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AssigneeBicycleTx Limited
InventorsLiuhong CHEN, Philip HUXLEY, Silvia Pavan, Katerine Van Rietschoten
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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 includes drug conjugates comprising said peptides, conjugated to one or more effector and/or functional groups, to pharmaceutical compositions comprising said peptide ligands and drug conjugates and to the use of said peptide ligands and drug conjugates in preventing, suppressing or treating a disease or disorder characterised by overexpression of EphA2 in diseased tissue (such as a tumour).
1-21. (canceled)
A method for preventing, suppressing, or treating a disease or disorder characterized by overexpression of EphA2 in diseased tissue in a patient, the method comprising administering to the patient a peptide ligand specific for EphA2 comprising a polypeptide comprising three cysteine residues, separated by two loop sequences, and a non-aromatic molecular scaffold which forms covalent bonds with the cysteine residues of the polypeptide, such that two polypeptide loops are formed on the molecular scaffold, wherein the peptide ligand comprises the amino acid sequence:
Dependencies are inferred from the claim text.