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Current Pharmaceutical Design

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https://www.readbyqxmd.com/read/27928964/hot-topics-in-pharmacogenetics-of-age-related-macular-degeneration
#1
Stephen G Schwartz, Milam A Brantley, Jaclyn L Kovach, Andrzej Grzybowski
Age-related macular degeneration (AMD) is a leading cause of irreversible visual loss and is primarily treated with nutritional supplementation as well as with anti-vascular endothelial growth factor (VEGF) agents for certain patients with neovascular disease. AMD is a complex disease with both genetic and environmental risk factors. In addition, treatment outcomes from nutritional supplementation and anti-VEGF agents vary considerably. Therefore, it is reasonable to suspect that there may be pharmacogenetic influences on these treatments...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928963/role-of-neurotrophic-factors-in-parkinson%C3%A2-s-disease
#2
Diogo Tomé, Carla Pais Fonseca, Filipa Lopes Campos, Graça Baltazar
Parkinson's disease is an age-associated progressive neurodegenerative disorder that has gained crescent social and economic impact due to the aging of the western society. All current therapies are symptomatic and fail to reverse or halt the progression of dopaminergic neurons loss. The discovery of the capability of neurotrophic factors to protect these neurons lead numerous research groups to focus their efforts in developing therapies aiming at promoting the control of Parkinson´s disease through the delivery of neurotrophic factors to the brain or by boosting their endogenous levels...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928962/neural-circuits-underlying-fly-larval-locomotion
#3
Hiroshi Kohsaka, Pierre A Guertin, Akinao Nose
Locomotion is a complex motor behavior that may be expressed in different ways using a variety of strategies depending upon species and pathological or environmental conditions. Quadrupedal or bipedal walking, running, swimming, flying and gliding constitute some of the locomotor modes enabling the body, in all cases, to move from one place to another. Despite these apparent differences in modes of locomotion, both vertebrate and invertebrate species share, at least in part, comparable neural control mechanisms for locomotor rhythm and pattern generation and modulation...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928961/darpins-bioengineering-and-its-theranostic-approaches-emerging-trends-in-protein-engineering
#4
Mahmood Rasool, Arif Malik, Mubashir Hussain, Kalsoom A Haq, Kiran Butt, Abdul Basit, Muhammad Imran Naseer, Muhammad Asif, Rozena Shaikh, Mohammad Zahid Mustafa, Qamre Alam, Ghulam Rasool, Waseem Ahmad, Absarul L Haque, Mohammad Amjad Kamal
The therapeutic significance of bioengineering proteins has increased dramatically as a new generation of pharmacological drug with a great potential in medical treatment. Protein engineering has improved the use of new non immunoglobulin affinity proteins. The designed ankyrin repeat proteins abbreviated as DARPins is an example. The molecules have smaller structural size, unlike immunoglobulins, but similar target affinity is of great significance. Such molecules get more binding specificity and greater thermodynamic stability...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928960/research-advances-in-molecular-modeling-in-cyclodextrins
#5
Qianqian Zhao, Weixiang Zhang, Runmiao Wang, Yitao Wang, Defang Ouyang
BACKGROUND: Cyclodextrins (CDs), as one type of the novel pharmaceutical excipients, have been widely used in drug delivery and pharmaceutical industry. Over the past decades, a large amount of molecular modeling studies in CDs were reported for profound understanding of structural, dynamic and energetic features of CDs systems. Thus, this review is focused on qualitative and quantitative analysis of research outputs on molecular modeling in CDs. METHODS: The original data were collected from Web of Science and analyzed by scientific knowledge mapping tools, including Citespace, Science of Science, VOSviewer, GPSvisualizer and Gephi software...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928959/potential-application-of-5-aryl-substituted-2-amino-benzamide-type-of-hdac1-2-selective-inhibitors-to-pharmaceuticals
#6
Shinichi Uesato, Yoshiyuki Hirata, Tsutomu Sasaki
Diverse histone deacetylase (HDAC) inhibitors have been developed to date. They control not only histone modification but also gene expression of diverse proteins and thus are expected to provide useful therapeutic effects on various diseases, including cancers, psychiatric and cognitive disorders and neurodegenerative diseases, as well as cardiovascular and diabetic diseases. Some isoform-nonselective HDAC inhibitors have been successfully used for clinical treatments of the haematological malignancies, including advanced forms of cutaneous T-cell lymphoma, refractory peripheral T-cell lymphoma and multiple myeloma...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928958/short-and-long-term-effects-of-a-dpp-4-inhibitor-versus-bedtime-nph-insulin-as-add-on-therapy-in-patients-with-type-2-diabetes
#7
Giordana Maluf da Silva, Katia Camarano Nogueira, Rosa Tsuneshiro Fukui, Marcia Regina Soares Correia, Rosa Ferreira Dos Santos, Maria Elizabeth Rossi da Silva
BACKGROUND: We conducted a comparison between the dipeptidyl-peptidase-4(DPP-4) inhibitor sitagliptin versus NPH insulin as an add-on therapies in patients with type 2 diabetes mellitus (T2D) failing oral medications. The objective was to ascertain the better indication in long-duration diabetes. METHODS: thirty-five T2D patients inadequately controlled with metformin plus glyburide were randomized to receive sitagliptin (n=18) or bedtime NPH insulin (n=17) for 12 months...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928957/long-circulating-liposomal-delivery-system-targeting-at-pdgfr-%C3%AE-enhances-the-therapeutic-effect-of-ifn-%C3%AE-on-hepatic-fibrosis
#8
Qinghua Li, Qi Yu, Jing Ju, Tiangeng You, Zhiqiang Yan, Xiangli Nan, Jie Zhong, Jing E Zhou
BACKGROUND: In this study, we developed a drug of IFN-α combined with pPB-SSLs, which specifically target at platelet-derived growth factor receptor-β (PDGFR-β). AIM: The aim of this study is to improve the limitations of IFN-α including insufficient drug concentration for the target cells and side-effects causing serious concerns in treatment of hepatic fibrosis. METHODS: We constructed the targeted stable liposomes (SSLs) that not only increase the half-life period of IFN-α, but also can deliver IFN-α to hepatic stellate cells (HSCs)...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928956/chemical-properties-of-caffeic-and-ferulic-acids-in-biological-system-implications-in-cancer-therapy-a-review
#9
Sarah S Damasceno, Bruna B Dantas, Demetrius Antônio M Araújo, José Galberto M da Costa
Caffeic and ferulic acids have been extensively evaluated for their antioxidant properties in biological system, such activity is responsible for limiting the excessive production of free radical species, that are associated with cell proliferation. However, more recent studies suggest chemopreventive action of these phenolic acids through the regulation of gene expression, chelation and / or reduction of transition metals, covalent adduct formation (which damage DNA) and toxicity. The biological efficacy of these promising chemopreventive agents depends strongly on their chemical structure...
December 8, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928968/rationale-for-assessing-safety-and-efficacy-of-drug-candidates-alone-and-in-combination-with-medical-devices-the-case-study-of-spinalontm
#10
Pierre A Guertin
The aim of this review is to describe the rationale and main underlying reasons for undertaking, during clinical development, the study of drug candidates used separately and/or in combination with other technologies. To ease comprehension, reference will be made to the case of SpinalonTM, a new fixed-dose combination (FDC) product composed of levodopa/carbidopa/buspirone. This drug is capable of triggering, within minutes after a single administration orally, 45 minute- episodes of basic involuntary 'reflex' walking in paraplegic animals...
December 7, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928967/hot-topics-in-dry-eye-disease
#11
Pablo Alberto Chiaradia, Luis Alberto Zeman Bardeci, Sebastián Dankert, Marcos Omar Mendaro, Andrzej Grzybowski
BACKGROUND: Dry eye disease (DED) is a multifactorial disease of the tears and ocular surface that results in symptoms such as discomfort, visual disturbance, and tear film instability, with potential damage to the ocular surface. The principal pathological mechanisms of DED are hyperosmolarity and inflammation. These mechanisms are deeply interrelated and lead to a self-perpetuating "vicious circle". METHODS: The objective of this review is to describe novel pharmacological and non-pharmacological treatments for DED...
December 7, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928966/hot-topics-in-perioperative-antibiotics-for-cataract-surgery
#12
Patrycja Kuklo, Andrzej Grzybowski, Stephen G Schwartz, Harry W Flynn, Avinash Pathengay
BACKGROUND: Acute-onset postoperative endophthalmitis is an uncommon but potentially serious complication of cataract surgery. Since there are relatively few randomized clinical trials comparing the timing and administration of prophylactic antibiotics, there are wide variations in prevention practices around the world. METHODS: Literature review. RESULTS: Antibiotics may be used before surgery, during surgery, or after surgery in an attempt to decrease the rates of endophthalmitis...
December 7, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27928965/targeting-the-hedgehog-pathway-for-locally-advanced-and-metastatic-basal-cell-carcinoma
#13
Vivian T Yin, Bita Esmaeli
Basal cell caricnoma (BCC), the most common periocular magliancy, is treated with complete surgical excision. However, in patients not amenable to surgery or when surgical resection means loss of vital organs or disfiguring procedures due to locally advanced or metastatic disease, targeting the hedgehog pathway offers anovel treatment approach for such patients. Mutation in PTCH1 and SMO has been identified in patients with basal cell nevoid syndrome as well as in patients with sporadic BCC. Inhibition of SMO by vismodegib or sonidegib, the two sonic hedgehog inhibitor drugs approved by the Food and Drug Administration in the United States, has shown overall response rate for locally advanced and metastatic BCC around 50%...
December 7, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27924726/neurodegenerative-disease-a-perspective-on-cell-based-therapy-in-the-new-era-of-cell-free-nano-therapy
#14
Su M Metcalfe, Sean Bickerton, Tarek Fahmy
Neurodegenerative diseases (NDD) result in irreversible loss of neurons. Dementia develops when disease-induced neuronal loss becomes sufficient to impair both memory and cognitive functioning and, globally, dementia is increasing to epidemic proportions as populations age. In the current era of regenerative medicine intense activity is asking, can loss of endogenous neurons be compensated by replacement with exogenously derived cells that have either direct, or indirect, neurogenic capacity? But, more recently, excitement is growing around an emerging alternative to the cell-based approach - here nanotechnology for targeted delivery of growth factor aims to support and expand resident central nervous system (CNS) stem cells for endogenous repair...
December 6, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27917718/the-role-of-rho-kinase-inhibitors-in-corneal-endothelial-dysfunction
#15
Naoki Okumura, Shigeru Kinoshita, Noriko Koizumi
BACKGROUND: The cornea is transparent tissue that serves as the window of the eye, allowing light to enter from the outer environment. The corneal endothelium maintains corneal transparency; thus, its dysfunction results in corneal haziness and causes severe vision loss. The only available therapeutic choice for treating corneal endothelial dysfunction has been transplantation using donor corneas; consequently, researchers have been pressed to develop new therapeutic options. METHODS: The goal of the review is to provide an overview of the research into Rho kinase (ROCK) inhibitors in the field of corneal endothelium therapy and the potential for clinical use of ROCK inhibitors...
December 5, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27917717/reversal-agents-for-oral-antiplatelet-and-anticoagulant-treatment-during-bleeding-events-current-strategies
#16
Peter Raimondi, Elaine M Hylek, Konstantinos N Aronis
There is an increasing prevalence of cardiovascular diseases that warrant antithrombotic therapy. Antithrombotic therapy includes antiplatelet agents and anticoagulation therapy with vitamin K antagonists (VKAs) or non-Vitamin K oral anticoagulants (NOACs). Antithrombotic therapy is associated with increased rates of bleeding. In this review we summarize the evidence and provide strategies for the management of severe bleeding in the setting of antithrombotic therapy. There is limited data on the management of bleeding in the setting of antiplatelet therapy...
December 5, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27917716/antithrombotic-treatment-management-in-patients-with-intracerebral-hemorrhage-reversal-and-restart
#17
Dimitrios Giakoumettis, George A Alexiou, Dimitrios A Vrachatis, Kostas Themistoklis, Pantelis Stathis, Manolis Vavuranakis, Marios S Themistocleous
BACKGROUND: Intracerebral hemorrhage is the pathological accumulation of blood within the brain. It is a type of stroke more likely to be lethal or to severely disable the patient and results from a wide variety of causes. On the other hand antithrombotic therapy is used for the prevention or/and the therapy of thromboembolic episodes. Antithrombotic drugs are very effective in reducing risk or mortality rate after a thromboembolic event, yet they are associated with significant hemorrhages...
December 5, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27917715/antiplatelet-agents-and-anticoagulants-in-patients-with-chronic-kidney-disease-from-pathophysiology-to-clinical-practice
#18
Jens Lutz, Kerstin Jurk
Progressive impairment of renal function can lead to uremia, which is associated with thus increasing the risk of bleeding as well as thrombosis. Furthermore, many patients with chronic kidney disease (CKD) have an indication for an anticoagulation or antiplatelet therapy due to atrial fibrillation, coronary artery disease, thromboembolic disease, or peripheral artery disease. The treatment usually includes vitamin-K antagonists (VKAs) and/or platelet aggregation inhibitors. The direct oral anticoagulants (DOACs) inhibiting factor Xa or thrombin activity represent an alternative for heparins and VKAs...
December 5, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27917714/antiplatelet-and-anticoagulation-treatment-in-patients-with-thrombocytopenia
#19
Nuccia Morici, Silvia Cantoni, Paola Vallerio, Marco Cattaneo, Stefano Savonitto
Thrombocytopenia (TP) is a common finding in patients hospitalized for cardiovascular causes and needing antiplatelet and anticoagulant therapies. However, TP is not only a numeric parameter, but mostly a dynamic condition affected by the patients' underlying disorders and concomitant treatments. Platelets are important players in the hemostatic process, taking part to both primary and secondary hemostasis. Although both TP and antithrombotic treatment contribute to the risk of bleeding, the complexity of the pathogenesis of bleeding events makes it difficult to predict them accurately simply based on these two parameters...
December 5, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27917713/antiplatelets-and-antithrombotics-in-patients-with-liver-insufficiency-from-pathophysiology-to-clinical-practice
#20
Melanie Deutsch, John Koskinas
The liver represents the site of synthesis of most procoagulant and anticoagulant factors, fibrinolytic proteins and thrombopoetin while being also involved in the clearance of hemostatic and fibrinolyic proteins. Therefore in patients with liver insufficiency a great variety of disturbances can be documented resulting however in a new "rebalanced" hemostatic system with a labile equilibrium between thromboses or bleeding. Interestingly patients with liver insufficiency may present with arterial or venous thrombotic episodes requiring antiplatelet and/or antithrombotic therapy despite low platelet count or prolonged INR...
December 5, 2016: Current Pharmaceutical Design
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