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US 2022/0024975 A1Published application
Alpha-v beta-6 integrin ligands and uses thereof
AssigneeArrowhead Pharmaceuticals, Inc.
InventorsAaron Almeida, Zhen Li, Erik W. Bush, Tao Pei, Agnieszka Glebocka, Anthony Nicholas, Jeffrey Carlson, Matthew Fowler-Watters
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Abstract
Integrin ligands having serum stability and affinity for αvβ6 integrins are described. Compositions comprising αvβ6 integrin ligands having serum stability and having affinity for αvβ6 integrins and methods of using them are also described.
Claims47
An αvβ6 integrin ligand comprising:
- (SEQ ID NO:
- 85)
- Z-RG1DLXaa1Xaa2L
- (Formula I);
- or
- (SEQ ID NO:
- 86)
- Z-RG1DLXaa1Xaa2L-J-R1
- (Formula II);
- or
- (SEQ ID NO:
- 87)
- Z-RG1DLXaa1Xaa2L-J-R1-R2
- (Formula III);
- or
- (SEQ ID NO:
- 88)
- (Z-RG1DLXaa1Xaa2L-J-R1)n-R3
- (Formula IV);
- or
- (SEQ ID NO:
- 89)
- (Z-RG1DLXaa1Xaa2L-J-R1)n-R4-(R3)p
- (Formula V);
- or
- (SEQ ID NO:
- 92)
- Z-RG1DLXaa1Xaa2L-Xaa3Xaa4L-R1
- (Formula VI);
- or
- (SEQ ID NO:
- 105)
- (Z-RG1DLXaa1Xaa2L-J-R1)n-R4-(R2)p
- (Formula VII);
- wherein
- Z is an amine-terminal cap;
- R is L-arginine;
- G1 is L-glycine or N-methyl glycine;
- D is L-aspartic acid (L-aspartate);
- L is L-leucine;
- Xaa1 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- Xaa2 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- Xaa3 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- Xaa4 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- R1 is optional and, if present, includes PEG and/or a linking group;
- J is optional and, if present, includes one or more L-α amino acids, L-β amino acids α,α-disubstituted amino acids, or a combination thereof;
- R2 comprises a reactive group or a protected reactive group;
- R3 comprises a cargo molecule;
- n is an integer greater than 0;
- p is an integer greater than 0;
- and
- R4 is optional and, if present, comprises a scaffold and/or linking group that includes at least one attachment point for each ligand present and at least one attachment point for each cargo molecule present.
49 more elements
An αvβ6 integrin ligand comprising:
- (SEQ ID NO:
- 96)
- RG1DLXaa1Xaa2L-Xaa3Xaa4L-R1
- (Formula VIII)
- wherein
- R is L-arginine;
- G1 is L-glycine or N-methyl glycine;
- D is L-aspartic acid (L-aspartate);
- L is L-leucine;
- Xaa1 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- Xaa2 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- Xaa3 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- Xaa4 is an L-α amino acid, an L-β amino acid, or an α,α-disubstituted amino acid;
- R1 is optional and, if present, includes PEG and/or a linking group;
- and at least one of Xaa1, Xaa2, Xaa3, and Xaa4 is a non-standard amino acid.
12 more elements
Dependencies are inferred from the claim text.