Aging has serious consequences on skeletal muscle. ‘Sarcopenia’, the progressive loss of muscle mass and associated muscle weakness during elderly, affects radically the functional capacity and general health in adult people and renders frail elders susceptible to serious injury from sudden falls and fractures and at risk for losing their functional independence. There is a vital need to recognise the molecular mechanisms and regulatory factors, underlying age-related muscle wasting and to develop therapeutic strategies that can attenuate, prevent, or finally reverse sarcopenia. In this context, sexual hormones play a key role.
The book, SEX STEROIDS AND APOPTOSIS IN SKELETAL MUSCLE: MOLECULAR MECHANISMS, written by Dr. Andrea Vasconsuelo aims to provide a new way to perceive the role of sex hormones in skeletal muscle. The book present in integrated form the latest information on sarcopenia and its relation with apoptosis, from leading researchers studying the cellular and molecular mechanisms underlying age-linked changes in skeletal muscle emphasising on the role of satellite cells. The authors succeed to explain, how hormones are involved in muscle homeostasis and in the regulation of apoptosis process and how these two functions connect to maintain a healthy muscle or to trigger pathologies. Therefore, the goal of this work is the combination of that information focusing on the molecular level and resulting in the clarification of molecular mechanisms implicated in skeletal muscle aging; when apoptosis is more intense and sex hormones levels decline. Very interesting, the book contains a chapter describing molecular structure of phytoestrogens and their action on sex steroids receptors. In addition, it is possible to emphasize the drafting writing promoting easy and pleasant reading, numerous and careful documentation, high quality images of the authors’ experiments and comprehensive and updated bibliography. This ebook is of interest to graduates and postgraduates in the fields of medicine and biochemistry, researchers of different aspects of ageing biology and people of the pharmaceutical, and health-care industry. Read out the full version here.
ASHITA SHARMA, MANISH KUMAR, SARWINDERJEET KAUR, AVINASH KAUR NAGPAL
Environmental contaminants are constantly increasing in the environment due to the ill planned economic development. Increase in degenerative diseases as a result of continuous exposure to environmental contaminants is posing a serious threat to mankind. While living in such an environment, it has become an absolute necessity to find ways to enhance the protective nature of human metabolic response against the exposure to carcinogens. Various phytochemicals were considered as nectar against many degenerative diseases in ancient civilizations. Modern science is also making efforts to understand the protective effects of natural products. There is a need to compile the information about pollutants which can damage mankind and the protectants to safeguard our existence. The book is a unique and well-arranged compilation of these important aspects.
The first section of the book covers various sources and effects of emerging contaminants in our ambient environment. Environmental contaminants are associated with an increase in incidences of various types of cancers. The chapter entitled “Environmental risk and cancer” covers all such pollutants in detail. Due to the emergence of various contaminants, it has also become important for scientific community to assess the toxicity of various chemical agents present in the environment. Next chapters of the book suggest various plant and bacterial bioassays which could be used to analyze the toxic potential. Injudicious urbanization and economic development have increased the concentrations of some toxins into the environment which could have been prevented if judiciously used; pesticides and biphenyls are perfect examples. In the second section, editors have tried to compile the information about various natural products and their protective effects against carcinogenic potential of environmental contaminants. The metabolic link between plant products and cancer chemoprevention is also summarized well in one of the chapters in the book. The volume of Environmental Contaminants and Natural Products is a concise and well-organized handbook for researchers working in the field. Read out the full version here.
Author(s): Neva Alasağ*, Erol Şener, Dilek Doğrukol-Ak.
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Current Pharmaceutical Design publishes timely in-depth/mini reviews and research articles from leading pharmaceutical researchers in the field, covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area guest edited by an acknowledged authority in the field.
Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design including: medicinal chemistry, pharmacology, drug targets and disease mechanism.
Articles from the journal: Current Pharmaceutical Design; Volume: 25, Issue: 3
Kinetoplastid and apicomplexan parasites include protozoans which are responsible for human diseases, and cause a serious impact on human health and the socioeconomic growth of developing countries. Chemotherapy is the main option to control these pathogenic organisms. The organisms’ nuclear metabolism is considered a promising area for the provision of antimicrobial therapeutic targets.
The viability of parasitic protozoa is severely diminished by imparing thymidylate (dTMP) biosynthesis. The absence of enzymatic activities which are specifically involved in the formation of dTMP (e.g. dUTPase, thymidylate synthase, dihydrofolate reductase or thymidine kinase) results in decreased de-oxythymidine triphosphate (dTTP) levels and the so-called thymineless death.
In this process, the ratio of deoxyuridine triphosphate (dUTP) as compared to dTTP in the cellular nucleotide pool has a crucial role. A high dUTP/dTTP ratio leads to uracil misincorporation into DNA, which then leads to the activation of DNA repair pathways, DNA fragmentation and eventually cell death.
For the identification and development of drugs, the essential character of dTMP synthesis has stimulated interest. These agents specifically block the biochemical steps involved in thymine nucleotide formation.
The review covers available literature related to drug discovery of agents targeting thymidylate biosynthesis in kinetoplastid (genera Trypanosoma and Leishmania) and apicomplexan (Plasmodium spp and Toxoplasma gondii) protozoans.The most relevant findings concerning novel inhibitory molecules with anti-parasitic activity against these human pathogens are presented in the review. Read full press release to find out more at: https://www.eurekalert.org/pub_releases/2018-12/bsp-tk122618.php
This article by Dr. Dolores Gonzalez Pacanowska et al. is published in Current Medicinal Chemistry, 2018. The article is available from the following link: http://www.eurekaselect.com/165707
Author(s): Apilak Worachartcheewan*, Napat Songtawee, Suphakit Siriwong, Supaluk Prachayasittikul*, Chanin Nantasenamat, Virapong Prachayasittikul.
Background: Human immunodeficiency virus (HIV) is an infective agent that causes an acquired immunodeficiency syndrome (AIDS). Therefore, the rational design of inhibitors for preventing the progression of the disease is required.
Objective: This study aims to construct quantitative structure-activity relationship (QSAR) models, molecular docking and newly rational design of colchicine and derivatives with anti-HIV activity.
Methods: A data set of 24 colchicine and derivatives with anti-HIV activity were employed to develop the QSAR models using machine learning methods (e.g. multiple linear regression (MLR), artificial neural network (ANN) and support vector machine (SVM)), and to study a molecular docking.
Results: The significant descriptors relating to the anti-HIV activity included JGI2, Mor24u, Gm and R8p+ descriptors. The predictive performance of the models gave acceptable statistical qualities as observed by correlation coefficient (Q2) and root mean square error (RMSE) of leave-one out cross-validation (LOO-CV) and external sets. Particularly, the ANN method outperformed MLR and SVM methods that displayed LOO−CV 2 Q and RMSELOO-CV of 0.7548 and 0.5735 for LOOCV set, and Ext 2 Q of 0.8553 and RMSEExt of 0.6999 for external validation. In addition, the molecular docking of virus-entry molecule (gp120 envelope glycoprotein) revealed the key interacting residues of the protein (cellular receptor, CD4) and the site-moiety preferences of colchicine derivatives as HIV entry inhibitors for binding to HIV structure. Furthermore, newly rational design of colchicine derivatives using informative QSAR and molecular docking was proposed.
Conclusion: These findings serve as a guideline for the rational drug design as well as potential development of novel anti-HIV agents. To read out more, please visit: http://www.eurekaselect.com/165617/article