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US-2024390271-A1 · Nov 28, 2024 · US
Specific active site inhibitors of enzymes and methods of producing same
US10214570B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10214570-B2 |
| Application number | US-201113814146-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jun 8, 2011 |
| Priority date | Aug 10, 2010 |
| Publication date | Feb 26, 2019 |
| Grant date | Feb 26, 2019 |
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- Title
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- Abstract
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Abstract
Official abstract text for this publication.
The present disclosure provides a method of producing enzyme-specific inhibitors or substrate binding partners comprising: identifying active site residues of the substrate in the enzyme substrate complex or in substrate binding partner-substrate complex; randomizing the active site residues to produce a combinatorial library of substrate variants; and selecting substrate variants that inhibit enzyme activity or bind substrate as substrate-specific binding partners. The present disclosure also provides ubiquitin enzyme specific inhibitors and ubiquitin variants that bind ubiquitin interaction motifs.
First claim
Opening claim text (preview).
The invention claimed is: 1. A specific inhibitor of a deubiquitinating enzyme, wherein the deubiquitinating enzyme is USP8, and wherein the inhibitor is ubiquitin variant comprising the amino acid sequence set forth in SEQ ID NO: 2 or 3. 2. The inhibitor of claim 1 , wherein the ubiquitin variant comprises the amino acid sequence set forth in SEQ ID NO: 2. 3. The inhibitor in claim 1 , wherein the ubiquitin variant comprises the amino acid sequence set forth in SEQ ID NO: 3. 4. A nucleic acid encoding the inhibitor of claim 1 . 5. The nucleic acid of claim 4 in a recombinant expression vector. 6. The nucleic acid of claim 5 in a host cell. 7. The nucleic acid of claim 4 , wherein the ubiquitin variant comprises the amino acid sequence set forth in SEQ ID NO: 2. 8. The nucleic acid of claim 4 , wherein the ubiquitin variant comprises the amino acid sequence set forth in SEQ ID NO: 3.
Assignees
Inventors
Classifications
- C07K14/47Primary
from mammals · CPC title
from animals; from humans {(enzyme inhibitors A61K38/005)} · CPC title
- C07K14/435Primary
from animals; from humans · CPC title
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- What does patent US10214570B2 cover?
- The present disclosure provides a method of producing enzyme-specific inhibitors or substrate binding partners comprising: identifying active site residues of the substrate in the enzyme substrate complex or in substrate binding partner-substrate complex; randomizing the active site residues to produce a combinatorial library of substrate variants; and selecting substrate variants that inhibit …
- Who is the assignee on this patent?
- Sidhu Sachdev, Beatty Linda, Ernst Andreas, and 1 more
- What technology area does this patent fall under?
- Primary CPC classification C07K14/47. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Feb 26 2019 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).