- Synthetic aptamer-polymer hybrid constructs for programmed drug delivery into specific target cells
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Viruses have evolved specialized mechanisms to efficiently transport nucleic acids and other biomolecules into specific host cells. They achieve this by performing a coordinated series of complex functions, resulting in delivery that is far more efficient than existing synthetic delivery mechanisms. Inspired by these natural systems, we describe a process for synthesizing chemically defined molecular constructs that likewise achieve targeted delivery through a series of coordinated functions. We employ an efficient "click chemistry" technique to synthesize aptamer-polymer hybrids (APHs), coupling cell-targeting aptamers to block copolymers that secure a therapeutic payload in an inactive state. Upon recognizing the targeted cell-surface marker, the APH enters the host cell via endocytosis, at which point the payload is triggered to be released into the cytoplasm. After visualizing this process with coumarin dye, we demonstrate targeted killing of tumor cells with doxorubicin. Importantly, this process can be generalized to yield APHs that specifically target different surface markers.
- Oh, Seung Soo,Lee, Bongjae F.,Leibfarth, Frank A.,Eisenstein, Michael,Robb, Maxwell J.,Lynd, Nathaniel A.,Hawker, Craig J.,Soh, H. Tom
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- Epoxy-terminated vinyl ether monomer as well as preparation method and application thereof
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The invention relates to an epoxy-terminated vinyl ether monomer as well as a preparation method thereof. The preparation method comprises the following steps: 1, hydroxyl-terminated vinyl ether withthe molecular structural formula shown in the specification and epoxy-terminated chloroalkane with the molecular structural formula shown in the specification are taken as raw materials for standby application, R1 is H or-(CH2) n-, n is 1-5, R2 is straight chain-(CH2) n- (n is 2-7) or alkyl with a branched chain, R3 is-(CH2) n-, and n is 1-4; and 2) in a closed environment, the raw materials in the step 1), strong base, an initiator and a phase transfer catalyst are added for reacting to obtain the target product. The ether monomer provided by the invention has an epoxy-terminated and vinyl-terminated structure; the monomer is high in activity, unsaturated groups can be copolymerized easily, -SiH/-SH/-OH can be subjected to an addition reaction easily, the epoxy-terminated end-capping modification process becomes simple, a material modified with the monomer has an epoxy-terminated group and can be easily subjected to block grafting and graft grafting with epoxy resin, and possibility is provided for further modification of follow-up materials.
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Paragraph 0032-0033
(2020/11/12)
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- DETERMINATION OF OPTIMUM CONDITIONS FOR SYNTHESIS OF GLYCIDYL VINYLOXYETHYL ETHER BY MATHEMATICAL EXPERIMENTAL DESIGN
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Synthesis of glycidyl vinyloxyethyl ether by reaction of ethylene glycol monovinyl ether with epichlorohydrin in the presence of sodium hydroxide has been investigated by mathematical experimental design.
- Belozerov, L. E.,Stankevich, V. K.,Ezhova, L. N.,Balakhchi, G. K.,Trofimov, B. A.
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p. 1231 - 1232
(2007/10/02)
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