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filingDate 2016-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2018-05-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2018513843-A
titleOfInvention Insulin analogues containing glucose-controlled conformational switches
abstract SOLUTION: A two-chain insulin analogue has (i) an A chain modified with a monomeric glucose binding element at or near its N-terminus, and (ii) this bond can be replaced by glucose. It includes a B chain modified at or near its C-terminus by an element reversibly linked to a monomeric glucose binding element. The monomeric glucose binding element may be a (selectively halogenated) phenylboronic acid derivative. The B chain may be modified with a diol-containing element derived from a monosaccharide, disaccharide, or oligosaccharide, a non-saccharide diol-containing structure, or an α-hydroxycarboxylic acid-containing structure. The analog can be prepared by trypsin-mediated semi-synthesis. The formulation is dissolved in a soluble solution at pH 7.0-8.0 in the presence or absence of zinc ions at a molar ratio of 0.0-3.0 per insulin analog monomer, U-10-U The strength can be -1000. A diabetic patient can be administered a physiologically effective amount of the insulin analog subcutaneously, intraperitoneally, or orally. [Selection] Figure 3A
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID130383
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID134603
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID2734537
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419490211
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP01331
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID426090082
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ7UHE2
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419532391
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http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID397853
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID411161974
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCAAW83741
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419594851
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP22629
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID289
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCA9M2P1
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ3SFE8
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCQ1IZL1
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http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCB5Y1P2
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Total number of triples: 462.