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https://www.readbyqxmd.com/read/28944908/hypermethylation-of-wif1-and-its-inhibitory-role-in-the-tumor-growth-of-endometrial-adenocarcinoma
#1
Xinchao Deng, Congzhe Hou, Huali Wang, Tingting Liang, Lin Zhu
Endometrial carcinoma is the most common malignancy of the female genital tract and is the fourth most common malignancy among women worldwide. Endometrial adenocarcinoma (EAC) accounts for ~80% of endometrial carcinoma cases. Numerous critical genetic events have been determined to serve an essential role in EAC progression; however, the precise molecular mechanisms underlying EAC progression remain unclear. Pyrosequencing and methylation‑specific PCR were used to detect the methylation status of Wnt inhibitory factor 1 (WIF1)...
September 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944885/exploring-the-key-genes-and-pathways-of-osteosarcoma-with-pulmonary-metastasis-using-a-gene-expression-microarray
#2
Zhongju Shi, Hengxing Zhou, Bin Pan, Lu Lu, Zhijian Wei, Linlin Shi, Xue Yao, Yi Kang, Shiqing Feng
Osteosarcoma is a common and highly malignant tumour in children and teenagers that is characterized by drug resistance and high metastatic potential. Patients often develop pulmonary metastasis and have a low survival rate. However, the mechanistic basis for pulmonary metastasis remains unclear. To identify key gene and pathways associated with pulmonary metastasis of osteosarcoma, the authors downloaded the gene expression dataset GSE85537 and obtained the differentially expressed genes (DEGs) by analyzing high‑throughput gene expression in primary tumours and lung metastases...
September 21, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944856/systemic-overexpression-of-the-11%C3%AE-%C3%A2-hsd1-promotes-endoplasmic-reticulum-stress-in-multiple-tissues-and-the-development-of-metabolic-syndrome-in-mice
#3
Chenxiao Li, Jihan Xia, Wenjuan Zhu, Leilei Xin, Cuiping An, Shulin Yang, Kui Li
Glucocorticoids are associated with lipid metabolism and their abnormal expression has an important function in the development of metabolic syndrome. The 11β‑hydroxysteroid dehydrogenase type 1 (11β‑HSD1) is a metabolic enzyme of glucocorticoids and may be a potential drug target for the treatment of metabolic syndrome. However, the association between the systemic expression of 11β‑HSD1 and metabolic syndrome remains to be elucidated. The present study used a cytomegalovirus promoter to obtain mice that systemically overexpressed the 11β‑HSD1 gene...
September 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944848/cmip-is-oncogenic-in-human-gastric-cancer-cells
#4
Jianlin Zhang, Jin Huang, Xingyu Wang, Weidong Chen, Qinqing Tang, Maoyong Fang, Yeben Qian
Gastric cancer is one of the most common cancers and the second leading cause of cancer‑associated mortality worldwide. Recurrence, metastasis and resistance to drug treatment are the main barrier to survival of patients with advanced stage gastric cancer. Further study of the molecular mechanisms involved will improve the therapeutic options for gastric cancer. In a previous study, c‑Maf was discovered as an oncogene transduced in the avian AS42 retrovirus, and was found to be overexpressed in multiple myeloma and angioimmunoblastic T‑cell lymphoma...
September 20, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944829/thymic-function-in-the-regulation-of-t-cells-and-molecular-mechanisms-underlying-the-modulation-of-cytokines-and-stress-signaling-review
#5
Fenggen Yan, Xiumei Mo, Junfeng Liu, Siqi Ye, Xing Zeng, Dacan Chen
The thymus is critical in establishing and maintaining the appropriate microenvironment for promoting the development and selection of T cells. The function and structure of the thymus gland has been extensively studied, particularly as the thymus serves an important physiological role in the lymphatic system. Numerous studies have investigated the morphological features of thymic involution. Recently, research attention has increasingly been focused on thymic proteins as targets for drug intervention. Omics approaches have yielded novel insights into the thymus and possible drug targets...
September 19, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944823/integrated-strategy-of-differentially-expressed-genes-associated-with-ulcerative-colitis
#6
Juerong Feng, Qian Gao, Qing Liu, Fan Wang, Xue Lin, Qiu Zhao, Jing Liu, Jin Li
Ulcerative colitis (UC) is a chronic inflammatory bowel disease that is associated with both genetic and environmental factors; however, the underlying pathogenesis of UC remains unclear. The present study aimed to further explore 12 microarray datasets from patients with UC obtained from the Gene Expression Omnibus repository, for potential genetic pathogenesis of UC through a global bioinformatics view, which included identification of differentially expressed genes (DEGs), functional enrichments, protein‑protein interactions, transcriptional and post‑transcriptional regulation and drug‑gene associations...
September 18, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28944770/targeting-microbial-biofilms-current-and-prospective-therapeutic-strategies
#7
REVIEW
Hyun Koo, Raymond N Allan, Robert P Howlin, Paul Stoodley, Luanne Hall-Stoodley
Biofilm formation is a key virulence factor for a wide range of microorganisms that cause chronic infections. The multifactorial nature of biofilm development and drug tolerance imposes great challenges for the use of conventional antimicrobials and indicates the need for multi-targeted or combinatorial therapies. In this Review, we focus on current therapeutic strategies and those under development that target vital structural and functional traits of microbial biofilms and drug tolerance mechanisms, including the extracellular matrix and dormant cells...
September 25, 2017: Nature Reviews. Microbiology
https://www.readbyqxmd.com/read/28944765/folate-receptor-targeted-nir-sensitive-polydopamine-nanoparticles-for-chemo-photothermal-cancer-therapy
#8
Hao Li, Zhen Jin, Sunghoon Cho, Mi Jeong Jeon, Van Du Nguyen, Jong-Oh Park, Sukho Park
We propose the use of folate-receptor-targeted, near-infrared-sensitive polydopamine nanoparticles (NPs) for chemo-photothermal cancer therapy as an enhanced type of drug-delivery system which can be synthesized by in situ polymerization and conjugation with folic acid. The NPs consist of a Fe3O4/Au core, coated polydopamine, conjugated folic acid, and loaded anti-cancer drug (doxorubicin). The proposed multifunctional NPs show many advantages for therapeutic applications such as good biocompatibility and easy bioconjugation...
September 25, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28944736/liposomes-for-the-delivery-of-streptokinase
#9
Lalit Kumar, Shivani Verma, Bhuvaneshwar Vaidya
Streptokinase is an efficient thrombolytic agent used to treat thromboembolic disorders. Conventional streptokinase formulations have limited thrombolytic activity and several shortcomings because of their immunogenicity and dose-related side effects including short half-life, lack of tissue targeting and peripheral bleeding. Different liposomal formulations have been explored by researchers in order to improve thrombolytic activity of streptokinase. Liposomal formulations could improve plasma stability, retain drug for longer periods of time in the circulation and promote selective delivery to the thrombus...
October 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28944735/strategies-in-the-design-of-gold-nanoparticles-for-intracellular-targeting-opportunities-and-challenges
#10
Yamin Yang, Lei Ren, Hongjun Wang
With unique physicochemical properties, gold nanoparticles (Au NPs) have demonstrated their potential as drug carriers or therapeutic agents. Effective guidance of Au NPs into specific intracellular destinations becomes increasingly important as we strive to further improve the efficiency of drug delivery and modulate controllable cellular responses. In this review, we summarized recent advances in designing Au NPs with the capabilities of cellular penetration and internalization, endosomal escape, intracellular trafficking and subcellular localization via various approaches including physical injection, tuning the physiochemical parameters of Au NPs, and surface modification with targeting ligands...
October 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28944731/the-fda-unapproved-drugs-initiative-an-observational-study-of-the-consequences-for-drug-prices-and-shortages-in-the-united-states
#11
Ravi Gupta, Sanket S Dhruva, Erin R Fox, Joseph S Ross
BACKGROUND: Hundreds of drug products are currently marketed in the United States without approval from the FDA. The 2006 Unapproved Drugs Initiative (UDI) requires manufacturers to remove these drug products from the market or obtain FDA approval by demonstrating evidence of safety and efficacy. Once the FDA acts against an unapproved drug, fewer manufacturers remain in the market, potentially enabling drug price increases and greater susceptibility to drug shortages. There is a need for systematic study of the UDI's effect on prices and shortages of all targeted drugs...
October 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28944729/using-performance-based-risk-sharing-arrangements-to-address-uncertainty-in-indication-based-pricing
#12
Kai Yeung, Meng Li, Josh J Carlson
BACKGROUND: The rise in pharmaceutical expenditures in recent years has increased health care payer interest in ensuring good value for the money. Indication-based pricing (IBP) sets separate, indication-specific prices paid to the manufacturer according to the expected efficacy of a drug in each of its indications. IBP allows payers to consistently pay for value across indications. While promising, a limitation of IBP as originally conceived is that efficacy estimates are typically based on clinical trial data, which may differ from real-world effectiveness...
October 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28944677/a-multiplex-and-label-free-relative-quantification-approach-for-studying-protein-abundance-of-drug-metabolizing-enzymes-in-human-liver-microsomes-using-swath-ms
#13
Rohitash Jamwal, Benjamin J Barlock, Sravani Adusumalli, Ken Ogasawara, Brigitte L Simons, Fatemeh Akhlaghi
We describe a sequential windowed acquisition of all theoretical fragment ion mass spectra (SWATH-MS) based method for label-free, simultaneous, relative quantification of drug metabolism enzymes in human liver microsomes (HLM; n=78). In-solution tryptic digestion was aided by a pressure cycling method which allowed a 90-min incubation time, a significant reduction over classical protocols (12-18 h). Digested peptides were separated on an Acquity UHPLC Peptide BEH C18 column using a 60-min gradient method at a flow rate of 0...
September 25, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28944613/propensity-score-matched-all-comers-population-treated-with-ultra-thin-strut-bare-metal-and-sirolimus-probucol-coated-drug-eluting-stents-of-identical-stent-architecture
#14
Florian Krackhardt, Mohd Ali Rosli, Matthias Leschke, André Schneider, Christian Sperling, Tay Mok Heang, Maxime Pons, Pedro Jerónimo Sousa, Behrouz Kherad, Matthias Waliszewski
OBJECTIVE: The objective of this study was to compare the safety and efficacy of a polymer-free sirolimus coated, ultrathin strut drug eluting stent (PF-SES) to its uncoated bare-metal stent (BMS) platform of identical stent architecture. BACKGROUND: Recently published randomized trials comparing BMS to DES with a focus on shortened dual-antiplatelet therapy reported incidences of stent thrombosis (ST) and bleeding complications (LEADERS FREE) in favor of drug eluting stents (DES)...
September 25, 2017: Catheterization and Cardiovascular Interventions
https://www.readbyqxmd.com/read/28944587/finding-the-genetic-mechanisms-of-folate-deficiency-and-neural-tube-defects-leaving-no-stone-unturned
#15
REVIEW
Kit Sing Au, Tina O Findley, Hope Northrup
Neural tube defects (NTDs) occur secondary to failed closure of the neural tube between the third and fourth weeks of gestation. The worldwide incidence ranges from 0.3 to 200 per 10,000 births with the United States of American NTD incidence at around 3-6.3 per 10,000 dependent on race and socioeconomic background. Human NTD incidence has fallen by 35-50% in North America due to mandatory folic acid fortification of enriched cereal grain products since 1998. The US Food and Drug Administration has approved the folic acid fortification of corn masa flour with the goal to further reduce the incidence of NTDs, especially among individuals who are Hispanic...
September 25, 2017: American Journal of Medical Genetics. Part A
https://www.readbyqxmd.com/read/28944571/ensemble-docking-to-difficult-targets-in-early-stage-drug-discovery-methodology-and-application-to-fibroblast-growth-factor-23
#16
Hector A Velazquez, Demian Riccardi, Zhousheng Xiao, L Darryl Quarles, C Ryan Yates, Jerome Baudry, Jeremy C Smith
Ensemble docking is now commonly used in early-stage in silico drug discovery, and can be used to attack difficult problems such as finding lead compounds which can disrupt protein:protein interactions. We give an example of this methodology here, as applied to fibroblast growth factor 23 (FGF23), a protein hormone that is responsible for regulating phosphate homeostasis. The first small molecule antagonists of FGF23 were recently discovered by combining ensemble docking with extensive experimental target validation data(1) ...
September 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28944552/an-av-rgd-integrin-inhibitor-toolbox-drug-discovery-insight-challenges-and-opportunities
#17
Richard Hatley, Simon Macdonald, Robert Slack, Joelle Le, Steve Ludbrook, Pauline Lukey
There is a requirement for efficacious and safe medicines to treat diseases with high unmet need. The resurgence in av RGD integrin inhibitor drug discovery is poised to contribute to this requirement. However, drug discovery in the av integrin space is notoriously difficult due to the receptors being structurally very similar as well as the polar zwitterionic nature of the pharmacophore. This review aims to guide drug discovery research in this field through an av inhibitor toolbox, consisting of small molecules and antibodies...
September 25, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28944496/the-unidirectional-hypoxia-activated-prodrug-oct1002-inhibits-growth-and-vascular-development-in-castrate-resistant-prostate-tumors
#18
Heather Nesbitt, Jenny Worthington, Rachel J Errington, Laurence H Patterson, Paul J Smith, Stephanie R McKeown, Declan J McKenna
BACKGROUND: OCT1002 is a unidirectional hypoxia-activated prodrug (uHAP) OCT1002 that can target hypoxic tumor cells. Hypoxia is a common feature in prostate tumors and is known to drive disease progression and metastasis. It is, therefore, a rational therapeutic strategy to directly target hypoxic tumor cells in an attempt to improve treatment for this disease. Here we tested OCT1002 alone and in combination with standard-of-care agents in hypoxic models of castrate-resistant prostate cancer (CRPC)...
September 24, 2017: Prostate
https://www.readbyqxmd.com/read/28944416/regulating-the-alky-chain-length-of-fatty-acid-didanosine-prodrugs-and-evaluating-its-role-in-albumin-binding
#19
Hongxiang Chen, Gang Wang, Lanzhen Sun, Huicong Zhang, Mengchi Sun, Jin Sun, Lei Shang, Cong Luo
Rational design of prodrugs for efficient albumin binding shows distinct advantages in drug delivery in terms of drug availability, systemic circulation, and potential targeting effect. And fatty acids are good candidates due to their high affinity to albumin. However, how the alkyl chain length of fatty acids affects the binding dynamics between prodrugs and albumin, despite its importance, is still unclear. In the present study, three prodrugs of didanosine (DDI) and fatty acids were designed and synthesized to evaluate the effect of the alkyl chain length on prodrug-albumin binding process, including capric acid-didanosine (CA-DDI), myristic acid-didanosine (MA-DDI), and stearic acid-didanosine (SA-DDI)...
September 24, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28944107/ensemble-molecular-dynamics-of-a-protein-ligand-complex-residual-inhibitor-entropy-enhances-drug-potency-in-butyrylcholinesterase
#20
Eric J Sorin, Walter Alvarado, Samantha Cao, Amethyst Radcliffe, Phuc La, Yi An
Butyrylcholinesterase is a key enzyme that catalyzes the hydrolysis of the neurotransmitter acetylcholine and shows an increased activity in patients suffering from Alzheimer's disease (AD), making this enzyme a primary target in treating AD. Central to this problem, and to similar scenarios involving biomolecular recognition, is our understanding of the nature of the protein-ligand complex. The butyrylcholinesterase enzyme was studied via all-atom, explicit solvent, ensemble molecular dynamics simulations sans inhibitor and in the presence of three dialkyl phenyl phosphate inhibitors of known potency to a cumulative sampling of over 40 μs...
2017: Bioenergetics: Open Access
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