IP Library › Granted Patent US 9,034,574
Granted Patent B2
US 9,034,574 · App. 12/521,109 · Granted May 19, 2015

Agents for reversing epigenetic silencing of genes

Inventors: William G. Nelson (Towson, MD); Srinivasan Yegnasubramanian (Baltimore, MD); Xiaohui Lin (Redlands, CA); Traci J. Speed (Baltimore, MD); Zachery Reichert (Baltimore, MD)
Assignee: The Johns Hopkins University
G01N33/5011A61K31/4184G01N33/6875G01N2500/00
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Quick Facts
Patent No.
US 9,034,574
App. No.
12/521,109
Granted
May 19, 2015
Kind
B2
Abstract

The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.

Claims (8)

1. A method of treating prostate cancer in a subject, comprising administering to the subject a methylbinding domain (MBD) pathway antagonist of structural Formula III:

2. The method of claim 1 , wherein the prostate cancer is metastatic prostate cancer.

3. The method of claim 1 , wherein the subject is a human.

4. The method of claim 1 , wherein the MBD pathway antagonist inhibits interaction of MBD2 with methylated genomic DNA.

5. The method of claim 1 , wherein the MBD pathway antagonist reduces methyl binding domain protein 2 (MBD2) activity.

6. The method of claim 5 , wherein the MBD pathway antagonist reactivates expression of GSTP1 gene having CpG island hypermethylation.

7. The method of claim 6 , wherein the antagonist inhibits interaction of MBD2 with methylated genomic DNA.

8. The method of claim 1 , wherein the MBD pathway antagonist reduces methyl CpG binding protein 2 (MeCP2) activity.

Assignments (2)
CONFIRMATORY LICENSE Recorded Dec 28, 2017
From: JOHNS HOPKINS UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 044968/0898 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 16, 2009
From: NELSON, WILLIAM G.; YEGNASUBRAMANIAN, SRINIVASAN; LIN, XIAOHUI; SPEED, TRACI J.; REICHERT, ZACHERY
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 022968/0159 →
Continuity (2)
Provisional Application 60877310 · Dec 27, 2006
Related Publication 20100093768A1 · Apr 15, 2010