Patent ID: 11939403
Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Field: Biotechnology (Chemistry)
Classification: CPC C | IPC C

Claim 20:
21. A method of designing and preparing a permeable cyclic decapeptide-peptoid ligand,
wherein the permeable cyclic decapeptide-peptoid ligand is of a class of ligands of a structure, wherein Za1 is X1 or methyl (CH3—),
wherein Za2 is X2 or methyl (CH3—),
wherein Za4 is H or 2-methylpropyl, wherein Za5 is H or 2-methylpropyl, wherein Zb1 is X1 or methyl (CH3—),
wherein Zb2 is X2 or methyl (CH3—),
wherein Zb4 is H or methyl (CH3—),
wherein Zb5 is H or methyl (CH3—),
wherein Zc1 is 2-methylpropyl, , or methyl (CH3—),
wherein Zc2 is 2-methylpropyl, , or methyl (CH3—),
wherein X1 is selected from the group consisting of ethyl (Et-), , 2-propoxy-3-propyl, , and (1,3-benzodioxol-5-yl)-methyl, wherein X2 is selected from the group consisting of pentyl, , cyclohexylmethyl, , and (oxan-4-yl)methyl, , and
wherein X3 is selected from the group consisting of methyl, , and benzyl, comprising determining whether a dissociation constant of the ligands of the class and a therapeutic target at physiological conditions is minimized by the ligands being rigid or flexible,
when the dissociation constant is minimized by the ligands of the class being rigid, selecting Za4 as H, Zb1 as CH3, Za5 as H, and Zb2 as CH3 to obtain a rigid permeable cyclic decapeptide-peptoid ligand,
when the dissociation constant is minimized by the ligands of the class being flexible, selecting Za4 as 2-methylpropyl, Zb1 as X1, Za5 as 2-methylpropyl, and Zb2 as X2 to obtain a flexible permeable cyclic decapeptide-peptoid ligand, and
synthesizing the permeable cyclic decapeptide-peptoid ligand.