INSULIN RECEPTOR PARTIAL AGONISTS

To provide insulin dimers that act as partial agonists at the insulin receptor.SOLUTION: The invention provides a compound having the formula in the figure, where the disulfide linkages between the Cys6 and Cys11 residues of the A-chain polypeptide and the disulfide linkages between the Cys7 and Cys...

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Hauptverfasser:	DMITRI PISSARNITSKI, SHI ZHI-CAI, ZHU YUPING, MU YINGJUN, RAVI NARGUND, AHMET KEKEC, HUO PEI, FENG DANQING, CHRISTINA B MADSEN-DUGGAN, YAN LIN, WU ZHICAI, LIN SONGNIAN
Format:	Patent
Sprache:	eng ; jpn
Schlagworte:	CHEMISTRY HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	To provide insulin dimers that act as partial agonists at the insulin receptor.SOLUTION: The invention provides a compound having the formula in the figure, where the disulfide linkages between the Cys6 and Cys11 residues of the A-chain polypeptide and the disulfide linkages between the Cys7 and Cys20 of the A-chain and the Cys7 and Cys19 of the B-chain polypeptide, respectively, are represented by the solid lines therebetween; and where the linking moieties are covalently linked to the ε-amino acid of the shown lysine residue.SELECTED DRAWING: Figure 1 【課題】インスリン受容体において部分アゴニストとして作用するインスリン二量体の提供。【解決手段】を有する化合物であって、Ａ鎖ポリペプチドのＣｙｓ６残基とＣｙｓ１１残基との間のジスルフィド結合ならびにＡ鎖のＣｙｓ７およびＣｙｓ２０とＢ鎖ポリペプチドのＣｙｓ７およびＣｙｓ１９との間のジスルフィド結合は、それぞれ、その間の実線によって表され；連結部分は示されるリジン残基のεアミノ酸と共有結合している、化合物。【選択図】図１