OBJECTIVE To evaluate the reliability of the Advanced Dundee Endoscopic Psychomotor Tester (ADEPT). DESIGN The Advanced Dundee Endoscopic Psychomotor Tester was developed for objective evaluation of bimanual endoscopic tasks. The system is in several aspects relevant to an actual endoscopic environment, and initial studies showed a strong correlation with clinical competence. Twenty medical s...

Non-steroidal anti-inflammatory drugs (NSAIDs) have been widely used for the management of inflammation, pain and nociception. Gastric intolerance caused by most of the NSAIDs used today restricts their use. Several approaches have been proposed to modify the parent NSAIDs molecule in order to reduce their gastric toxicity. Oral prodrug approach is one of such approaches. This review focuses on...

Pentabenzensulfonate (QPBS), a potential prodrug for quercetin, was designed and synthesized in high yield. It possesses better physical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kinetics than its original form. The LogP value (2.04) and the half-life of the hydrolysis value (3.85 h) show that oral bioavailability is improved evidently compared with ...

Compound 1 (IT-M-07000) was previously reported as a candidate prodrug of Am80 (Tamibarotene; used to treat acute promyelocytic leukemia), and shown to be efficiently metabolized to Am80 via β-oxidation. Here, we describe in detail the synthesis of 1, together with another tetradeuterated candidate prodrug, IT-YA-00616 (2), as well as two congeners, and several metabolic intermediates of 1 prev...

Prodrug design for brain delivery of small- and medium-sized neuropeptides was reviewed, focusing on thyrotropin-releasing hormone and structurally related peptides as examples. We have summarized our most important advances in methodology, as well as assessed the benefits and limitations of bioreversible chemical manipulation techniques to achieve targeting of the parent molecules into the cen...

induced phenotype in combination with the prodrug, there was a significant increase in cell death, with up to 80% of cells dead after 48 hours. Lee et al then performed real-time tracking of prodrug activation in cancer cell cultures. Twenty-four hours after treatment with radiation and prodrug, more than half of the doxorubicin had been activated and localized to the nucleus. Without radiation...

Activation of the prodrug 4-iodo-3-nitrobenzamide critically depends on the cellular reducing system specific to cancer cells. In non-malignant cells, reduction of this prodrug to the non-toxic amine occurs by the flavoprotein of complex?I of mitochondria receiving Mg2+-ATP-dependent reducing equivalents from NADH to NADPH via pyridine nucleotide transhydrogenation. This hydride transfer is def...

The aim of this study was to synthesize a peptide prodrug of glucosamine (GlcN) with increased gut permeability through the gut peptide transporter 1 (PepT1). Glycine-Valine ester derivative of GlcN (GVG) was synthesised using solid phase synthesis followed by characterization and evaluation of its physicochemical and intestinal stability. In addition, GVG was evaluated for its ability to be bi...

PURPOSE Combination therapy is increasingly used as a primary cancer treatment regimen. In this report, we designed EGFR peptide decorated nanoparticles (NPs) to co-deliver docetaxel (DTX) and pH sensitive curcumin (CUR) prodrug for the treatment of prostate cancer. RESULTS EGFR peptide (GE11) targeted, pH sensitive, DTX and CUR prodrug NPs (GE11-DTX-CUR NPs) had an average diameter of 167nm ...