- Synthesis method of NH2-PEG5-NHBoc
-
The invention provides a synthesis method of NH2-PEG5-NHBoc. The NH2-PEG5-NHBoc represents [2-(2-{2-[2-(2-amino-ethyoxyl)ethyoxyl]ethyoxyl}ethyoxyl)ethyl]carbamic acid tert-butyl ester. The synthesis method comprises the following steps: step S1, by taking 2-(2-(triphenylmethyl)ethyoxyl)-1-ol and (2-(2-(2-(benzyloxy)ethyoxyl)ethyoxyl)-ethyl-4-p-toluenesulfonate as initial raw materials, carrying out substitution reaction to generate a first intermediate product; S2, carrying out catalytic hydrogenation on the first intermediate product and hydrogen, and then carrying out nucleophilic substitution reaction with Boc anhydride to generate a second intermediate product; S3, carrying out nucleophilic substitution reaction on the second intermediate product and paratoluensulfonyl chloride to generate a third intermediate product; S4, carrying out nucleophilic substitution reaction on the third intermediate product and sodium azide to generate a fourth intermediate product; and S5, carrying out a reduction reaction on the fourth intermediate product and hydrogen, so as to generate the NH2-PEG5-NHBoc. The synthesis method is low in cost and high in yield.
- -
-
Paragraph 0058; 0070-0072; 0073; 0085-0087; 0088; 0100-0102
(2021/10/11)
-
- Synthetic self-localizing ligands that control the spatial location of proteins in living cells
-
Small-molecule ligands that control the spatial location of proteins in living cells would be valuable tools for regulating biological systems. However, the creation of such molecules remains almost unexplored because of the lack of a design methodology. Here we introduce a conceptually new type of synthetic ligands, self-localizing ligands (SLLs), which spontaneously localize to specific subcellular regions in mammalian cells. We show that SLLs bind their target proteins and relocate (tether) them rapidly from the cytoplasm to their targeting sites, thus serving as synthetic protein translocators. SLL-induced protein translocation enables us to manipulate diverse synthetic/endogenous signaling pathways. The method is also applicable to reversible protein translocation and allows control of multiple proteins at different times and locations in the same cell. These results demonstrate the usefulness of SLLs in the spatial (and temporal) control of intracellular protein distribution and biological processes, opening a new direction in the design of small-molecule tools or drugs for cell regulation.
- Ishida, Manabu,Watanabe, Hideaki,Takigawa, Kazumasa,Kurishita, Yasutaka,Oki, Choji,Nakamura, Akinobu,Hamachi, Itaru,Tsukiji, Shinya
-
supporting information
p. 12684 - 12689
(2013/09/23)
-