Differential suppression of the aryl hydrocarbon receptor nuclear translocator-dependent function by an aryl hydrocarbon receptor PAS-A-derived inhibitory molecule.

The aryl hydrocarbon receptor (AhR) heterodimerizes with the aryl hydrocarbon receptor nuclear translocator (Arnt) for transcriptional regulation. We generated three N-terminal deletion constructs of the human AhR of 12-24 kDa in size--namely D1, D2, and D3--to suppress the Arnt function. We observed that all three deletions interact with the human Arnt with similar affinities.

The acute antinociceptive effect of hyperbaric oxygen is not accompanied by an increase in markers of oxidative stress.

Aims: Exposure to hyperbaric oxygen (HBO2) causes an antinociceptive response in mice. However, breathing oxygen (O2) at an elevated pressure can potentially cause oxygen toxicity. The aim of this study was to identify the determinants of HBO2 antinociception and the toxicity profile of HBO2.

Basic concepts in opioid prescribing and current concepts of opioid-mediated effects on driving.

Background: Many patients with chronic pain receive substandard analgesic therapy. Incomplete or inadequate care often stems from physician fears of patient addiction and/or drug toxicity. As a result, many chronic pain patients are undertreated and have unrelieved pain that tempts them to overuse or to abuse prescribed pharmacologic treatments.

Novel ortho ester-based, pH-sensitive cationic lipid for gene delivery in vitro and in vivo.

Context: Cationic lipoplexes are less toxic than viral gene vectors and more convenient to prepare but their efficiencies of gene delivery are generally lower.

Objective: To develop ortho ester-based, pH-sensitive lipoplexes for efficient gene delivery both in cultured cells and in vivo.

Materials And Methods: A novel cationic and acid-labile lipid (DOC) containing a cationic headgroup and a cholesterol-derived lipid tail joined together by an acid-labile ortho ester linker was designed and synthesized.

Effects of caffeinated versus decaffeinated energy shots on blood pressure and heart rate in healthy young volunteers.

Study Objective: To evaluate the effects of a caffeinated 5-hour Energy shot compared with a decaffeinated 5-hour Energy shot as assessed by changes in blood pressure and heart rate in healthy, nonhypertensive volunteers.

Design: Randomized, double-blind, controlled, crossover study.

Setting: University campus.

Use of simulation-based teaching methodologies in US colleges and schools of pharmacy.

OBJECTIVES. To characterize the use of high-fidelity mannequins and standardized patients in US pharmacy colleges and schools. METHODS.

A cell-penetrating peptide suppresses the hypoxia inducible factor-1 function by binding to the helix-loop-helix domain of the aryl hydrocarbon receptor nuclear translocator.

The heterodimeric hypoxia inducible factor-1 (HIF-1) complex is composed of the hypoxia inducible factor-1 alpha (HIF-1α) and the aryl hydrocarbon receptor nuclear translocator (ARNT). Activation of the HIF-1 function is essential for tumor growth and metastasis. We previously showed that transfection of a plasmid containing an ARNT-interacting peptide (Ainp1) cDNA suppresses the HIF-1 signaling in Hep3B cells.

Variations in risk assessment models may contribute to the existing gap between venous thromboembolism prophylaxis guidelines and adherence.

Background: Risk assessment models (RAMs) may allow the clinician to determine need for deep vein thrombosis (DVT) prophylaxis. Individual healthcare facilities often develop their own RAMs. The purpose of this study was to determine: 1.

Molecular docking and synthesis of novel quinazoline analogues as inhibitors of transcription factors NF-κB activation and their anti-cancer activities.

NF-kB is a transcription factor protein complex that can be found in almost all animal cell types and is a key player in some cancers and inflammatory responses. It can enhance the proliferation rate, reduce apoptosis, as well as creating more blood flow to ensure the survival of cancer, thus blocking the NF-kB pathway has potential therapeutic benefit. We designed a series of compounds based on a quinazoline scaffold pharmacophore model which may have high binding affinity with the p50 subunit of NF-kB.

In silico model of drug permeability across sublingual mucosa.

The objective of this work was to develop an in silico model to predict the sublingual permeability of a drug based on physicochemical descriptors of a molecule. Fourteen model drugs with diverse physicochemical properties were selected for this study. Molecular volume, molecular weight, logP, logD (pH 6.

Redefining the role of the pharmacist: medication therapy management.

Purpose: The purpose of this paper is to explore better use of pharmacists in rural communities as a partial solution to scarcity of physicians and other health care providers. It discusses expected reduction in public subsidies for rural health care and the changing market for pharmacists. The paper emphasizes the use of pharmacists as a backdrop for description of medication therapy management (MTM).

Development and assessment of social and emotional competence through simulated patient consultations.

Objective: To determine whether a quantitative tool could be used to measure social emotional competence and whether the development of social emotional competence through a pharmacy practicum course is possible.

Design: First-year pharmacy students completed the Social Emotional Development Inventory (SED-I) online and then participated in a series of mock patient consultations on smoking cessation and nonprescription medication.

Assessment: The 212 students enrolled in the course completed the SED-I.

Assessing quality of life in an ambulatory medicare population.

Objective: Medicare beneficiaries have unique health-related challenges causing significant impact on quality of life. This study examined the overall health-related quality of life (HRQOL) and differences in HRQOL between subgroups of an ambulatory Medicare beneficiary population.

Methods: Nine outreach events were held during the 2011 Medicare Part D prescription drug open-enrollment period, in which 397 beneficiaries were assisted with Part D plan evaluation and comprehensive medication therapy review.

Sex differences in mesenteric endothelial function of streptozotocin-induced diabetic rats: a shift in the relative importance of EDRFs.

Several studies suggest that diabetes affects male and female vascular beds differently. However, the mechanisms underlying the interaction of sex and diabetes remain to be investigated. This study investigates whether there are 1) sex differences in the development of abnormal vascular responses and 2) changes in the relative contributions of endothelium-derived relaxing factors in modulating vascular reactivity of mesenteric arteries taken from streptozotocin (STZ)-induced diabetic rats at early and intermediate stages of the disease (1 and 8 wk, respectively).

Evaluation of pharmacy practice residents' research abstracts and publication rate.

Objective: To determine the type, scope, and publication rate of pharmacy practice residency projects conducted in a subgroup of the United States.

Methods: Data were collected from the abstract book of the 28th Western States Conference for Pharmacy Residents, Fellows, and Preceptors (May 20-23, 2008). Data on project publication rate, institution affiliation, residency year, research practice setting, research therapeutic area, research hypothesis category, study design, statistical plan, and abstract reporting were extracted independently by two investigators.

Impact of an elective course on pharmacy students' attitudes, beliefs, and competency regarding Medicare Part D.

Objective: To determine the impact of an elective course on pharmacy students' perceptions, knowledge, and confidence regarding Medicare Part D, medication therapy management (MTM), and immunizations.

Design: Thirty-three pharmacy students were enrolled in a Medicare Part D elective course that included both classroom instruction and experiential training.

Assessment: Students' self-reported confidence in and knowledge of Part D significantly improved upon course completion.

Vemurafenib in patients with BRAF V600E mutation-positive advanced melanoma.

Background: Vemurafenib is an oral, small-molecule kinase inhibitor that selectively targets activated BRAF V600E and has been approved for the treatment of advanced BRAF mutation-positive melanoma.

Objective: This article reviews the clinical pharmacology, efficacy, tolerability, and pharmacokinetics of vemurafenib and in addition outlines proposed mechanisms of vemurafenib resistance.

Methods: A literature search of MEDLINE and ScienceVerse Scopus was performed using the key words malignant melanoma, BRAF, vemurafenib, and PLX4032.

Novel pH-sensitive cationic lipids with linear ortho ester linkers for gene delivery.

In an effort to develop pH-sensitive lipoplexes for efficient gene delivery, we report three novel cationic lipids containing a linear ortho ester linker that conjugates either the headgroup (Type I) or one hydrocarbon chain (Type II) with the rest of the lipid molecule. The cationic lipids carry either an iodide or a chloride counterion. Compared to our previously reported cyclic ortho ester linker, the linear ortho ester linker facilitated the construction of cationic liposomes and lipoplexes with different helper lipids.

Belimumab: review of use in systemic lupus erythematosus.

Background: Belimumab, a monoclonal antibody that inhibits B-lymphocyte stimulating protein, was the first biologic agent approved for, and the first drug approved in 55 years for, the treatment of systemic lupus erythematosus (SLE) by the US Food and Drug Administration (FDA).

Objective: This article reviews the current research on belimumab and provides recommendations on its use in the treatment of SLE.

Methods: The Cochrane Library, EBSCO, IPA, MEDLINE, and SCOPUS were searched for research published from January 2000 to November 2011, using the search terms belimumab, Benlysta, and Lympho-Stat B.

New oral anticoagulants for atrial fibrillation: a review of clinical trials.

Background: Warfarin had been the only oral anticoagulant for stroke prevention in patients with atrial fibrillation (AF) for decades. Direct thrombin inhibitors and factor Xa inhibitors are new anticoagulants recently approved for prevention of stroke or systemic embolism in patients with AF.

Objective: The aim of this article was to provide a systematic review of recently published clinical data on the direct thrombin inhibitors and factor Xa inhibitors in the management of AF.

Suppression of the hypoxia inducible factor-1 function by redistributing the aryl hydrocarbon receptor nuclear translocator from nucleus to cytoplasm.

The aryl hydrocarbon receptor nuclear translocator (ARNT) heterodimerizes with hypoxia inducible factor-1α (HIF-1α), followed by upregulation of genes that are essential for carcinogenesis. We utilized a novel peptide (Ainp1) to address whether the HIF-1α signaling could be suppressed by an ARNT-mediated mechanism. Ainp1 suppresses the HIF-1α-dependent luciferase expression in Hep3B cells and this suppression can be reversed by ARNT.