Compstatin analogues and their medical uses
AssigneeZp Spv 3 K/S
InventorsAnne Pernille Tofteng Shelton, Jacob Ulrik Fog, Jens Kvist Madsen
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AssigneeZp Spv 3 K/S
InventorsAnne Pernille Tofteng Shelton, Jacob Ulrik Fog, Jens Kvist Madsen
Estimating the term…
Compstatin analogues having improved binding and complement-inhibiting activity as compared to the 13 amino acid compstatin peptide (ICVVQDWGHHRCT (cyclic C2-C12)) (SEQ ID NO: 1) are described, in particular compstatin analogues that additionally possess useful physicochemical properties, such as increased solubility. These analogues include variants with an isoleucine residue at position 3 in place of the wild type valine residue, which provides compstatin peptides with improved binding and complement-inhibiting activity and also enables the introduction of other modifications, for example modifications that are capable of increasing solubility, such as the introduction of charged or polar amino acids at position 9 and/or the introduction of N- and/or C-terminal sequences.
A method of inhibiting complement activation for treating a subject in need thereof, the method comprising administering to the subject a compstatin analogue of Formula I:
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