Development of a Novel Affinity Labeling Method for Target Identification of Bioactive Small Molecules.
[Development of a Novel Affinity Labeling Method for Target Identification of Bioactive Small Molecules]. Yakugaku Zasshi. 2019;139(12):1513-1521 Authors: Yamaguchi T Abstract Target identification (target-ID) is an important step in elucidating the mechanisms of action of bioactive small molecules. In the past few decades, a number of target-ID methods have been developed. Among these, affinity labeling has been reliably used for specific modifications, as well as for the identification of weakly interacting protein targets, membrane-associated protein targets, and target-interacting proteins under native cellular conditions, which are generally difficult to achieve by conventional pull-down methods. In general, affinity labeling utilizes chemical probes composed of a bioactive small molecule, a reactive group, and a detection unit. However, the design and synthesis of highly functionalized chemical probes is often time-consuming. To address this issue, we have recently developed some simple affinity labeling methods using small fluorogenic tags, such as 4-alkoxy-7-nitro-2,1,3-benzoxadiazole (O-NBD), 2,3-dichloromaleimide (diCMI), and 4-azidophthalimide (AzPI), and successfully achieved the specific fluorescent labeling of target proteins, even in living cells. These methods should be useful for target-ID in phenotypic drug discovery. PMID: 31787638 [PubMed - in process]
Authors: Zhylkaidarova A, Kaidarova D, Batyrbekov K, Shatkovskaya O, Begimbetova D Abstract We carried out an analysis of the total incidence of colon cancer throughout Kazakhstan. Retrospectively, according to the regional reports on endoscopic screening, the study showed an increase in the age-related incidence of colorectal cancer (CRC) cases from 2004-2008 to 2009-2014. The peak of morbidity in both periods was noted in the age category of>70 years. The indicators of the territorial distribution of CRC incidence make it possible to divide the regions into areas with low or high rates of CRC. Specific indicat...
Conclusions: The transduodenal approach for obtaining samples from solid lesions using a 19-G flexible needle seems feasible and accurate. PMID: 32447874 [PubMed - as supplied by publisher]