Bookmark and Share
BioAssay: AID 540328

Broad Institute Identification of MITF small molecule inhibitors Activator Probe Project

This project aims to execute a robust and sensitive primary screen to identify activators of MITF activity. The short-term goals of these experiments are to identify MITF activators that recapitulate genetic manipulation of MITF. The longer term goal is to use these probes to elucidate molecular pathways regulating MITF activity with the goal of translating this knowledge and these leads into more ..
_
   
 Related BioAssays
 Related BioAssays
AID: 540328
Data Source: Broad Institute (2084_Activator_Project)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2011-08-02
Modify Date: 2011-08-05
Related Experiments
AIDNameTypeComment
488899MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_SinglePoint_HTS_ActivityScreeningdepositor-specified cross reference: MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_SinglePoint_HTS_Activity
540258MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Activator_Dose_CherryPick_ActivityConfirmatorydepositor-specified cross reference: 725 CherryPick compounds at Dose in 2084-01 01 TRPM-1 promoter activity assay measuring Activity
540259MITF Act Counter Assay: HeLa CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-08_Activator_Dose_CherryPick_ActivityConfirmatorydepositor-specified cross reference: 725 CherryPick compounds at Dose in 2084-08 08 Cytotoxicity in HeLa Cells measuring Activity
588334MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Activator_SinglePoint_HTS_ActivityScreeningdepositor-specified cross reference
651775MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Activator_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
Description:
Primary Collaborators:
David Fisher,MGH,Dfisher3@partners.org
Rizwan Haq,MGH,rhaq@partners.org

Project Goal:
This project aims to execute a robust and sensitive primary screen to identify activators of MITF activity. The short-term goals of these experiments are to identify MITF activators that recapitulate genetic manipulation of MITF. The longer term goal is to use these probes to elucidate molecular pathways regulating MITF activity with the goal of translating this knowledge and these leads into therapeutic opportunities. One desired activity of an activator is to increase melanin production. Increased melanin production in the skin of mice serves to protect these animals from UV-induced DNA damage and subsequent melanoma formation.


MITF, melanin, melanoma
Biological Relevance:
Micropthalmia-associated transcription factor (MITF) is a tissue-restricted basic helix-loop-helix leucine zipper (bHLH-Zip) transcription factor that is essential for melanocyte differentiation, function and survival. In approximately 15% of melanomas, amplification of MITF is oncogenic, as their survival and growth is dependent on MITF expression. In nearly all other melanomas, MITF remains essential for cell survival, making MITF an attractive lineage-specific target for melanoma therapy. Controlling the activity of MITF could be useful in understanding ways of combating melanoma by inhibition or increasing melanin production in keratinocytes to prevent UV-induced skin damage.
Additional Information
Grant Number: 1 R03 DA031089-01

PageFrom: