Bachovchin_2010_Probe.Report.1__

Reference

Title : Probe Report for RBBP9 Inhibitors - Probe 2 - Bachovchin_2010_Probe.Report.1__
Author(s) : Bachovchin DA , Speers AE , Brown SJ , Cravatt BF , Spicer T , Mercer BA , Ferguson J , Hodder P , Rosen HR
Ref : Probe Report , : , 2010
Abstract :

The retinoblastoma (RB) tumor suppressor protein controls cell cycle progression by regulating the activity of the transcription factor E2F, which activates genes essential for DNA replication. Thus, factors that bind and regulate RB activity are considered valuable targets for preventing tumorigenesis. The enzyme RB binding protein 9 (RBBP9) is widely expressed in different tissues and upregulated in certain tumors. As a result, the identification of compounds that selectively inhibit RBBP9 activity would serve as potentially valuable probes for the study of apoptosis, cell cycle, and tumorigenesis. We previously reported a modestly potent, RBBP9 reversible inhibitor, ML081 (CID-6603320). However, ML081 exhibits high cytotoxicity. We, therefore, have now identified a newer probe, ML114 (CID-5934766), which is 10-fold more potent than ML081, exhibits no cytotoxicity, and is from an entirely different structural and mechanistic class of compounds that covalently inhibit RBBP9. This new probe will be useful for in vitro assays in which it is desirable to specifically block RBBP9 activity for primary research purposes.

PubMedSearch : Bachovchin_2010_Probe.Report.1__
PubMedID: 21433382
Gene_locus related to this paper: human-RBBP9

Related information

Inhibitor Emetine    ML114
Gene_locus human-RBBP9
Family Hydrolase_RBBP9_YdeN

Citations formats

Bachovchin DA, Speers AE, Brown SJ, Cravatt BF, Spicer T, Mercer BA, Ferguson J, Hodder P, Rosen HR (2010)
Probe Report for RBBP9 Inhibitors - Probe 2
Probe Report :

Bachovchin DA, Speers AE, Brown SJ, Cravatt BF, Spicer T, Mercer BA, Ferguson J, Hodder P, Rosen HR (2010)
Probe Report :