General Linker Diversification Approach to Bivalent Ligand Assembly: Generation of an Array of Ligands for the Cation-Independent Mannose 6-Phosphate Receptor.

General Linker Diversification Approach to Bivalent Ligand Assembly: Generation of an Array of Ligands for the Cation-Independent Mannose 6-Phosphate Receptor.
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DOI:
10.1021/acs.orglett.7b01914
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发表时间:
2017-08-18
期刊:
影响因子:
5.2
通讯作者:
Berkowitz DB
Berkowitz DB
中科院分区:
化学1区
文献类型:
--
作者:
Fei X;Zavorka ME;Malik G;Connelly CM;MacDonald RG;Berkowitz DB

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A generalized strategy is presented for the rapid assembly of a set of bivalent ligands with a variety of linking functionalities from a common monomer. Herein, an array of phosphatase-inert mannose-6-phosphonate-presenting ligands for the cation-independent-mannose 6-phosphate receptor (CI-MPR) is constructed. Receptor binding affinity varies with linking functionality—the simple amide and 1,5-triazole(tetrazole) being preferred over the 1,4-triazole. This approach is expected to find application across chemical biology, particularly in glycoscience, wherein multivalency often governs molecular recognition.
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