Kinase inhibitors that bind to the ATP cleft can be broadly classified into two groups: those that bind exclusively to the ATP site with the kinase assuming a conformation otherwise conducive to phosphotransfer (type I), and those that exploit a hydrophobic site immediately adjacent to the ATP pocket made accessible by a conformational rearrangement of the activation loop (type II). To date, all type II inhibitors were discovered by using structure-activity-guided optimization strategies. Here, we describe a general pharmacophore model of type II inhibition that enables a rational "hybrid-design" approach whereby a 3-trifluoromethylbenzamide functionality is appended to four distinct type I scaffolds in order to convert them into their corresponding type II counterparts. We demonstrate that the designed compounds function as type II inhibitors by using biochemical and cellular kinase assays and by cocrystallography with Abl.

Compared with other types of packaging, edible coatings are becoming more and more popular because of their more environmentally friendly properties and active ingredients carrying ability. The edible coating can reduce the influence of essential oils (EOs) on the flavor of the product and also can prolong the action time of EOs through the slow-release effect, which effectively promote the application of EOs in food. Understanding the different combinations of edible coatings and EOs as well as their antimicrobial effects on different microorganisms will be more powerful and targeted to promote the application of EOs in real food systems. The review focus on the contribution of the combination of EOs and edible coatings (EO-edible coatings) to prolong the shelf life of food products, (1) specifically addressing the main materials used in the preparation of EO-edible coatings and the application of EO-edible coatings in the product, (2) systematically summarizing the main production method of EO-edible coatings, (3) discussing the antiseptic activity of EO-edible coatings on different microorganisms in food.

We have developed a new type of surface-enhanced Raman scattering (SERS) substrate that consists of per-6-deoxy-(6-thio)-beta-cyclodextrin (CD-SH) modified by silver nanoparticles (AgNPs) for sensing of polycyclic aromatic hydrocarbons (PAHs), a kind of environmental pollutant, with very low affinity to metallic surfaces. The designed system can induce some PAH molecules (anthracene and pyrene) to insert into the hydrophobic cavity of beta-CD, which enables one to detect SERS of PAHs because the analytes are very close to the AgNPs surface, which is the zone of electromagnetic enhancement. The measured spectra can easily distinguish the two kinds of PAH compounds in a mixture by their own characteristic peaks. In addition, we carried out selective detection of PAHs by SERS of the inclusion complexes with different concentrations in the presence of CD-SH functionalized AgNPs. Moreover, this sensing platform has been applied to quantitative detection of PAH in a mixture consisting of anthracene and pyrene. The CD molecule has the feature of high selectivity due to its size of cavity, significantly enhancing the sensitivity of the system after CD-SH adsorbs on AgNPs via the terminal thiol. This proposed method for the detection of PAHs holds great potential in environmental analytical chemistry.

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