Bookmark and Share
BioAssay: AID 652103

qHTS for Inhibitors of phosphatidylinositol 5-phosphate 4-kinase (PI5P4K): Summary

Phosphatidylinositol (PI) signaling has been shown to impact a large and diverse set of cellular processes including proliferation, survival, and growth; their dysregulation is common in cancer and other diseases. Recently, PI5P has been shown to regulate the tumor suppressor ING2. In addition to finding PI5P, we discovered the type II phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) family more ..
_
   
AID: 652103
Data Source: NCGC (PI5P4K000)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2013-03-14
Modify Date: 2013-03-18
Target
Related Experiments
AIDNameTypeComment
652105qHTS for Inhibitors of phosphatidylinositol 5-phosphate 4-kinase (PI5P4K)Confirmatorydepositor-specified cross reference: qHTS AID
743285qHTS for Inhibitors of PI5P4K: ADP-Glo counter assayConfirmatorydepositor-specified cross reference
743286qHTS for Inhibitors of PI5P4K: Confirmation in Primary AssayConfirmatorydepositor-specified cross reference
743379On Hold
743380On Hold
743381On Hold
743382On Hold
743383On Hold
Description:
Phosphatidylinositol (PI) signaling has been shown to impact a large and diverse set of cellular processes including proliferation, survival, and growth; their dysregulation is common in cancer and other diseases. Recently, PI5P has been shown to regulate the tumor suppressor ING2. In addition to finding PI5P, we discovered the type II phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) family (alpha, beta, gamma isoforms) that catalyze the conversion of PI5P to PI(4,5)P2. Alternatively, PI(4,5)P2 can also be synthesized through phosphatidylinositol-4-phosphate (PI4P) by the type I phosphatidylinositol 4-phosphate 5-kinases (PI4P5K). These PI5P4K enzymes therefore represent one way by which cells can regulate endogenous PI5P levels and play important roles in insulin signaling and in stress responses. Furthermore, recent findings have demonstrated a critical role for PI5P4K in tumor cell growth and support a potential role in oncogenesis for PI5P4K.

This proposal aims to identify and optimize specific modulators of human PI5P4K, phosphatidylinositol-5-phosphate 4-kinase (Type II PIPK), a family of kinases that regulate AKT signaling and tumor cell growth. In this project we aim to identify inhibitors of human PI5P4K using a quantitative high-throughput screening approach against the MLSMR containing ~400,000 small molecules.

NIH Chemical Genomics Center [NCGC]
NIH Molecular Libraries Probe Centers Network [MLPCN]

MLPCN Grant: MH096575
Assay Submitter (PI): Atsuo Sasaki, Beth Israel Deaconess Medical Center
Protocol
Please see linked AIDs for detailed protocols.
Comment
This project is ongoing and will be updated at a later point.
Additional Information
Grant Number: MH096575

PageFrom: