Asgpr-binding compounds for the degradation of extracellular proteins
US-2024424108-A1 · Dec 26, 2024 · US
US8946145B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8946145-B2 |
| Application number | US-201013318272-A |
| Country | US |
| Kind code | B2 |
| Filing date | May 3, 2010 |
| Priority date | May 1, 2009 |
| Publication date | Feb 3, 2015 |
| Grant date | Feb 3, 2015 |
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Compounds comprising peptides capable of binding C3 protein and inhibiting complement activation are disclosed. These compounds display greatly improved complement activation-inhibitory activity as compared with currently available compounds. The compounds comprise compstatin analogs having a constrained backbone at position 8 (glycine) and, optionally, specific substitutions for threonine at position 13.
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What is claimed: 1. A modified compstatin peptide (ICVVQDWGHHRCT (cyclic C2-C12); SEQ ID NO:1), in which the Gly at position 8 is N-methylated to constrain the backbone conformation of the peptide at that location, and comprising one or more additional modifications selected from: a) acetylated N-terminus; b) Ala instead of His at position 9 of the peptide; c) Trp or an analog of Trp instead of Val at position 4 of the peptide; d) halogenated Trp at position 7 of the peptide…
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