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filingDate 2019-11-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2022-02-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-2022511761-A
titleOfInvention Genetically encoded macrocyclic peptide library with pharmacophore
abstract The present invention relates to a method of forming a macrocyclic peptide having a pharmacophore and the produced macrocyclic peptide, wherein the method comprises a peptide containing two thiol groups in the cysteine side chain, a reactive compound 1,5-dichloro. Includes a step of reacting with Pentandion-2,4. The reaction of the reactive compound with the peptide produces a 1,3-diketone-containing macrocyclic polypeptide. The macrocyclic compound having a 1,3-diketone group is then modified by reaction of the macrocycle with an alkyl or arylhydrazine group having a pharmacophore under benign aqueous conditions. Macrocycles are displayed in libraries such as phage display libraries and can be used to biopan for affinity for selected targets.
priorityDate 2018-11-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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