MASTER REGULATORS OF GENE EXPRESSION
A transcription factor reads the genome and orchestrates its expression by integrating accessory proteins at specific regions of DNA.
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SUPREME
DRUG
TARGETS
Transcription factors (TFs) have long been the aspirational targets of drug developers, based on their central role in cancer and other diseases.
What are TFs
TFs are DNA-binding proteins that can activate or repress DNA transcription and, therefore control gene expression.
Why they matter
As drug targets, TFs differ from many other target classes given that they determine cell and tissue identity, controlling which genes are or are not expressed.
THE LARGEST PROTEIN FAMILY:
TF MUTATIONS CAUSE:
ELUSIVE
FOR
DECADES
Despite a broad consensus around their role in disease and vast therapeutic potential, transcription factors have been elusive targets for drug discovery.
- <1% of TFs have been successfully targeted for therapeutics.
- Targeting of TFs has previously been limited by the inability to systematically link their biochemical function to targetable sites for small molecule drug discovery.
A FLARE
OF
INSPIRATION
Setting the stage
Flare Therapeutics’ scientific co-founders have decades of experience understanding the biology and structure of TFs. Their seminal work includes elucidating molecular mechanisms for targeting TFs with ligands and structure-function relationships of TF complexes.
FlareTx’s integrated platform leverages two complementary strategies to identify ligandable pockets within transcription factors: pocket mapping and chemoproteomics
Pocket mapping uses advanced genetics and structural biology to pinpoint novel druggable and functional nodes within transcription factors. The second approach, chemoproteomics, employs innovative chemistry and cellular screening to explore the nucleus directly, revealing hidden pockets that may only appear within complex protein structures or specific cellular states. This approach allows FlareTx to discover ligands across the so-called “undruggable” proteome, opening up new possibilities for correcting abnormal gene expression linked to disease.
MASTER REGULATORS OF GENE EXPRESSION
A transcription factor reads the genome and orchestrates its expression by integrating accessory proteins at specific regions of DNA.
........
THE HISTORICALLY NARROW VIEW MAKES TFs ELUSIVE
Significant efforts have been made to target transcription factors because of their central role in disease. However, these efforts have focused on individual transcription factor domains in isolation. This reductionist framework obscures the most crucial aspects of TF biochemistry.
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AN APPRECIATION OF THE COMPLEX CHOREOGRAPHY
Precise gene control requires cooperative communication and allosteric interaction among the elements of the transcription machinery. Taking an approach that reflects the cooperative nature of TFs reveals new insights and therapeutic opportunities.
........
AN APPRECIATION OF THE COMPLEX CHOREOGRAPHY
Precise gene control requires cooperative communication and allosteric interaction among the elements of the transcription machinery. Taking an approach that reflects the cooperative nature of TFs reveals new insights and therapeutic opportunities.
........