41302-32-3Relevant articles and documents
Aminoglycoside hybrids as potent RNA antagonists
Tok, Jeffrey B.-H.,Cho, Junhyeong,Rando, Robert R.
, p. 5741 - 5758 (1999)
Aminoglycosides specifically bind to the A-site decoding region of prokaryotic 16S rRNA with dissociation constants in the 1-2 μM range. The aminoglycoside paromomycin binds to a truncated A-site construct with a K(d) = 1.85 μM. Paromomycin analogs are described here in which the aminoglycoside is linked via spacer groups to either thiazole orange or pyrene. These analogs bind specifically to the truncated A-site construct, but with affinities considerably higher than paromomycin itself. The binding of the hybrid molecules to the A-site is greater the shorter the spacer group.
PRODUCTION METHOD OF IODOALKANE DERIVATIVE USING MICROWAVE
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Paragraph 0074-0078, (2021/07/27)
PROBLEM TO BE SOLVED: To provide a production method of an iodoalkane derivative, with which the iodoalkane derivative can be produced even in a nonpolar solvent. SOLUTION: In a production method of a 5-iodovaleric acid ester, for example a 5-halogenovaleric acid ester represented by formula (1A) (in formula, R is a 1-6C alkyl group or a 7-11C aralkyl group and X is a chlorine atom or a bromine atom), is made to react with an alkali metal iodide salt by being brought into contact therewith in an organic solvent, in the presence of a tetrasubstituted ammonium salt, and further under microwave irradiation, in which 5-iodovaleric acid ester is represented by formula (3A), (in formula, R is synonymous with that in formula (1A)). SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
Modulation of BCR signaling by the induced dimerization of receptor-associated SYK
Westbroek, Mark L.,Geahlen, Robert L.
, (2017/12/26)
Clustering of the B cell antigen receptor (BCR) by polyvalent antigens is transmitted through the SYK tyrosine kinase to the activation of multiple intracellular pathways that determine the physiological consequences of receptor engagement. To explore factors that modulate the quantity and quality of signals sent by the crosslinked BCR, we developed a novel chemical mediator of dimerization to induce clustering of receptor-associated SYK. To accomplish this, we fused SYK with E. coli dihydrofolate reductase (eDHFR), which binds the small molecule trimethoprim (TMP) with high affinity and selectivity and synthesized a dimer of TMP with a flexible linker. The TMP dimer is able to induce the aggregation of eDHFR-linked SYK in live cells. The induced dimerization of SYK bound to the BCR differentially regulates the activation of downstream transcription factors, promoting the activation of Nuclear Factor of Activated T cells (NFAT) without affecting the activation of NFκB. The dimerization of SYK enhances the duration but not the amplitude of calcium mobilization by enhancing the extent and duration of its interaction with the crosslinked BCR at the plasma membrane.
Synthesis of Non-natural, Frame-Shifted Isoprenoid Diphosphate Analogues
Temple, Kayla J.,Wright, Elia N.,Fierke, Carol A.,Gibbs, Richard A.
supporting information, p. 6038 - 6041 (2016/12/09)
A set of synthetic approaches was developed and applied to the synthesis of eight frame-shifted isoprenoid diphosphate analogues. These analogues were designed to increase or decrease the methylene units between the double bonds and/or the pyrophosphate m
