Compositions and methods for inducing conformational changes in cereblon and other E3 ubiquitin ligases
US-10668057-B2 · Jun 2, 2020 · US
Methods for measuring small molecule affinity to cereblon
US11644461B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-11644461-B2 |
| Application number | US-202017026105-A |
| Country | US |
| Kind code | B2 |
| Filing date | Sep 18, 2020 |
| Priority date | Feb 3, 2017 |
| Publication date | May 9, 2023 |
| Grant date | May 9, 2023 |
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- Title
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Abstract
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A complex comprises a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN, and uses thereof for identifying therapeutic compounds.
First claim
Opening claim text (preview).
What is claimed is: 1. A complex comprising (i) a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and (ii) a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN; wherein the Cy5-conjugated small molecule has a structure of Formula (I) and wherein the Cy5-conjugated small molecule binds in a hydrophobic tri-tryptophan pocket formed by Trp380, Trp386, and Trp400 on the CRBN. 2. The complex of claim 1 , further comprising a DNA damage-binding protein 1 (DDB1). 3. The complex of claim 2 , wherein the complex is prepared by mixing 6xHis-CRBN-DDB1 complex with europium-anti-his antibody and the Cy5-conjugated small molecule of Formula (I). 4. The complex of claim 3 , wherein the complex is prepared by mixing 60 nM 6xHis-CRBN-DDB1, 3 nM europium-anti-his antibody, and 30 nM Cy5-conjugated small molecule of Formula (I). 5. A composition comprising the complex of claim 1 . 6. A composition comprising the complex of claim 2 .
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Classifications
Regulators; Modulating activity · CPC title
- G01N33/542Primary
with steric inhibition or signal modification, e.g. fluorescent quenching · CPC title
from mammals · CPC title
Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A) · CPC title
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Frequently asked questions
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- What does patent US11644461B2 cover?
- A complex comprises a CRBN having a europium-anti-his antibody on the N-terminus of the CRBN, and a Cy5-conjugated small molecule, wherein the Cy5-conjugated small molecule binds the CRBN, and uses thereof for identifying therapeutic compounds.
- Who is the assignee on this patent?
- Celgene Corp
- What technology area does this patent fall under?
- Primary CPC classification G01N33/542. Mapped technology areas include Physics.
- When was this patent published?
- Publication date Tue May 09 2023 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 12 related publications on this page (citations in our corpus or others sharing the same primary CPC).