Accessing the Druggable Genetic Programs Governed by Mammalian bHLH-PAS Transcription Factors (360G-Wellcome-210664_Z_18_Z)
We have recently projected that the human bHLH-PAS proteins form a class of transcription factors with great therapeutic promise, and propose to subject this family to in-depth chemical and functional explorations. The sixteen members of this family are functionally non-redundant and have genetic links to cancers, metabolic syndromes, inflammatory diseases, and psychiatric conditions. They share common architectural features that include a conserved DNA-binding domain and dual PAS domains. Our specific aims are: 1. Identify chemical ligands for members of the human bHLH-PAS family. 2. Determine the ligand-dependent genomic signatures and cellular pathways governed by family members. 3. Probe the mechanisms by which chemical ligands manifest their activities through this family. These studies allow us to transition from having visualized their ligand binding properties to employing chemical tools for interrogating and manipulating their functional activities as transcription factors.
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Grant Details
Amount Awarded | 2161828 |
Applicant Surname | Rastinejad |
Approval Committee | Science Interview Panel |
Award Date | 2018-04-10T00:00:00+00:00 |
Financial Year | 2017/18 |
Grant Programme: Title | Investigator Award in Science |
Internal ID | 210664/Z/18/Z |
Lead Applicant | Prof Fraydoon Rastinejad |
Partnership Value | 2161828 |
Planned Dates: End Date | 2024-08-31T00:00:00+00:00 |
Planned Dates: Start Date | 2018-09-01T00:00:00+00:00 |
Recipient Org: Country | United Kingdom |
Region | South East |