US 8,476,458 B2Granted

Methods and compositions for modulating P300/CBP activity

AssigneesThe Wistar Institute, The John Hopkins University

InventorsRonen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee

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Abstract

The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.

Claims2

Dependent claims

A p300/CBP inhibitor selected from the group of:

Dependencies are inferred from the claim text.

Facts

Application: 12/665,751Filed 19 Jun 2008 · us provisional application
Priority: 21 Jun 2007
Published: US 2010/0216853 A126 Aug 2010
Granted: 2 Jul 2013
Term ends: Not estimatedThe source records don’t support an estimate.

Classification27 codes

A61K 31/5585
Having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes: having five-membered rings containing oxygen as the…
A61K 31/4015
Having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil: having oxo groups…
A61K 31/402
Having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil: 1-aryl substituted,…
A61K 31/4025
Having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil: not condensed and…