Unknown

Dataset Information

0

Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases.


ABSTRACT: p300 and CREB-binding protein (CBP) are essential for a multitude of cellular processes. Dysregulation of p300/CBP histone acetyltransferase activity is linked to a broad spectrum of human diseases including cancers. A novel drug-like spirohydantoin (21) has been discovered as a selective orally bioavailable inhibitor of p300/CBP histone acetyltransferase. Lead compound 21 is more potent than the first-in-class lead A-485 in both enzymatic and cellular assays and lacks the off-target inhibition of dopamine and serotonin transporters, that was observed with A-485.

SUBMITTER: Ji Z 

PROVIDER: S-EPMC8392731 | biostudies-literature |

REPOSITORIES: biostudies-literature

Similar Datasets

| S-EPMC5767893 | biostudies-literature
| S-EPMC9274749 | biostudies-literature
| S-EPMC7294707 | biostudies-literature
| S-EPMC9165588 | biostudies-literature
| S-EPMC5949730 | biostudies-literature
| S-EPMC4948009 | biostudies-literature
| S-EPMC8201761 | biostudies-literature
| S-EPMC2643075 | biostudies-literature
| S-EPMC4867477 | biostudies-literature
| S-EPMC8155265 | biostudies-literature