In spite of increasing evidence that
parasitic worms may protect
humans from developing allergic and autoimmune diseases and the continuing
identification of defined helminth-derived immunomodulatory molecules,
to date no new anti-inflammatory drugs have been developed from these
organisms. We have approached this matter in a novel manner by synthesizing
a library of drug-like small molecules based upon phosphorylcholine,
the active moiety of the anti-inflammatory Acanthocheilonema
viteae product, ES-62, which as an immunogenic protein
is unsuitable for use as a drug. Following preliminary in vitro screening
for inhibitory effects on relevant macrophage cytokine responses,
a sulfone-containing phosphorylcholine analogue (11a)
was selected for testing in an in vivo model of inflammation, collagen-induced
arthritis (CIA). Testing revealed that 11a was as effective
as ES-62 in protecting DBA/1 mice from developing CIA and mirrored
its mechanism of action in downregulating the TLR/IL-1R transducer,
MyD88. 11a is thus a novel prototype for anti-inflammatory
drug development.
Mathematical ability is a major contributory factor to the success of a student in any science course. This paper aims to determine the source of the difficulty that students often find when performing calculations in chemistry. Through the design and analysis of a set of chemistry questions and analogous mathematics questions, set in a Standard Grade context, it is revealed that a basic grasp of mathematics is missing
Recognising the importance of graduates being equipped with appropriate employability skills alongside their subject-specific skills, we have had transferable skills training embedded throughout our degree programmes for 30 years. More recently, a specific employability skills module for final-year honours students has been created. This module consists of a programme of activities supporting employability skills, which was delivered to final-year undergraduate students from 2012 to 2015. A key feature in the development and delivery of these activities was the involvement of external experts. Detailed questionnaires have captured student perceptions and thematic analysis has revealed key themes. The module has been perceived to be highly useful, resulting in significant increases in students’ confidence across key areas of employability skills. Furthermore, students may hold skewed perceptions of the relevance of generic employability skills to their chosen career path. This fact should be considered when delivering employability skills programmes
Animal African trypanosomiasis (AAT) is a significant socioeconomic burden for sub-Saharan Africa due to its huge impact on livestock health. Existing therapies including those based upon Minor Groove Binders (MGBs), such as the diamidines, which have been used for decades, have now lost efficacy in some places due to the emergence of resistant parasites. Consequently, the need for new
For many years, a key driver for Higher Education Institutions (HEIs) has been ensuring that students are prepared for employment post-graduation. This has often resulted in HEIs providing specific modules of study focussing on employability and soft skills. The existing research literature presents a variety of strategies for embedding employability within curricula, often focusing on frameworks to review the provision of employability opportunities within a degree programme. The authors have previously investigated an employability module within an Undergraduate Chemistry Programme at their UK HEI, particularly focusing on students' perceptions -these coalesced around the themes of personal progression, relevance of the module and interactions. However, before using these findings to further develop the module, it was deemed necessary to investigate the module in a different context. This study investigates the employability module in an Australian HEI and its delivery to undergraduate and postgraduate students from a range of different disciplines. Free text comments from questionnaires answered by 85 participants were subjected to thematic analysis in order to understand students' perceptions of the module in this new context. The new thematic map was compared to that from the original study to reveal several key similarities and differences between students' perceptions. However, the most important finding is thast employability modules should be tailored to a specific cohort to ensure they are aligned with their needs. This suggests that Central University employability module providers should work closely with individual departments to maximise the impact of these for students.
ARTICLE HISTORY
A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimisation towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biological activity.
This study details the synthesis and biological evaluation of a collection of 19 structurally related Minor Groove Binders (MGBs), derived from the natural product distamycin, which were designed to probe antifungal and antimycobacterial activity. From this initial set, we report several MGBs that are worth more detailed investigation and optimisation. MGB-4, MGB-317 and MGB-325 have promising MICs of 2, 4 and 0.25 μg/mL, respectively, against the fungus C. neoformans.MGB-353 and MGB-354 have MICs of 3.1 μM against the mycobacterium M. tuberculosis. The selectivity and activity of these compounds is related to their physicochemical properties and the cell wall/membrane characteristics of the infective agents.
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