Structure-Activity Relationship Explorations and Discovery of a Potent Antagonist for the Free Fatty Acid Receptor 2

Free fatty acid receptor 2 (FFA2) is a sensor for short-chain fatty acids that has been identified as an interesting potential drug target for treatment of metabolic and inflammatory diseases. Although several ligand series are known for the receptor, there is still a need for improved compounds. One of the most potent and frequently used antagonists is the amide-substituted phenylbutanoic acid known as CATPB ( 1 ). We here report the structure-activity relationship exploration of this compound, leading to the identification of homologues with increased potency. The preferred compound 37 (TUG-1958) was found, besides improved potency, to have high solubility and favorable pharmacokinetic properties.     

Do funded papers attract more usage?

Research funding has been seen as one of the most important resource in the reward system of science. And usage of publications denotes an interesting perspective of user behavior in scientific communication. This study aims to address the relationship between funding and Usage Count, which is a new metrics item established on the platform of Web of Science. Full records of 300,010 articles published in 2013 were downloaded in October 2015, and divided into six disciplines, including information science library science, education educational research, economics, computer science, materials science, and chemistry. Seven indicators were proposed to measure the impact, including Funding rate, Citation per paper, Usage rate, Usage per paper, Citation difference, Usage difference, and Conversion rate. It concluded funding has impact on usage and citation, and funded papers attract more usage, but varying in different disciplines. Usage Count can be used in the extension of citation metrics but with limits. This study originally engages with usage metrics and detected that there is positive correlation between usage and funding.     

Modelling of chromatic contrast for retrieval of wallpaper images

Colour remains one of the key factors in presenting an object and, consequently, has been widely applied in retrieval of images based on their visual contents. However, a colour appearance changes with the change of viewing surroundings, the phenomenon that has not been paid attention yet while performing colour‐based image retrieval. To comprehend this effect, in this article, a chromatic contrast model, CAMcc, is developed for the application of retrieval of colour intensive images, cementing the gap that most of existing colour models lack to fill by taking simultaneous colour contrast into account. Subsequently, the model is applied to the retrieval task on a collection of museum wallpapers of colour‐rich images. In comparison with current popular colour models including CIECAM02, HSI and RGB, with respect to both foreground and background colours, CAMcc appears to outperform the others with retrieved results being closer to query images. In addition, CAMcc focuses more on foreground colours, especially by maintaining the balance between both foreground and background colours, while the rest of existing models take on dominant colours that are perceived the most, usually background tones. Significantly, the contribution of the investigation lies in not only the improvement of the accuracy of colour‐based image retrieval but also the development of colour contrast model that warrants an important place in colour and computer vision theory, leading to deciphering the insight of this age‐old topic of chromatic contrast in colour science. © 2014 Wiley Periodicals, Inc. Col Res Appl, 40, 361–373, 2015