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Current Medicinal Chemistry

Kazuaki Taguchi, Toru Maruyama, Masaki Otagiri
Carbon monoxide (CO), at low concentrations, can have a variety of positive effects on the body including anti-apoptosis, anti-inflammatory, anti-oxidative and anti-proliferative effects. Although CO has great potential for use as a potent medical bioactive gas, for it to exist in the body in stable form, it must be associated with a carrier. Hemoglobin (Hb) represents a promising material for use as a CO carrier because most of the total CO in the body is stored associated with Hb in red blood cells (RBC)...
November 13, 2018: Current Medicinal Chemistry
Monsurat M Lawal, Zainab K Sanusi, Thavendran Govender, Glenn E M Maguire, Bahareh Honarparvar, Hendrik G Kruger
Current investigations of the human immunodeficiency virus protease (HIV-1 PR) as a druggable target towards the treatment of AIDS require an update to facilitate further development of promising inhibitors with improved inhibitory activities. For the past two decades, up to 100 scholarly reports appeared annually on the inhibition and catalytic mechanism of HIV-1 PR. A fundamental literature review on the prerequisite of HIV-1 PR action leading to the release of infectious virion is absent. Herein, recent advances (both computationally and experimentally) on the recognition mode and reaction mechanism of HIV-1 PR involving its natural targets is provided...
November 13, 2018: Current Medicinal Chemistry
Félix Javier Jiménez-Jiménez, Hortensia Alonso-Navarro, Elena García-Martín, José A G Agúndez
BACKGROUND: The pathophysiology and neurochemical mechanisms of essential tremor (ET) are not fully understood, because only a few post-mortem studies have been reported, and the lack of a good experimental model for this disease. OBJECTIVE: The main aim of this review is to update data regarding the neurochemical features of ET. Alterations of certain catecholamine systems, the dopaminergic, serotonergic, GABAergic, noradrenergic, and adrenergic systems have been described, and are the object of this revision...
November 11, 2018: Current Medicinal Chemistry
Antonio Speciale, Antonella Saija, Romina Bashllari, Maria Sofia Molonia, Claudia Muscara, Cristina Occhiuto, Francesco Cimino, Mariateresa Cristani
Chronic noncommunicable diseases (NCDs), mostly represented by cardiovascular diseases, diabetes, chronic pulmonary diseases, cancers, and several chronic pathologies, are one of the main causes of morbidity and mortality, and are mainly related to the occurrence of metabolic risk factors. Anthocyanins (ACNs) posses a wide spectrum of biological activities, such as anti-inflammatory, antioxidant, cardioprotective, and chemopreventive properties, which are able to promote human health. Although ACNs present an apparent low bioavailability, their metabolites may play an important role in the in vivo protective effects observed...
November 11, 2018: Current Medicinal Chemistry
Chao Li, Dayong Shi
Marine organisms are abundant sources of bioactive natural products. Among metabolites produced by sponges and their associated microbial communities, halogenated natural compounds accounted for an important part due to their potent biological activities. The present review updates and compiles a total of 258 halogenated organic compounds isolated in the past three decades, especially brominated derivatives derived from 31 genera of marine sponges. These compounds can be classified as the following classes: brominated polyunsaturated lipids, nitrogen compounds, brominated tyrosine derivatives and other halogenated compounds...
November 11, 2018: Current Medicinal Chemistry
Ting-Ting Zhao, Hai-Bin Gong, Hai-Liang Zhu, Yu-Qing Xu, Hui-Min Hu
Isoliquiritigenin (2',4',4-trihydroxychalcone, ISL) is one of the most important chalcone compound which mainly derived from licorice root and many other plants. It exhibits a remarkable range of potent biological and pharmacological activities such as antioxidative, antitumor, antiaging, anti-inflammatory, anti-diabetic activities, etc. Numerous research teams have demonstrated that ISL process the ability to antigrowth and proliferation in various cancer cells in vitro and in vivo. Meanwhile, the underlying mechanisms of ISL inhibits cancer cell proliferation have not been well explored...
November 11, 2018: Current Medicinal Chemistry
A G Rodríguez-Hernández, R Vazquez-Duhalt, A Huerta-Saquero
Nanomaterials have become part of our daily lives, particularly nanoparticles contained in food, water, cosmetics, additives and textiles. Nanoparticles interact with organisms at the cellular level. The cell membrane is the first protective barrier against the potential toxic effect of nanoparticles. This first contact, including the interaction between the cell membranes -and associated proteins- and the nanoparticles is critically reviewed here. Nanoparticles, depending on their toxicity, can cause cellular physiology alterations, such as disruption in cell signaling or changes in gene expression, and they can trigger immune responses and even apoptosis...
November 11, 2018: Current Medicinal Chemistry
Georgeta M Simu, Jeanne Atchana, Codruta M Soica, Dorina E Coricovac, Sebastian C Simu, Cristina A Dehelean
In the present work, recent data onto the sources, occurrence and fate of human-use pharmaceutical active compounds (PhACs) in the aquatic environment have been reviewed. Since PhACs and their metabolites are usually present as mixtures in the environment at very low concentrations, , a particular emphasis was placed onto the PhACs mixtures, as well as on their short-term and long-term effects against human and environmental health. Moreover, a general overview of the main conventional as well as of the latest trends in wastewaters decontaminant technologies was outlined...
November 7, 2018: Current Medicinal Chemistry
Paolo D'Arrigo, Martina Tufano, Anna Rea, Vincenza Vigorito, Nunzia Novizio, Salvatore Russo, Maria Fiammetta Romano, Simona Romano
The immune system actively counteracts the tumorigenesis process; a breakout of the immune system function, or its ability to recognize transformed cells, can favor cancer development. Cancer becomes able to escape from immune system control by using multiple mechanisms, which are only in part known at a cellular and molecular level. Among these mechanisms, in the last decade, the role played by the so-called "inhibitory immune checkpoints" is emerging as pivotal in preventing the tumor attack by the immune system...
November 5, 2018: Current Medicinal Chemistry
Yusuke Nakatsu, Yasuka Matsunaga, Koji Ueda, Takeshi Yamamotoya, Yuki Inoue, Masa-Ki Inoue, Yu Mizuno, Akifumi Kushiyama, Hiraku Ono, Midori Fujishiro, Hisanaka Ito, Takayoshi Okabe, Tomoichiro Asano
The prolyl isomerase Pin1 is a unique enzyme, which isomerizes the cis-trans conformation between pSer/pThr and proline, and thereby regulates the function, stability and/or subcellular distribution of its target proteins. Such regulations by Pin1 are involved in numerous physiological functions as well as the pathogenic mechanisms underlying various diseases. Notably, Pin1 deficiency or inactivation is a potential cause of Alzheimer disease, since Pin1 induces the degradation of Tau. In contrast, Pin1 overexpression is highly correlated with the degree of malignancy of cancers, as Pin1 controls a number of oncogenes and tumor suppressors...
November 5, 2018: Current Medicinal Chemistry
Kwang-Sun Kim
Vectors are living organisms that transmit infectious diseases from an infected animal to humans or another animal. Biological vectors such as mosquitoes, ticks, and sand flies carry pathogens that multiply within their bodies prior to delivery to a new host. The increased prevalence of vector-borne diseases (VBDs) such as Aedes-borne dengue, Chikungunya (CHIKV), Zika (ZIKV), malaria, tick-borne disease (TBD), and scrub typhus has a huge impact on the health of both humans and livestock worldwide. In particular, zoonotic diseases transmitted by mosquitoes and ticks place a considerable burden on public health...
November 5, 2018: Current Medicinal Chemistry
Xiao Xiao, James Trevor Oswald, Ting Wang, Weina Zhang, Wenliang Li
As one of the leading and most important metal-based drugs, platinum based pharmaceuticals are widely used in the treatment of solid malignancies. However, significant side effects and acquired drug resistance have limited their clinical applications, despite this, platinum has shown strong inhibitory effects for a wide assortment of tumors. Drug delivery systems using emerging technologies such as liposomes, dendrimers, polymers, nanotubes and other nano-compositions, all show promise for the safe delivery of platinum based compounds...
November 4, 2018: Current Medicinal Chemistry
Anna Rita Bilia, Vieri Piazzini, Laura Risaliti, Giulia Vanti, Marta Casamonti, Meng Wang
Natural products are fascinating molecules in drug discovery for their exciting structure variability and also for their interaction with various targets. Drugs multi-targeting effect represents a more realistic approach to develop successful medications for many diseases. However, besides a large number of successful in vitro and in vivo studies, mostly of clinical trials fail. This is generally related to the scarce water solubility, low lipophilicity and inappropriate molecular size of natural compounds, which undergo structural instability in biological milieu, rapid clearance and high metabolic rate...
November 1, 2018: Current Medicinal Chemistry
Sandra Amaral, Renata Santos Tavares, Sara Escada-Rebelo, Maria Ines Sousa, Andreia Silva, Joao Ramalho-Santos
The alarming increase in the number of diabetic patients worldwide raises concerns regarding its impact on global health, not to mention on social and economic aspects. Furthermore, the association of this complex metabolic disease with male reproductive impairment is worrying, mainly due to the increasing chances that young individuals, at the acme of their reproductive window, could be affected by the disease, further contributing to the disturbing decline in male fertility worldwide. The cornerstone of Diabetes management is glycemic control, proven to be effective in avoiding, minimizing or preventing the appearance or development of disease-related complications...
November 1, 2018: Current Medicinal Chemistry
Adriana Egui, Paola Lasso, Elena Perez-Antón, M Carmen Thomas, Manuel C Lopez
Chagas disease courses with different clinical phases and has a variable clinical presentation and progression. The acute infection phase mostly exhibits a non-specific symptomatology. In the absence of treatment, the acute phase is followed by a chronic phase, which is initially asymptomatic. This chronic asymptomatic phase of the disease is characterized by a fragile balance between the host's immune response and the parasite replication. The loss of this balance results crucial for progression of the sickness...
November 1, 2018: Current Medicinal Chemistry
Fernando Magro, Rosa Coelho, Armando Peixoto
Immune-mediated inflammatory diseases share several pathogenic pathways and this pushes sometimes to extrapolate from one disease or indication to others. A biosimilar can be defined as a biotherapeutic product which is similar in terms of quality, safety, and efficacy to an already licensed reference biotherapeutic product. We review the substrate for extrapolation, the current approval process for biosimilars and the pioneering studies on biosimilars performed in rheumatoid arthritis patients. A biosimilar has the same amino acid sequence as its innovator product...
November 1, 2018: Current Medicinal Chemistry
Lukasz Kurgan, Chen Wang
Therapeutic activity of a significant majority of drugs is determined by their interactions with proteins. Databases of drug-protein interactions (DPIs) primarily focus on the therapeutic protein targets while the knowledge of the off-targets is fragmented and partial. One way to bridge this knowledge gap is to employ computational methods to predict protein targets for a given drug molecule, or interacting drugs for given protein targets. We survey a comprehensive set of 35 methods that were published in high-impact venues and that predict DPIs based on similarity between drugs and similarity between protein targets...
November 1, 2018: Current Medicinal Chemistry
Fei Wang, Xiujuan Lei, Fang-Xiang Wu
Drug repositioning is an important area of biomedical research. The drug repositioning studies have shifted to computational approaches. Large-scale perturbation databases, such as the Connectivity Map and the Library of Integrated Network-Based Cellular Signatures, contain a number of chemical-induced gene expression profiles and provide great opportunities for computational biology and drug repositioning. One reason is that the profiles provided by the Connectivity Map and the Library of Integrated Network-Based Cellular Signatures databases show an overall view of biological mechanism in drugs, diseases and genes...
November 1, 2018: Current Medicinal Chemistry
Kathleen F Edwards, Joel F Liebman
Orphan drug products (e.g., drugs and biologics) in the United States are those that treat people with rare chronic diseases, often cancer or metabolic disease. The rare disease condition being treated by these orphan drugs must serve a patient population of less than 200,000 people in the U.S. in order to earn the orphan drug product title. Just as the disease conditions are seen as "orphans," so, we assert is the thermochemical understanding of the drugs themselves in terms of the chemical structures that define those drugs...
November 1, 2018: Current Medicinal Chemistry
Ana Maria Toader, Snezana D Zaric, Christina M Zalaru, Marilena Ferbinteanu
We revisit in the key of structural chemistry one of the most known and important drugs: the aspirin. Although apparently simple, the factors determining the molecular structure and supramolecular association in crystals are not trivial. We addressed the problem from experimental and theoretical sides, considering issues from X-ray measurements and results of first-principle reconstruction of molecule and lattices by ab initio calculations. Some puzzling problems can give headaches to specialists and intrigue the general public...
October 31, 2018: Current Medicinal Chemistry
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