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Current Drug Targets

Xun Che, Wei Dai
AhR is an environmental response gene that mediates cellular responses to a variety of xenobiotic compounds that frequently function as AhR ligands. Many AhR ligands are classified as carcinogens or pro-carcinogens. Thus, AhR itself acts as a major mediator of the carcinogenic effect of many xenobiotics in vivo. In this concise review, mechanisms by which AhR trans-activates downstream target gene expression, modulates immune responses, and mediates malignant transformation and tumor development are discussed...
November 8, 2018: Current Drug Targets
Surovi Saikia, Manobjyoti Bordoloi, Rajeev Sarmah
The key down player remains for drug industries is the selection of biological target currently attracting huge investments to validate them in patient subsets in order to study potential drugs. GPCRs are one such druggable target wherein non-olfactory GPCRs are encoded by 50% of the human genome-encoded which are therapeutically unexploited. The concept of ploypharmacology has become essential part of therapeutics for complex diseases like schizophrenia, cancer etc and considering the promiscuity and selectivity GPCRs could emerge as novel targets...
November 5, 2018: Current Drug Targets
Zar Chi Thent, Gabriele R A Froemming, Suhaila Abd Muid
Increasing interest on vascular pseudo-ossification has alarmed the modern atherosclerotic society. High phosphate is one of the key factors in vascular pseudo ossification, also known as vascular calcification. The active process of deposition of the phosphate crystals in vascular tissues results in arterial stiffness. High phosphate condition is mainly observed in chronic kidney disease patients. However, prolong exposure with high phosphate enriched foods such as canned drinks, dietary foods, etc. can be considered as modifiable risk factors for vascular complication in population with regardless of chronic kidney disease...
October 31, 2018: Current Drug Targets
Rajinder Pal Mittal, Abhilash Rana, Vikas Jaitak
Antimicrobial resistance (AMR) is an emerging problem in the world that has a significant impact on our society. AMR made conventional drugs futile against microorganisms and diseases untreatable. Plant-derived medicines are considered as safe alternatives to synthetic drugs. The active ingredients and the mixtures of these natural medicines have been used for centuries, due to their easy availability, low cost, and negligible side effects. Essential oils (EOs) are the secondary metabolites that are produced by aromatic plants to protect them from microorganisms...
October 31, 2018: Current Drug Targets
Olivia F Cox, Paul W Huber
Post-translational modification by small ubiquitin-like modifier (SUMO) has emerged as a global mechanism for the control and integration of a wide variety of biological processes through the regulation of protein activity, stability and intracellular localization. As SUMOylation is examined in greater detail, it has become clear that the process is at the root of several pathologies including heart, endocrine, and inflammatory disease, and various types of cancer. Moreover, it is certain that perturbation of this process, either globally or of a specific protein, accounts for many instances of congenital birth defects...
October 26, 2018: Current Drug Targets
Shirin Eyvazi, Mohammad Saeid Hejazi, Homan Kahroba, Mozghan Abasi, Reza Eghdam Zamiri, Vahideh Tarhriz
Cyclin dependent kinase 9 (Cdk9) as a serine/threonine kinase belongs to a large number of Cdks. Cdk9 as a main core of PTEF-b complex phosphorylates RNA polymerase (RNAP) II and other transcription factors. Therefore it regulates gene transcription elongation in many physiologic processes. The seemingly disparate roles of Cdk9 in the different stages of various cellular pathways appear that Cdk9 can be an appealing target in treatment of several physiologic conditions. In this review, we have summarized the recent findings of molecular interaction between Cdk9 and critical molecules which modulated their activity levels by Cdk9 in various disease pathways...
October 26, 2018: Current Drug Targets
Pedro Henrique Souza Cesar, Mariana Aparecida Braga, Marcus Vinicius Cardoso Trento, Danilo Luccas Menaldo, Silvana Marcussi
Disintegrins are non-enzymatic proteins that interfere on cell-cell interactions and signal transduction, contributing to the toxicity of snake venoms and playing an essential role in envenomations. Most of their pharmacological and toxic effects are the result of the interaction of these molecules with cell surface ligands, which has been widely described and studied. These proteins may act on platelets, leading to hemorrhage, and may also induce apoptosis and cytotoxicity, which highlights a high pharmacological potential for the development of thrombolytic and antitumor agents...
October 22, 2018: Current Drug Targets
Jianzhao Gao, Zhen Miao, Zhaopeng Zhang, Hong Wei, Lukasz Kurgan
Background:Ion channels are a large and growing protein family. Many of them are associated with diseases and consequently they are targets for over 700 drugs. Discovery of new ion channels is facilitated with computational methods that predict ion channels and their types from protein sequences. However, these methods were never comprehensively compared and evaluated. OBJECTIVE: We offer first-of-its-kind comprehensive survey of the sequence-based predictors of ion channels. We describe a comprehensive collection of eight predictors that include five methods that predict ion channels, their types and four classes of the voltage-gated channels...
October 22, 2018: Current Drug Targets
Surovi Saikia, Manobjyoti Bordoloi
Molecular docking is a process through which small molecules are docked into the macromolecular structures for scoring its complementary values at the binding sites. It is a vibrant research area with dynamic utility in structure based drug-designing, lead optimization, biochemical pathway and for drug designing being the most attractive tools. Two pillars for a successful docking experiment are correct pose and affinity prediction. Each program has its own advantages and drawbacks with respect to their docking accuracy, ranking accuracy and time consumption so a general conclusion cannot be drawn...
October 22, 2018: Current Drug Targets
Angeles C Tecalco-Cruz, Josue O Ramirez-Jarquin, Eduardo Cruz-Ramos
More than 70% of all breast cancer cases are estrogen receptor alpha-positive (ERα). ERα is a member of the nuclear receptor family, and its activity is implicated in the gene transcription linked to the proliferation of breast cancer cells, as well as in extranuclear signaling pathways related to the development of resistance to endocrine therapy. Several protein-protein interactions and post-translational modifications of ERα represent critical mechanisms that modulate its activity...
October 15, 2018: Current Drug Targets
Joanna Drogosz, Anna Janecka
Sesquiterpene lactones, secondary metabolites of plants, present in a large number of species mostly from the Asteracea family, were used in the traditional medicine of many countries for the treatment of various pathological conditions. They exert a broad range of activities, including anti-inflammatory, anti-bacterial and anti-cancer properties. The best known sesquiterpene lactones which are already used as drugs or are in clinical trials are artemisinin, thapsigargin and parthenolide. Yet another sesquiterpene lactone, helenalin, an active component of Arnica montana, known for its strong anti-inflammatory activity, has been used for centuries in folk medicine to treat minor injuries...
October 12, 2018: Current Drug Targets
Jiu-Xin Tan, Hao Lv, Fang Wang, Fu-Ying Dao, Wei Chen, Hui Ding
Enzymes are proteins that act as biological catalysts to speed up cellular biochemical processes. According to their main Enzyme Commission (EC) numbers, enzymes are divided into six categories: EC-1: oxidoreductase; EC-2: transferase; EC-3: hydrolase; EC-4: lyase; EC-5: isomerase and EC-6: synthetase. Different enzymes have different biological functions and acting objects. Therefore, knowing which family an enzyme belongs to can help infer its catalytic mechanism and provide information about the relevant biological function...
October 2, 2018: Current Drug Targets
Gangliang Huang
The interaction between a sugar molecule and a target is relatively weak. By simultaneously linking multiple sugar molecules to one nanoparticle for forming the glyconanoparticle, the targeting can be greatly improved. This is due to the existence of multivalent interactions between the glyconanoparticle and the target. Based on this, by linking the drug to the glyconanoparticle, the targeted delivery of drug can be achieved. Therefore, glyconanoparticles have very important applications in drug delivery. Herein, the application of glyconanoparticles in drug delivery was summarized and analyzed, and countermeasures were put forward for the existing problems...
September 26, 2018: Current Drug Targets
Lidong Wang, Ruijun Zhang
Ubiquitination is an important post-translational modification in regulating protein functions, which provides a key insight to discover the causes associated with cancer, cardiovascular and other diseases. Recent attempts have been made for capturing potential ubiquitination sites with the aid of chemo-proteomic approaches and computational methods. Experimental identification of ubiquitination sites is especially vulnerable to the temporality and reversibility of ubiquitination processes, which is also costly and time-consuming...
September 24, 2018: Current Drug Targets
Amr Menshawy, Omar Mattar, Kirolos Barssoum, Ammar M AboEl-Naga, Haitham Mohamed Salim, Ahmed Mesbah Fahmy Mohamed, Ahmed Elgebaly, Sherief Abd-Elsalam
AIM: The role of rifaximin in the prevention of spontaneous bacterial peritonitis(SBP) is not well studied. The aim of this meta-analysis was to evaluate the role of rifaximin in the prevention of SBP. METHODS: A computerized literature search for relevant clinical trials was conducted during August 2017. Data on Frequency of SBP, the success rate of prevention of SBP, mortality rate, hepatorenal syndrome, septic shock, hepatic encephalopathy, and GIT bleeding were extracted and pooled as risk ratio (RR) with their 95% confidence interval (CI) in a meta-analysis model...
September 24, 2018: Current Drug Targets
Carlos G Ferreira, Andrea Nicolini, Liliana Dalurzo, Stephen Stefani, Vanessa Teiche, Natasha Leighl
The development of therapies that restore or activate the host immune response - the so called "immuno-oncologic" therapy - has improved the survival of some cancer patients harboring specific tumor types. These drugs, however, are very expensive which has greatly limited their use and consequently reduced the number of patients who could likely benefit. Not to mention, that the proportion of patients who display a clinical benefit from therapy is limited. Thus, from a clinical e health economics perspective there is a pressing need to identify and treat those patients for whom a given immuno-oncologic therapy is most likely to be beneficial...
September 10, 2018: Current Drug Targets
Rakesh Sharma
Stem Cell Research and Tissue Engineering, in present time, have emerged as a legalized and regulated stem cell treatment option globally, but scientifically, their success is unestablished. Novel stem cell-based therapies have evolved as innovative and routine clinical solutions by commercial companies and hospitals across the world. Such rampant spread of stem cell clinics throughout UK, US, Europe and Asia reflect the public encouragement of benefits to incurable diseases. However, ever growing stem cell therapy developments need constant dogwatch and careful policy making by government regulatory bodies for prompt action in case of any untoward public concern...
August 30, 2018: Current Drug Targets
Shiqi Luo, George Binh Lenon, Harsharn Gill, Heidi Yuen, Angela Wei Hong Yang, Andrew Hung, Linh Toan Nguyen
BACKGROUND: Overweight or obesity has become a world-wide health concern. Pharmacotherapies are introduced because lifestyle modifications alone are insufficient for weight management. The treatment outcomes of current approved anti-obesity agents are not satisfying due to drug-related intolerances. Therefore natural therapies including herbal medicines are popular alternatives for weight reduction; however there are limited studies about their mechanism of actions Methods: Five databases include PubMed, Scopus, Google Scholar, Science direct, Proquest were searched in order to investigate the targets and safety profiles of the current and past anti-obesity drugs that have been approved by Food and drug administration (FDA) or European Medicines Agency (EMA)...
August 30, 2018: Current Drug Targets
Yanzhou Yang, Hoi-Hung Cheung, Cheng Zhang, Ji Wu, Wai-Yee Chan
In previous studies, oxidative stress damage was solely considered to be the mechanism of ovarian aging, and several antioxidants were used to delay ovarian aging. But recently, more reports have found that endoplasmic reticulum stress, autophagy, sirtuins, mitochondrial dysfunction, telomeres, gene mutation, premature ovarian failure, and polycystic ovary syndrome are all closely related to ovarian aging, and these factors all interact with oxidative stress. These novel insights on ovarian aging are summarized in this review...
August 28, 2018: Current Drug Targets
Qinyuan Li, Qian Yi, Lin Tang, Siying Luo, Yuan Tang, Guangli Zhang, Zhengxiu Luo
BACKGROUND: Air pollution is a major cause of asthma exacerbation. Most studies have proven that exposure to coarse and fine particulate matter is associated with asthma exacerbation. Ultrafine particles (UFP, aerodynamic diameter ≤ 0.1 μm) are the smallest airborne particles, which are capable of penetrating deep into the lungs because of their small size. Toxicological studies have suggested that exposure to UFPs may have serious effects on respiratory health. However, epidemiological evidence on the effects of UFP exposure on asthma exacerbation remains unclear...
August 28, 2018: Current Drug Targets
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