Bicyclic peptide ligands specific for EphA2
AssigneeBicycleTx Limited
InventorsPunit Upadhyaya, Johanna Lahdenranta, Gemma Elizabeth Mudd, Kevin McDonnell
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Abstract
The present invention relates to polypeptides which are covalently bound to non-aromatic molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of the Eph receptor tyrosine kinase A2 (EphA2). The invention also relates to pharmaceutical compositions comprising said peptide ligands and to the use of said peptide ligands in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).
Claims10
An EphA2 binding bicyclic peptide ligand comprising:
- (a) a peptide comprising the amino acid sequence A [HArg]DC[HyP]LVNPLCLEP[d1Nal]WTC (SEQ ID NO:
- 35), wherein [HArg] is homoarginine, [HyP] is hydroxyproline, and [d1Nal] is d-1-naphthylalanine;
- and
- (b) a 1,1′,1″-(1,3,5-triazinane-1,3,5-triyl) triprop-2-en-1-one (TATA) molecular scaffold covalently bonded to the peptide via each of the three cysteines of the amino acid sequence, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.