PDE8, a type of phosphodiesterase (PDE), is proven to be crucial in various cellular activities and physiological activities by influencing second messenger systems. It is involved in a wide range of diseases, including Alzheimer’s disease and various heart diseases. However, there is limited information about PDE8 selective inhibitors. This work aimed to improve the solubility and yield of PDE8 in the supernatant by exploring suitable culture conditions, including temperatures and different additives.

Polo-like kinase 1 (Plk1) is a master regulator of mitosis, initiating key steps of cell cycle regulation, and its overexpression is associated with certain types of cancer. In this study, the authors carefully designed peptides that were able to bind to Plk1 at a location that is important for its proper localization and function. Future studies could further develop these peptides to selectively target Plk1 in cancer cells and induce mitotic arrest.

Irrespective of the final application of a molecule, synthetic accessibility is the rate-determining step in discovering and developing novel entities. However, synthetic complexity is challenging to quantify as a single metric, since it is a composite of several measurable metrics, some of which include cost, safety, and availability. Moreover, defining a single synthetic accessibility metric for both natural products and non-natural products poses yet another challenge given the structural distinctions between these two classes of compounds. Here, we propose a model for synthetic accessibility of all chemical compounds, inspired by the Central Limit Theorem, and devise a novel synthetic accessibility metric assessing the overall feasibility of making chemical compounds that has been fitted to a Gaussian distribution.

Naturally occurring neuroactive alkaloids are often studied for their potential to treat Neurological diseases. This team of students study Rivastigmine, a potent cholinesterase inhibitor that is a synthetic analog of physostigmine, which comes from the Calabar bean plant Physostigma venenosum. By comparing the effects of optimized synthetic analogs to the naturally occurring alkaloid, they determine the most favorable analog for inhibition of acetylcholinesterase (AChE), the enzyme that breaks down the neurotransmitter acetylcholine (ACh) to terminate neuronal transmission and signaling between synapses.

Wang and Gong developed a novel dynamic gene-searching algorithm called Dynamic Gene Search (DyGS) to create a gene panel for each of the 12 cancers with the highest annual incidence and death rate. The 12 gene panels the DyGS algorithm selected used only 3.5% of the original gene mutation pool, while covering every patient sample. About 40% of each gene panel is druggable, which indicates that the DyGS-generated gene panels can be used for early cancer detection as well as therapeutic targets in treatment methods.

In organic synthesis, protecting groups are derivatives of reactive functionalities that play a key role in ensuring chemoselectivity of chemical transformations. To protect alcohols and amines, acid-labile tert-butyloxycarbonyl protecting groups are often employed but are avoided when the substrate is acid-sensitive. Thus, orthogonal base-labile protecting groups have been in demand to enable selective deprotection and to preserve the reactivity of acid-sensitive substrates. To meet this demand, we present 4-nitrophenyl carbonates and carbamates as orthogonal base-labile protecting group strategies.

In​ the​ field​ of​ medicine,​ natural​ treatments​ are​ becoming ​increasingly ​vital ​towards ​the ​cure ​of ​cancer. Zhu et al. wanted to investigate the effects of lettuce extract on cancer cell survival and proliferation. They used an adenocarcinoma cell line, COLO320DM, to determine whether crude extract from a lettuce species called Niuli​ Lactucis Agrestibus​ would affect cancer cell survival, migration, and proliferation. They found that Niuli extract inhibited cancer cell survival, increased expression of cell cycle inhibitors p21 and p27, and inhibited migration. However, Niuli extract did not have these effects on healthy cells. This work reveals important findings about a potential new source of anti-colorectal cancer compounds.

Staphylococcus aureus is a major pathogen in both hospitals and the community and can cause systemic infections such as pneumonia. Multi-drug resistant strains, such as Methicillin-resistant S. aureus (MRSA) are particularly worrisome. In order to reduce the development of bacterial resistance, we hypothesized that two selected traditional Chinese medicines, Shuang-Huang-Lian (SHL) and Lan-Qin, would be effective against S. aureus. The results showed that SHL had a synergistic effect with gentamicin as well as additive effects with penicillin and cefazolin against S. aureus compared with using antibiotics alone.

Here the authors investigate the contributions of man-made surfaces in Laramie, Wyoming to the Urban Heat Island (UHI) effect. Heat absorption and release by five surfaces were measured in the autumn of 2018. By recording temperatures of man-made and natural surfaces at early morning, mid-afternoon, and evening using an infrared thermometer, the authors determined that man-made surfaces retained more heat in fall than natural surfaces.

Rhizopus stolonifer is a mold commonly found growing on bread that can cause many negative health effects when consumed. Preservatives are the well-known answer to this problem; however, many preservatives are not naturally found in food, and some have negative health effects of their own. We focused on honey as a possible solution because of its natural origin and self-preservation ability. We hypothesized that honey would decrease the growth rate of R. stolonifer . We evaluated the honey with a zone of inhibition (ZOI) test on agar plates. Sabouraud dextrose agar was mixed with differing volumes of honey to generate concentrations between 10.0% and 30.0%. These plates were then inoculated with a solution of spores collected from the mold. The ZOI was measured to determine antifungal effectiveness. A statistically significant difference was found between the means of all concentrations except for 20.0% and 22.5%. Our findings support the hypothesis as we showed a positive correlation between the honey concentration and growth rate of mold. By using this data, progress could be made on an all-natural, honey-based preservative.