Chimeric inhibitor molecules of complement activation
US-9815876-B2 · Nov 14, 2017 · US
US8933201B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-8933201-B2 |
| Application number | US-96916110-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 15, 2010 |
| Priority date | Jun 7, 2006 |
| Publication date | Jan 13, 2015 |
| Grant date | Jan 13, 2015 |
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The presently disclosed and claimed inventive concepts include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and α 2 -antiplasmin and abnormal cell proliferation. The presently disclosed and claimed inventive concepts also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed and claimed inventive concepts further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma α 2 -antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.
Opening claim text (preview).
What is claimed is: 1. A compound having the formula: B-Xaa 1 -Sp-Xaa 2 -Cyc (Formula I) wherein: B is at least one of acetyl, pyroglutamate, and succinyl; Xaa 1 is a positively-charged amino-acid; Sp is a spacer molecule having a length in the range of 0.3 nm to 2.5 nm; Xaa 2 is glycine, D-alanine, D-serine, or D-threonine; and Cyc is boronyl proline or cyanopyrrolidine; and wherein the compound binds to the active site of Antiplasmin Cleaving Enzyme (APCE) a…
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