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US 2020/0046840 A1Published application
Peptide for cytosolic delivery
AssigneeKyoto University
InventorsShiroh FUTAKI, Kentarou SAKAMOTO, Misao AKISHIBA
Life of this patent
Estimating the term…
Abstract
Provided is a peptide represented by the following formula (I): R1-IWLTALX5FLGX6X1AAX7X2X3AX8QX4LSX9L-R2 (I) wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, R1, and R2 are as defined in the specification.
Claims15
A peptide represented by the following formula (I):
- R1-IWLTALX5FLGX6X1AAX7X2X3AX8QX4LSX9L-R2 (I)
- wherein X1 and X2 are the same or different, and each represents H or A;
- X3 represents E, L-2-aminoadipic acid (Aad), 2-aminopimelic acid, or 2-aminosuberic acid;
- X4 represents Q, L-2-aminoadipic acid (Aad), 2-aminopimelic acid, 2-aminosuberic acid, or E;
- X5 to X9 are the same or different, and each represents Lys (K), Arg (R), homoarginine, ornithine, homolysine, or 2-amino-7-guanidinoheptanoic acid;
- provided that a case where X1=H, X2=H, X3=E, X4=Q, and X5 to X9=K is excluded, and
- when X4=E, and X5 to X9=K, one or both of X1 and X2 are A;
- R1 represents a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aralkyloxycarbonyl group, an aryloxycarbonyl group, an alkoxy group, an aralkyloxy group, an aryloxy group, or a target substance;
- and
- R2 represents a hydroxyl group (OH), an amino group (NH2), a monoalkylamino group, a monoarylamino group, monocycloalkylamino, a dialkylamino group, an alkoxy group, an aralkyloxy group, an aryloxy group, or a target substance.
7 more elements
A peptide represented by the following formula (IA):
- R1-(IWLTALX5FLGX6X1AAX7X2X3AX8QX4LSX9L-Y)n-R2 (IA)
- wherein X1 and X2 are the same or different, and each represents H or A;
- X3 represents E, L-2-aminoadipic acid (Aad), 2-aminopimelic acid, or 2-aminosuberic acid;
- X4 represents Q, L-2-aminoadipic acid (Aad), 2-aminopimelic acid, 2-aminosuberic acid, or E;
- X5 to X9 are the same or different, and each represents Lys (K), Arg (R), homoarginine, ornithine, homolysine, or 2-amino-7-guanidinoheptanoic acid;
- provided that a case where X1=H, X2=H, X3=E, X4=Q, and X5 to X9=K is excluded, and
- when X4=E, and X5 to X9=K, one or both of X1 and X2 are A;
- R1 represents a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aralkyloxycarbonyl group, an aryloxycarbonyl group, an alkoxy group, an aralkyloxy group, an aryloxy group, or a target substance;
- R2 represents a hydroxyl group (OH), an amino group (NH2), a monoalkylamino group, a monoarylamino group, monocycloalkylamino, a dialkylamino group, an alkoxy group, an aralkyloxy group, an aryloxy group, or a target substance;
- Y represents a single bond or a spacer;
- and
- n is 2, 3, 4, 5, 6, 7, 8, 9 or 10.
9 more elements
A dendrimer represented by the following formula (IB):
- Z—(Ra)m (IB)
- wherein Z represents a branched multivalent linker;
- Ra is the same or different, and each represents R1-IWLTALX5FLGX6X1AAX7X2X3AX8QX4LSX9L-Y- or Y-IWLTALX5FLGX6X1AAX7X2X3AX*QX4LSX9L-R2;
- wherein X1 and X2 are the same or different, and each represents H or A;
- X3 represents E, L-2-aminoadipic acid (Aad), 2-aminopimelic acid, or 2-aminosuberic acid;
- X4 represents Q, L-2-aminoadipic acid (Aad), 2-aminopimelic acid, 2-aminosuberic acid, or E;
- X5 to X9 are the same or different, and each represents Lys (K), Arg (R), homoarginine, ornithine, homolysine, or 2-amino-7-guanidinoheptanoic acid;
- provided that a case where X1=H, X2=H, X3=E, X4=Q, and X5 to X9=K is excluded, and
- when X4=E, and X5 to X9=K, one or both of X1 and X2 are A;
- R1 represents a hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aralkyloxycarbonyl group, an aryloxycarbonyl group, an alkoxy group, an aralkyloxy group, an aryloxy group, or a target substance;
- R2 represents a hydroxyl group (OH), an amino group (NH2), a monoalkylamino group, a monoarylamino group, monocycloalkylamino, a dialkylamino group, an alkoxy group, an aralkyloxy group, an aryloxy group, or a target substance;
- Y represents a single bond or a spacer;
- and
- m is an integer of 2 to 8.
11 more elements
Dependencies are inferred from the claim text.