of predetermined exercise intensity maintenance and sport ability declination. The usage of traditional Chinese medicine (TCM) in the treatment of fatigue has long been practiced in clinical and showed significant effects. This article covers related literatures in recent years and sorts the effective ingredients from TCM for treating fatigue into a few categories including alkaloids, saponins, polysaccharides, polyphenols, polypeptide, terpene, proteins and other active ingredients...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413957/sulfur-containing-acridine-derivatives-in-preclinical-studies-with-cancer-cell-lines
#11
Salem Othman, Kožurková Mária
The possible use of acridines as anticancer agents was first considered in the 1920´s. Since then, a large number of acridine drugs have been tested as antitumour agents, including compounds containing sulphur on the acridine chromophore. In this review, we will discuss recent studies which have investigated the anticancer activity of this class of acridine derivatives.
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28413956/structure-roles-and-inhibitors-of-a-mitotic-protein-kinase-haspin
#12
Katrin Kestav, Asko Uri, Darja Lavogina
Background Haspin (haploid germ cell-specific nuclear protein kinase) is an atypical serine/threonine-protein kinase that was for a long time considered an inactive pseudokinase due to low degree of structural homology of Haspin with the 'classical' protein kinases. However, the discovery of Haspin-catalyzed phosphorylation of histone H3 at Thr3 residue unveiled importance of Haspin in mitosis and provided yet another link between mitotic phosphorylation pathways and chromatin modifications. Results In this review of 111 publications, we have (1) briefly summarized catalytic properties and physiological roles of Haspin, (2) focussed on the architecture of Haspin and mechanisms behind its substrate recognition, (3) provided detailed insight into the advances in the development and characterization of Haspin-selective inhibitors, and (4) given overview of inhibitor scaffolds that despite targeting other protein kinases feature Haspin as a common off-target...
April 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28412903/phage-life-cycles-behind-bacterial-biodiversity
#13
Tomasz Olszak, Agnieszka Latka, Bartosz Roszniowski, Miguel Angel Valvano, Zuzanna Drulis-Kawa
Bacteriophages (phages or bacterial viruses) are the most abundant biological entities in our planet; their influence reaches far beyond the microorganisms they parasitize. Phages are present in every environment and shape up every bacterial population in both active and passive ways. They participate in the circulation of organic matter and drive the evolution of microorganisms by horizontal gene transfer at unprecedented scales. The mass flow of genetic information in the microbial world influences the biosphere and poses challenges for science and medicine...
April 13, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28412902/nanosafety-towards-safer-nanoparticles-by-design
#14
Neus G Bastús, Víctor Puntes
The continuous development of Nanotechnology is progressively introducing nanoparticles into society. However, little is known about the safety of nanoparticles and functions of engineered nanomaterials, in particular how the physicochemical properties of the materials relate to mechanisms of injury at the nano-bio interface. While comprehensive knowledge on the potential toxicity of NPs is still lacking, as time goes by and research in the field continues, different aspects, such as interactions with the immune system, perturbation of cellular membranes, transportation of toxic moieties and others are emerging as potentially hazardous aspects of NPs...
April 13, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28403788/effect-of-metformin-and-statin-use-on-survival-in-pancreatic-cancer-patients-a-systematic-literature-review-and-meta-analysis
#15
Jian-Yu E, Judith M Graber, Shou-En Lu, Yong Lin, Grace Lu-Yao, Xiang-Lin Tan
BACKGROUND AND OBJECTIVE: Current epidemiological studies report conflicting results for the effect of statin or metformin on pancreatic cancer overall survival. This literature review and meta-analysis summarizes the studies reporting an association between statin or metformin use and overall survival of pancreatic cancer patients. METHODS: We systematically searched for studies about the association between statin or metformin use and pancreatic cancer overall survival in electronic databases (PubMed, ISI Web of Science, MEDLINE, Cochrane, Scopus, Google Scholar)...
April 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28403790/molecular-design-and-medicinal-applications-of-nano-nitric-oxide-delivery-systems
#16
Kim Truc Nguyen, Zhouran Wu, Tiantian Huang, Chor Yong Tay
Nitric oxide (NO) regulates numerous biological processes that are important in the maintenance of homeostatic balance in the human body. Due to its innate biological significance, much effort has been vested to exploit NO as a pharmaceutical agent in recent years. The key to fully harness NO's therapeutic potential will require the innovative integration of the NO releasing molecules (NORMs) with cytocompatible nano-scale carriers so that controlled spatiotemporal delivery of NO to targeted diseases sites can be attained...
April 7, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28403789/metaflammation-tissue-specific-alterations-of-the-nlrp3-inflammasome-platform
#17
Raffaella Mastrocola, Manuela Aragno, Giuseppe Alloatti, Massimo Collino, Claudia Penna, Pasquale Pagliaro
In the last decades, the extension of life expectancy and the increased consumption of foods rich in saturated fats and added sugars have exposed the general population to emerging health problems. The prevalence of metabolic syndrome (MS), composed of a cluster of factors as obesity, dyslipidemia, hyperglycemia, and hypertension, is rapidly increasing in industrialized and developing countries leading to precocious onset of age-related diseases. Indeed, oxidative stress, accumulation of advanced glycation endproducts, and a chronic low-grade inflammation are common features of MS and physiological ageing...
April 7, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28403787/role-of-tissue-renin-angiotensin-system-and-the-chymase-angiotensin-1-12-axis-in-the-pathogenesis-of-diabetic-retinopathy
#18
Mohammad Shamsul Ola, Abdullah S Alhomida, Carlos M Ferrario, Sarfaraz Ahmad
Diabetic retinopathy (DR) is a major diabetes complication and the leading cause for vision loss and blindness in the adult human population. Diabetes, being an endocrinological disorder dysregulate a number of hormonal systems including the renin angiotensin system (RAS), which thereby may damage both vascular and neuronal cells in the retina. Angiotensin II (Ang II), an active component of the RAS is increased in diabetic retina, and may play a significant role in neurovascular damage leading to the progression of DR...
April 7, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28403786/immune-checkpoint-inhibitors-and-cardiac-toxicity-an-emerging-issue
#19
Gilda Varricchi, Giancarlo Marone, Valentina Mercurio, Maria Rosaria Galdiero, Domenico Bonaduce, Carlo G Tocchetti
Although survival of patients with different types of cancer has improved, cardiotoxicity induced by anti-neoplastic drugs remains a critical issue. Cardiac dysfunction after treatment with anthracyclines has historically been a major problem. However, also targeted therapies and biological molecules can induce reversible and irreversible cardiac dysfunction. Cancer immunotherapies over the last years have revolutionized the clinical management of a wide spectrum of solid and hematopoietic malignancies previously endowed with poor prognosis...
April 7, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28393692/nanostructures-for-ph-sensitive-drug-delivery-and-magnetic-resonance-contrast-enhancement-systems
#20
Xiao Sun, Guilong Zhang, Zhengyan Wu
According to the differences of microenvironments between tumors and healthy tissues, if the anticancer drugs or magnetic resonance contrast agents (MRCAs) can be controlled to precisely match physiological needs at targeted tumor sites, it is expected to acquire better therapeutic efficacy and more accurate diagnosis. Over the decade, stimuli-responsive nanomaterials have been a research hotspot for cancer treatment and diagnosis because they show many excellent functions, such as in vivo imaging, combined targeting drug delivery and systemic controlled release, extended circulation time, etc...
April 6, 2017: Current Medicinal Chemistry
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