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Current Drug Targets

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https://www.readbyqxmd.com/read/29336260/adipocytes-and-abdominal-aortic-aneurysm-putative-potential-role-of-adipocytes-in-the-process-of-aaa-development
#1
Hirona Kugo, Tatsuya Moriyama, Nobuhiro Zaima
Background Adipose tissue plays a role in the storage of excess energy as triglycerides (TGs). Excess fat accumulation causes various metabolic and cardiovascular diseases. It has been reported that ectopic fat deposition and excess TG accumulation in non-adipose tissue might be important predictors of cardiometabolic and vascular risk. For example, ectopic fat in perivascular tissue promotes atherosclerotic plaque formation in the arterial wall. Objective Recently, it has been reported that ectopic fat (adipocyte) in the vascular wall of an abdominal aortic aneurysm (AAA) is present in both human and experimental animal models...
January 15, 2018: Current Drug Targets
https://www.readbyqxmd.com/read/29336259/p53-as-the-focus-of-gene-therapy-past-present-and-future
#2
Joana Fa Valente, Joao A Queiroz, Fani Sousa
BACKGROUND: Several gene deviations can be responsible for triggering oncogenic processes. However, mutations in tumour suppressor genes are usually more associated to malignant diseases, being p53 one of the most affected and studied element. p53 is implicated in a number of known cellular functions, including DNA damage repair, cell cycle arrest in G1/S and G2/M and apoptosis, being an interesting target for cancer treatment. OBJECTIVE: Considering these facts, the development of gene therapy approaches focused on p53 expression and regulation seems to be a promising strategy for cancer therapy...
January 15, 2018: Current Drug Targets
https://www.readbyqxmd.com/read/29318968/the-role-of-dna-repair-pathways-in-aml-chemosensitivity
#3
Elizabeth A Pearsall, Lisa F Lincz, Kathryn Anne Skelding
BACKGROUND: Defects in DNA repair pathways are causal factors for a plethora of solid tumours, but are only just beginning to be explored in haematological malignancies. Genomic instability, including mutations in DNA sequences, chromosomal aneuploidy, translocations and gene amplifications contribute to the development and progression of AML. Prior DNA damaging agent exposure enhances the risk of developing AML, as does inheritance of genetic syndromes that involve alterations in DNA repair pathways...
January 9, 2018: Current Drug Targets
https://www.readbyqxmd.com/read/29303077/aptamers-and-aptasensors-as-novel-approach-for-microbial-detection-and-identification-an-appraisal
#4
Bushra Jamil, Muhammad Ali Syed
Tremendous efforts through dedicated research have been made for the development of robust, point of care, portable, cost effective, sensitive and specific assays of microbial detection for a wide range of applications. Biosensing and nanotechnology offer novel strategies of designing state of the art devices and assay formats with enhanced sensitivity and all other desired features. Monoclonal antibodies have been in use as biorecognition elements for decades. However, recent studies have demonstrated superiority of aptamers to monoclonal antibodies in a number of applications...
January 4, 2018: Current Drug Targets
https://www.readbyqxmd.com/read/29299986/significance-of-hepatoprotective-liver-specific-targeted-drug-delivery-a-review-on-novel-herbal-and-formulation-approaches-in-management-of-hepatotoxicity
#5
Surbhi Rohilla, D C Bhatt
BACKGROUND: The liver is the largest and vital organ present in all vertebrates. It performs various major functions such as detoxification, metabolism, protein synthesis, excretion and so on. Liver cells are divided into parenchymal cells and non-parenchymal cells. Hepatocytes, Kupffer cells, hepatic stellate cells and sinusoidal endothelial cells, etc are found in liver having different receptors present on their surface which can be used for liver targeting by binding to different ligands...
January 3, 2018: Current Drug Targets
https://www.readbyqxmd.com/read/29284389/efficacy-and-safety-of-serotonin-receptor-ligands-in-the-treatment-of-irritable-bowel-syndrome-a-review
#6
Agata Binienda, Martin Storr, Jakub Fichna, Maciej Salaga
Irritable bowel syndrome (IBS) is a chronic, recurrent bowel disorder with an unknown etiology, which is most likely multifactorial. Increased mucosal permeability, visceral hypersensitivity and activation status of intestinal mucosal immune cells cause changes in gastrointestinal (GI) motility, secretion and sensation observed in the course of IBS. Permanent, cumbersome symptoms, such as diarrhea, constipation and abdominal pain greatly lower quality of life of IBS patients. On this basis, according to the Rome IV criteria, different forms of IBS can be distinguished...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29284388/fenofibrate-and-telmisartan-in-the-management-of-abdominal-aortic-aneurysm
#7
Sophie E Rowbotham, Smriti M Krishna, Corey S Moran, Jonathan Golledge
Objective This mini-review provides the rationale and updated progress for ongoing randomized controlled trials assessing fenofibrate and telmisartan efficacy to limit abdominal aortic aneurysm (AAA) growth. Methods / Results Data from preclinical and human studies investigating the efficacy of fenofibrate and telmisartan to limit AAA growth is presented and provides the rationale for three current randomized controlled trials assessing these medications as potential interventions to limit aneurysm growth in AAA patients...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29284387/optimal-time-for-pharmacological-treatment-of-abdominal-aortic-aneurysm
#8
Yasunori Iida, Shigeharu Sawa, Hideyuki Shimizu
Abdominal aortic aneurysm (AAA), if left untreated, poses the main risks of progressive expansion, rupture, and hemorrhage, leading to death. Smoking and hypertension are the 2 major risk factors for AAA crucial in preventing its progression. The underlying fundamental pathophysiological cause of AAA is chronic inflammation. Large AAA with a risk of rupture is usually treated by graft replacement or endovascular aneurysm repair. Nonsurgical treatment is not an alternative for large AAA, but is potentially beneficial for small AAA which usually requires a watchful waiting approach with medication...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29284386/current-status-and-perspectives-on-pharmacologic-therapy-for-abdominal-aortic-aneurysm
#9
Koichi Yoshimura, Noriyasu Morikage, Shizuka Nishino-Fujimoto, Akira Furutani, Bungo Shirasawa, Kimikazu Hamano
Abdominal aortic aneurysm (AAA), a common disease involving the segmental expansion and rupture of the aorta, has a high mortality rate. Therapeutic options for AAA are currently limited to surgical repair to prevent catastrophic rupture. Non-surgical approaches, particularly pharmacotherapy, are lacking for the treatment of AAA. Here, we review both basic and clinical studies and discuss the current challenges to developing medical therapy that reduces AAA progression. Studies using animal models of AAA progression and human AAA explant cultures have identified several potential targets for preventing AAA growth...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29284385/therapeutic-applications-of-prostaglandins-and-thromboxane-a2-inhibitors-in-abdominal-aortic-aneurysms
#10
Courtois Audrey, Makrygiannis Georgios, Cheramy-Bien Jean-Paul, Purnelle Audrey, Pirotte Bernard, Jean Michel Dogné, Julien Hanson, Defraigne Jean-Olivier, Drion Pierre, Natzi Sakalihasan
Abdominal aortic aneurysm (AAA) is one of the leading causes of death in western countries. Surgery is still, at the present time, the sole treatment that has however a significant mortality and cost rate. Many pharmacological agents are under investigation aiming to reduce growth and prevent AAA rupture. These drugs target different pathological pathways and, notably, the excessive production of prostanoids by cyclooxygenases (COX). Intra-aneurysmal thrombus plays an adverse key role in the progression of AAA, platelets being a primary source of prostanoids as thromboxane A2...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29283071/silk-fibroin-based-drug-delivery-applications-promises-and-challenges
#11
Shahid Ud Din Wani, Gangadharappa Hosahalli Veerabhadrappa
BACKGROUND: Silk Fibroin (SF), a natural source material obtained from Bombyx mori, has been widely enlisted as biomaterial having outstanding mechanical properties. SF has been reported one of the propitious bio-polymer for various drug delivery systems, as well as drug delivery vehicle. OBJECTIVE: This review is summarised to provide in comprehensive applications of silk fibroin in various drug delivery systems, and also to present the current opportunities and requirements by furnishing a definitive assessment on silk fibroin as a polymer...
December 27, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29210646/pcsk9-and-hypercholesterolemia-therapeutical-approach
#12
Milan Obradovic, Bozidarka Zaric, Emina Sudar-Milovanovic, Branislava Ilincic, Milan Perovic, Edita Stokic, Esma Isenovic
Despite the intensive research and progress in modern pharmacotherapy, hypercholesterolemia and related cardiovascular complications remain one of the leading causes of mortality and disability in the modern world. A significant contribution to the treatment of hypercholesterolemia was made by the discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9). This enzyme is responsible for the degradation of the low-density lipoprotein (LDL) receptor (LDLR) found at the surface of the plasma membrane in the liver and directly associated with serum LDL level...
December 4, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29189148/identification-of-novel-ligands-for-therapeutic-lipopeptides-daptomycin-surfactin-and-polymyxin
#13
Satya Eswari Jujjavarapu, Swasti Dhagat, Vinay Kurrey
Due to increase in antibiotic-resistance among pathogens, there is a need for potent and safe drugs. An alternative to antibiotics is lipopeptides which are produced as a secondary metabolite by many microorganisms. They exhibit broad-spectrum activities against pathogens along with anti-cancer properties. Among various lipopeptides produced by microorganisms, daptomycin, surfactin, and polymyxin have gained popularity as medicines but their mechanism of action is not described properly. In silico drug design of these lipopeptides becomes a challenge due to their complex structures...
November 29, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29189147/disrupting-acetyl-lysine-interactions-recent-advance-in-the-development-of-bet-inhibitors
#14
Fa Zhang, Shutao Ma
BACKGROUND: Histone acetylation is an essential way of post-translational modification (PTM) and a significant component of epigenetic regulation that is mediated by Bromodomain-containing protein (BRD). In recent years, many researchers have found that a variety of malignancy, inflammatory and other diseases occurrence and development are associated with BRD4 expression disorders or dysfunction. Meanwhile, many the bromodomain inhibitors of the bromodomains and extra-terminal (BET) family is reported in many papers...
November 29, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29173164/epigenetic-mechanisms-role-in-hematopoietic-stem-cell-lineage-commitment-and-differentiation
#15
Sanjeev Raghuwanshi, Swati Dahariya, Ravinder Kandi, Usha Gutti, Ram Babu Undi, Durga Shankar Sharma, Narasaiah Kovuru, Itishri Sahu, Nagendra Sastry Yarla, Raja Gopal Venakata Saladi, Ravi Kumar Gutti
Major breakthroughs in last several decades have contributed to our knowledge of the genetic regulation in development. Although epigenetics is not a new concept, unfortunately, the role of epigenetics has not come to fruition in large past. But the field of epigenetics has exploded within the past decade. Now, growing evidences show a complex network of epigenetic regulation in development. The epigenetic makeup of a cell, tissue or individual is much more complex than their genetic complement. Epigenetic modifications are more important for normal development by maintaining the gene expression pattern in tissue- and context- specific manner...
November 22, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29173163/tocopherol-and-tocotrienol-therapeutic-potential-in-animal-models-of-stress
#16
Mohd Fahami Nur Azlina, Yusof Kamisah, Mohd Saad Qodriyah
BACKGROUND: Scientific reports had shown that stress is related to numerous pathological changes in the body. These pathological changes can bring about numerous diseases and can significantly cause negative effects in an individual. These include gastric ulcer, liver pathology and neurobehavioral changes. A common pathogenesis in many diseases related to stress involves oxidative damage. Therefore, the administration of antioxidants such as vitamin E is a reasonable therapeutic approach...
November 22, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29149828/vortioxetine-treatment-for-anxiety-disorder-a-meta-analysis-study
#17
Anne Yee, Chong Guan Ng, Loh Huai Seng
BACKGROUND: Vortioxetine is a multimodal antidepressant that has been developed for the treatment of major depressive and anxiety disorders. The aim of this review is to quantitatively synthesize all data of the efficacy, safety and tolerability of Vortioxetine in treating anxiety disorder. METHOD: Terms of "Vortioxetine" OR "LuAA21004" AND "anxiety" OR "fear" OR "panic" OR "phobia" were searched. A total of two phase II and five phase III clinical trials were found...
November 17, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29149827/therapeutic-applications-of-capsaicin-in-upper-airways
#18
Carlo Cavaliere, Simonetta Masieri, Franco Cavaliere
Capsaicin (8-methyl-N-vanillyl-6-nonenamide) is the substance responsible of the irritation caused by the contact of chili peppers with the skin or mucous membranes. This protoalkaloid acts by stimulating the transient receptor potential cation channel subfamily V member 1 (TRPV1), which is mainly expressed by nociceptive fibers of peripheral sensory neurons, but is also present in the central nervous system, and in some non-neuronal cells. Following the initial, intense neuronal excitation, a brief refractory period occurs...
November 17, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29149826/novel-functions-of-microrna-17-92-cluster-in-the-endocrine-system
#19
Shan Wan, Xiang Chen, Yuedong He, Xijie Yu
BACKGROUND: MiR-17-92 cluster is coded by MIR17HG in chromosome 13, which is highly conserved in vertebrates. Published literatures have proved that miR-17-92 cluster critically regulates tumorigenesis and metastasis. Recent researches showed that the miR-17-92 cluster also plays novel functions in the endocrine system. OBJECTIVE: To summarize recent findings on the physiological and pathological roles of miR-17-92 cluster in bone, lipid and glucose metabolisms...
November 17, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/29149825/dopamine-agonists-and-neurodegenerative-disorders
#20
Saba Khanam, Yasir Hasan Siddique
Background: Parkinson’s disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons within the substantia nigra pars compacta (SNpc). Despite of many researches, there is still no cure for this disease. Levodopa is first line treatment of PD, but the long term use of it leads to motor impairments and dyskinesias. The dopamine agonists are the preferred choice for the treatment of PD. They are neuroprotective in nature but also have side effects. Objective: Our aim was to review the work that has been carried out on dopamine agonists and the future possibilities to reduce their side effects...
November 17, 2017: Current Drug Targets
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