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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/28820072/structural-design-and-physicochemical-foundations-of-hydrogels-for-biomedical-and-pharmaceutical-applications
#1
Qingyong Li, Wen Li, Jie Xu, Zhengxiang Ning, Jiaoyan Ren, Wenzhen Liao
Biomedical research, known as medical research, is conducive to support and promote the development of knowledge in the field of medicine. Hydrogels have been extensively used in many biomedical fields due to theirs highly absorbent and flexible properties. The smart hydrogels, especially, can respond to a broad range of external stimuli such as temperature, pH value, light, electric and magnetic fields. With excellent biocompatibility, tunable rheology, mechanical properties, porosity, and hydrated molecular structure, hydrogels are considered as promising candidate for simulating local tissue microenvironment...
August 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28820071/antibody-fragments-as-potential-biopharmaceuticals-for-cancer-therapy-success-and-limitations
#2
Roman V Kholodenko, Daniel V Kalinovsky, Igor I Doronin, Eugene D Ponomarev, Irina V Kholodenko
Monoclonal antibodies (mAbs) are an important class of therapeutic agents approved for the therapy of many types of malignancies. However, in certain cases applications of conventional mAbs have several limitations in anticancer immunotherapy. These limitations include insufficient efficacy and adverse effects. The antigen-binding fragments of antibodies have a considerable potential to overcome the disadvantages of conventional mAbs, such as poor penetration into solid tumors and Fc-mediated bystander activation of the immune system...
August 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28820070/muc1-story-great-expectations-disappointments-and-the-renaissance
#3
Mikhail A Rubtsov, Marina S Syrkina, Yegor S Vassetzky
In the course of studying human mucin MUC1, an attitude towards this molecule has been changing time and again. Initially, the list of presumable functions of MUC1 was restricted to protecting and lubricating epithelium. To date, it is assumed to play an important role in cell signaling as well as in all stages of oncogenesis, from malignant cell transformation to tumor dissemination. The story of MUC1 is full of hopes and disappointments. However, the scientific interest to MUC1 has never waned, and the more profoundly it has been investigated, the clearer its hidden potential turned to be disclosed...
August 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28820069/apixaban-effective-and-safe-in-preventing-thromboembolic-events-in-patients-with-atrial-fibrillation-and-renal-failure
#4
Francesca Cortese, Pietro Scicchitano, Michele Gesualdo, Gabriella Ricci, Santa Carbonara, Carlo Franchini, Brigida Immacolata Pia Schiavone, Filomena Corbo, Marco Matteo Ciccone
Thromboembolic events, principally stroke, represent among the leading causes of morbidity and mortality of subjects with atrial fibrillation, with an incidence about 5 times higher compared to healthy subjects. Chronic kidney disease, frequently associated with atrial fibrillation, determines itself a further increase of thromboembolic events, bleeding and mortality. In addition, the presence of renal failure complicates the pharmacological management of these patients, mainly due to the side effects of antiarrhythmic and anticoagulant drugs with renal excretion, due to their accumulation...
August 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28820068/known-triterpenes-and-their-derivatives-as-scaffolds-for-the-development-of-new-therapeutic-agents-for-cancer
#5
Gregorio Peron, Giovanni Marzaro, Stefano Dall'Acqua
Plants produce several bioactive secondary metabolites whose are used as therapeutic agents to treat various diseases, among them cancer. Triterpenes are a category of secondary metabolites that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells. These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis, metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular growth, differentiation and migration, resulting in antitumor activity, as shown by the numerous published experimental results...
August 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28814242/antimicrobial-peptides-a-promising-therapeutic-strategy-in-tackling-antimicrobial-resistance
#6
Ramya Nuti, Sridhar Goud, A Prasanth Saraswati, Ravi Alvala, Mallika Alvala
BACKGROUND: Antimicrobial resistance (AMR) has posed a serious threat to global public health and it requires immediate action, preferably long term. Current drug therapies have failed to curb this menace due to the ability of microbes to circumvent the mechanisms through which the drugs act. From the drug discovery point of view, the majority of drugs currently employed for antimicrobial therapy are small molecules. Recent trends reveal a surge in the use of peptides as drug candidates as they offer remarkable advantages over small molecules...
August 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28814241/the-emerging-picture-of-cdk11-genetic-functional-and-medicinal-aspects
#7
Nikolas Ferreira Dos Santos Paparidis, Fernanda Canduri
Cyclin-dependent kinase 11 is a relatively neglected member of the transcriptional CDKs subfamily, despite possibly being the most versatile CDK in this group. Different CDK11 variants are known to play essential roles in major cellular processes as mRNA transcription (CDK11p110), mitosis (CDK11p58), and apoptosis (CDK11p46 and CDK11p60). Each CDK11 species targets a particular set of substrates related to its functional background, but all isoforms originate from the CDC2L gene complex in human chromosome 1p36...
August 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28814240/structure-properties-and-mechanisms-of-action-of-naturally-originated-phenolic-acids-and-their-derivatives-against-human-viral-infections
#8
Yi-Hang Wu, Bing-Yi Zhang, Li-Peng Qiu, Rong-Fa Guan, Zi-Hong Ye, Xiao-Ping Yu
BACKGROUND: A great effort has been made to develop efficacious antiviral drugs, but many viral infections are still lack of efficient antiviral therapies so far. The related exploration of natural products to fight viruses has been raised in recent years. Natural compounds with structural diversity and complexity offer a great chance to find new antiviral agents. Particularly, phenolic acids have attracted considerable attention owing to their potent antiviral abilities and unique mechanisms...
August 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28799499/orally-administrated-small-molecule-drugs-with-intestine-targeted-profile-recent-development-and-prospects
#9
Hua Cao, Kai Wang, Yang-Liang Ye, Jian-Hua Shen
Intestine targeted drugs are orally administered compounds exerting their therapeutic effects locally in the intestinal tract, thus avoiding side effects related to systemic exposure. Both academic and pharmaceutical research has, therefore, focused on such agents, but the systematic methodology needed for their design and evaluation has been unclear. Medicinal chemists have pursued design of intestine targeted compounds outside the "rule of five". This review summarized six categories of intestine targeted drugs, based on various design strategies, with careful analysis of recent examples from each category...
August 10, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28799498/structure-based-approaches-targeting-parasite-cysteine-proteases
#10
Rafael Pinto Vieira, Viviane Corrêa Santos, Rafaela Salgado Ferreira
Cysteine proteases are essential hydrolytic enzymes present in the majority of organisms, including viruses and unicellular parasites. Despite the high sequence identity displayed among these proteins, specific structural features across different species grant distinct functions to these biomolecules, frequently related to pathological conditions. Consequently, their relevance as promising targets for potential specific inhibitors has been highlighted and occasionally validated in recent decades. In this review, we discuss the recent outcomes on structure-based campaigns aiming the discovery of new inhibitor prototypes against cruzain and falcipain, as alternative therapeutic tools for Chagas disease and malaria treatments, respectively...
August 10, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28799497/cannabis-phenolics-and-their-bioactivities
#11
Federica Pollastro, Alberto Minassi, Luigia Grazia Fresu
Although Cannabis sativa L. is one of the most versatile plant species with multipurpose use both as medical, alimentary source and as psychoactive abuse, its biomedical relevance focused the attention on major cannabinoids. Phytochemical characterization of cannabis highlights the presence of various non-cannabinoids constituents including flavonoids, spiroindans, dihyrostilbenes, dihydrophenanthrenes, lignanamides, steroids and alkaloids. Cannabis is a plant with high pharmacological and nutrition values, its potentialities and applications are not only circumscribed to cannabinoids biological activities, but also defined by non-cannabinoid compounds...
August 10, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28799496/anti-inflammatory-natural-prenylated-phenolic-compounds-potential-lead-substances
#12
Viliam Brezáni, Karel Šmejkal, Jan Hošek, Veronika Tomášová
BACKGROUND: Natural phenolics are secondary plant metabolites, which can be divided into several categories with the common structural feature of phenolic hydroxyl. The biological activity of phenolics is often modified and enhanced by prenylation by prenyl and geranyl; higher terpenoid chains are rare. The type of prenyl connection and modification affects their biological activity. OBJECTIVE: This review summarizes information about prenylated phenols and some of their potential sources, and provides an overview of their anti-inflammatory potential in vitro and in vivo...
August 10, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28799495/a-nanotechnology-based-strategy-to-increase-the-efficiency-of-cancer-diagnosis-and-therapy-folate-conjugated-gold-nanoparticles
#13
Jaber Beik, Sara Khademi, Neda Attaran, Saeed Sarkar, Ali Shakeri-Zadeh, Habib Ghaznavi, Hossein Ghadiri
BACKGROUND: Gold nanoparticle (AuNP), owing to its elegant physicochemical properties, has been recently introduced as a promising theranostic nanoparticle. Folic acid is a necessary vitamin for cell proliferation and cancer cells highly require such an essential molecule to be replicated. Accordingly, surface functionalization of AuNP with folic acid may offer great potentials for development of a new nanotechnology based strategy to increase the efficiency of cancer diagnosis and therapy...
August 10, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28782469/immune-checkpoint-inhibitors-basics-and-challenges
#14
Bin Li, Ho Lam Chan, Pingping Chen
Cancer is one of the most deadly diseases in modern world. The last decade has witnessed dramatic advances in the cancer treatment through immunotherapy. One extremely promising means to achieve anti-caner immunity is to block the immune checkpoint pathways, which mechanism was adopted by cancer cells to disguise themselves as regular components of human body. While checkpoint blockade is universally effective against a broad spectrum of cancer types and mostly unrestricted by certain gene mutation status, only a minority of patients achieved a complete response to such treatment...
August 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28782468/induced-pluripotent-stem-cells-as-a-model-for-therapy-personalization-of-pediatric-patients-disease-modeling-and-drug-adverse-effects-prevention
#15
Elena Genova, Marco Pelin, Katsunori Sasaki, Yue Fengming, Gaetana Lanzi, Stefania Masneri, Alessandro Ventura, Gabriele Stocco, Giuliana Decorti
Understanding the biological and molecular processes underlying human pathologies is fundamental in order to develop innovative approaches to treat or prevent them. Among the technologies that could provide innovative disease models, induced pluripotent stem cells (iPSCs) is one of the most promising. Indeed, one application of iPSCs technology is personalized disease modeling. These cells, obtained by reprogramming patients' cells collected from accessible tissues, have the unique capability to differentiate, under an adequate stimulus, into any human cell type...
August 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28762313/adoptive-immunotherapy-for-b-cell-malignancies-using-cd19-targeted-chimeric-antigen-receptor-t-cells-a-systematic-review-of-efficacy-and-safety
#16
Lu Hao, Tongtong Li, Lung-Ji Chang, Xiaochuan Chen
BACKGROUND: Adoptive infusion of chimeric antigen receptor transduced T-cells (CAR-T) is a powerful tool of immunotherapy for hematological malignancies, as evidenced by recently published and unpublished clinical results. OBJECTIVE: In this report, we performed a meta-analysis to evaluate the efficacy and side effects of CAR-T on relapsed B-cell malignancies, including leukemia and lymphoma. METHODS: Clinical studies investigating efficacy and safety of CAR-T in acute and chronic lymphocytic leukemia and lymphoma were identified by searching PubMed and EMBASE...
August 1, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28762312/cadmium-organ-toxicity-and-therapeutic-approaches-a-review-on-brain-kidney-and-testis-damage
#17
Mariagrazia Rinaldi, Antonio Micali, Herbert Marini, Elena Bianca Adamo, Domenico Puzzolo, Antonina Pisani, Vincenzo Trichilo, Domenica Altavilla, Francesco Squadrito, Letteria Minutoli
BACKGROUND: Cadmium (Cd) is a heavy metal particularly hazardous for human health, as it is highly diffused and, therefore, a ubiquitous environmental toxicant. In fact, in the general population, the main sources of exposure are food, cigarette smoking, inhalation of ambient air, drinking water, contaminated soil or dust. Furthermore, an occupational exposure usually involves human during mining, fume inhalation or manufacturing nickel-cadmium battery, electroplating and paint pigments that utilize Cd...
August 1, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28762311/therapeutic-potential-of-co-enzyme-q10-in-retinal-diseases
#18
Xun Zhang, Ali Mohammad Tohari, Fabio Marcheggiani, Xinzhi Zhou, James Reilly, Luca Tiano, Xinhua Shu
Coenzyme Q10 (CoQ10) plays a critical role in mitochondrial oxidative phosphorylation by serving as an electron carrier in the respiratory electron transport chain. CoQ10 also functions as a lipid-soluble antioxidant by protecting lipids, proteins and DNA damaged by oxidative stress. CoQ10 deficiency has been associated with a number of human diseases including mitochondrial diseases, neurodegenerative disorders, cardiovascular diseases, diabetes, cancer, and with the ageing process. In many of these conditions CoQ10 supplementation therapy has been effective in slowing or reversing pathological changes...
August 1, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28762309/histone-deacetylase-inhibitors-in-tumor-immunotherapy
#19
Li-Ming Zhao, Jie-Huan Zhang
With an increasing understanding of the antitumor immune response, considerable progress has been made in the field of tumor immunotherapy in the last decade. Inhibition of HDACs represents a new strategy in tumor therapy and HDAC inhibitors have been recently developed and validated as potential antitumor drugs. In addition to the direct antitumor effects, HDAC inhibitors have been found to have the ability to improve tumor recognition by immune cells that may contribute to their antitumor activity. These immunomodolutory effects are desirable, and their in-depth comprehension will facilitate the design of novel regimens with improved clinical efficacy...
August 1, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28762310/sarcopenia-aging-and-prospective-interventional-strategies
#20
Tyler B Waltz, Elayne M Fivenson, Marya Morevati, Chuanhao Li, Kevin G Becker, Vilhelm A Bohr, Evandro Fei Fang
Sarcopenia, or age-related muscle decline, occurs in most organisms and burdens both human health and the healthcare system. As our population ages, additional options for treating sarcopenia are needed. Mitochondrial dysfunction is implicated in the onset of sarcopenia, so therapies directed at improving mitochondrial function in muscle should be considered. Many naturally-occurring compounds, derived from commonly consumed foods, possess anti-sarcopenic effects, such asnicotinamide riboside, tomatidine, and Urolithin A...
July 31, 2017: Current Medicinal Chemistry
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