نتایج جستجو برای: low bioavailable drug

تعداد نتایج: 1728796  

Journal: :Molecular cancer therapeutics 2009
Heath A Elrod Ping Yue Fadlo R Khuri Shi-Yong Sun

Perifosine is an orally bioavailable alkylphospholipid currently being tested in phase II clinical trials as a potential anticancer drug. In this study, we reveal a novel mechanism underlying the anticancer activity of perifosine that involves the induction of cyclooxygenase 2 (COX-2) in human cancer cells. Perifosine induced apoptosis and/or cell cycle arrest in several lung and head and neck ...

2014
Claudia M. Calvet Debora F. Vieira Jun Yong Choi Danielle Kellar Michael D. Cameron Jair Lage Siqueira-Neto Jiri Gut Jonathan B. Johnston Li Lin Susan Khan James H. McKerrow William R. Roush Larissa M. Podust

CYP51 is a P450 enzyme involved in the biosynthesis of the sterol components of eukaryotic cell membranes. CYP51 inhibitors have been developed to treat infections caused by fungi, and more recently the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease. To specifically optimize drug candidates for T. cruzi CYP51 (TcCYP51), we explored the structure-activity relationshi...

2006
David Porta George S. Bullerjahn Michael R. Twiss Steven W. Wilhelm Leo Poorvin Michael L. McKay

Low Fe bioavailability has been suggested as a potential constraint on primary production in the Great Lakes. Here we report on the use of a cyanobacterial bioreporter to assess available Fe in Lake Erie during summer and fall field seasons in 2001–02. Bioreporter luminescence was derived from a luciferase reporter controlled by iron-responsive promoter element isiAB. Filtered (< 0.2 μm) water ...

Journal: :Environmental Chemistry 2016

2013
G. Sahitya B. Krishnamoorthy M. Muthukumaran

Recently sustained release dosage forms has become standards in the modern pharmaceutical design and intensive research has been undertaken in achieving much better drug product effectiveness. The sustained release product will optimize therapeutic effect and safety of a drug at the same time improving patient convenience and compliance. Prior to the development of these major dosage forms, it ...

Journal: :Neurobiology of aging 2013
Eugene O'Hare David I C Scopes Eun-Mee Kim Philip Palmer Martyn Jones Andrew D Whyment David Spanswick Hozefa Amijee Edmund Nerou Bridgeen McMahon J Mark Treherne Ross Jeggo

Oligomers of beta-amyloid (Aβ) are implicated in the early memory impairment seen in Alzheimer's disease before to the onset of discernable neurodegeneration. Here, the capacity of a novel orally bioavailable, central nervous system-penetrating small molecule 5-aryloxypyrimidine, SEN1500, to prevent cell-derived (7PA2 [conditioned medium] CM) Aβ-induced deficits in synaptic plasticity and learn...

2015
Srinivasan Shanmugam

Pharmaceutical companies around the globe have always been in the urge of discovering innovative blockbuster drugs for various ailments by spending billions of dollars for the drug discovery programmes. Although identification of new chemical entities (NCEs) with alternate mode of actions for diseases is a primary concern for the pharmaceutical companies, application of innovative techniques an...

2016
Alexandros Fiamegos John Varkarakis Michael Kontraros Andreas Karagiannis Michael Chrisofos Dimitrios Barbalias Charalampos Deliveliotis

INTRODUCTION Data from animal, clinical and prevention studies support the role of androgens in prostate cancer growth, proliferation and progression. Results of serum based epidemiologic studies in humans, however, have been inconclusive. The present study aims to define whether serum testosterone can be used as a predictor of a posi¬tive second biopsy in males considered for re-biopsy. MATE...

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