54798-92-4Relevant articles and documents
Photosensitive compound, preparation method and application thereof, and photosensitive protein immobilized gel containing photosensitive compound
-
, (2021/02/24)
The invention discloses a photosensitive compound, a preparation method and application thereof, and photosensitive protein immobilized gel containing the photosensitive compound, wherein the structural formula of the photosensitive compound is shown as a formula (I), and R is an electron withdrawing group. The preparation method of the photosensitive compound comprises the following steps: dissolving N-(3-aminopropyl) methacrylate hydrochloride in an organic solvent, adding an electron withdrawing group-containing tetrazole compound and triethylamine into the organic solvent, carrying out a stirring reflux reaction for 10-20 h, and carrying out purification treatment to obtain the photosensitive compound. According to the invention, the photosensitive compound takes a tetrazole ring as aphotosensitive group, and the photosensitive protein immobilized gel comprises the compound as a photosensitive component; and a protein separation function and a protein immobilization function are integrated, protein can be immobilized in situ and stably in the gel, the gel is more powerful and efficient, and protein loss caused by elution is not likely to happen.
Genetically Encoded 2-Aryl-5-carboxytetrazoles for Site-Selective Protein Photo-Cross-Linking
Tian, Yulin,Jacinto, Marco Paolo,Zeng, Yu,Yu, Zhipeng,Qu, Jun,Liu, Wenshe R.,Lin, Qing
supporting information, p. 6078 - 6081 (2017/05/09)
The genetically encoded photo-cross-linkers promise to offer a temporally controlled tool to map transient and dynamic protein-protein interaction complexes in living cells. Here we report the synthesis of a panel of 2-aryl-5-carboxytetrazole-lysine analogs (ACTKs) and their site-specific incorporation into proteins via amber codon suppression in Escherichia coli and mammalian cells. Among five ACTKs investigated, N-methylpyrroletetrazole-lysine (mPyTK) was found to give robust and site-selective photo-cross-linking reactivity in E. coli when placed at an appropriate site at the protein interaction interface. A comparison study indicated that mPyTK exhibits higher photo-cross-linking efficiency than a diazirine-based photo-cross-linker, AbK, when placed at the same location of the interaction interface in vitro. When mPyTK was introduced into the adapter protein Grb2, it enabled the photocapture of EGFR in a stimulus-dependent manner. The design of mPyTK along with the identification of its cognate aminoacyl-tRNA synthetase makes it possible to map transient protein-protein interactions and their interfaces in living cells.
Synthesis and structure-activity relationships of antitubercular 2-nitroimidazooxazines bearing heterocyclic side chains
Sutherland, Hamish S.,Blaser, Adrian,Kmentova, Iveta,Franzblau, Scott G.,Wan, Baojie,Wang, Yuehong,Ma, Zhenkun,Palmer, Brian D.,Denny, William A.,Thompson, Andrew M.
experimental part, p. 855 - 866 (2010/06/15)
Recently described biphenyl analogues of the antituberculosis drug PA-824 displayed improved potencies against M. tuberculosis but were poorly soluble. Heterobiaryl analogues of these, in which the first phenyl ring was replaced with various 5-membered ring heterocycles, were prepared with the aim of identifying potent new candidates with improved aqueous solubility. The compounds were constructed by coupling the chiral 2-nitroimidazooxazine alcohol with various halomethyl-substituted arylheterocycles, by cycloadditions to a propargyl ether derivative of this alcohol, or by Suzuki couplings on haloheterocyclic methyl ether derivatives. The arylheterocyclic compounds were all more hydrophilic than their corresponding biphenyl analogues, and several showed solubility improvements. 1-Methylpyrazole, 1,3-linked-pyrazole, 2,4-linked-triazole, and tetrazole analogues had 3- to 7-fold higher MIC potencies against replicating M. tb than predicted by their lipophilicities. Two pyrazole analogues were >10-fold more efficacious than the parent drug in a mouse model of acute M. tb infection, and one displayed a 2-fold higher solubility. 2009 American Chemical Society.