Synthesis of Homopolymers and Copolymers Containing an Active Ester of Acrylic Acid by RAFT: Scaffolds for Controlling Polyvalent Ligand Display.
Synthesis of Homopolymers and Copolymers Containing an Active Ester of Acrylic Acid by RAFT: Scaffolds for Controlling Polyvalent Ligand Display.
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通过 RAFT 合成含有丙烯酸活性酯的均聚物和共聚物:用于控制多价配体显示的支架。
DOI:
10.1002/pola.23031
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发表时间:
2008
期刊:
影响因子:
--
通讯作者:
Kane,RaviS
中科院分区:
文献类型:
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作者:
Gujraty,KunalV;Yanjarappa,MallinamaduguJ;Saraph,Arundhati;Joshi,Amit;Mogridge,Jeremy;Kane,RaviS
We describe the synthesis of activated homopolymers and copolymers of controlled molecular weight based on the controlled radical polymerization ofN‐acryloyloxysuccinimide (NAS) by reversible addition fragmentation chain transfer (RAFT). We synthesized activated homopolymers in a range of molecular weights with polydispersities between 1 and 1.2. The attachment of an inhibitory peptide to the activated polymer backbone yielded a potent controlled molecular weight polyvalent inhibitor of anthrax toxin. To provide greater control over the placement of the peptides along the polymer backbone, we also used a semibatch copolymerization method to synthesize copolymers of NAS and acrylamide (AAm). This approach enabled the synthesis of copolymers with control over the placement of peptide‐reactive NAS monomers along an inert backbone; subsequent functionalization of NAS with peptide yielded well‐defined polyvalent anthrax toxin inhibitors that differed in their potencies. These strategies for controlling molecular weight, ligand density, and ligand placement will be broadly applicable for designing potent polyvalent inhibitors for a variety of pathogens and toxins and for elucidating structure–activity relationships in these systems. © 2008 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 46: 7249–7257, 2008