KAUST Research Conference

Computational Advances in Structural Biology

May 1 - 3, 2023 Auditorium between building 4 & 5

Targeting BTB domain proteins for cancer drug development


Abstract:
Cancer has recently become one of the leading causes of mortality worldwide. The present standard of care methods including tumor resection, chemotherapy and radiotherapy have poor prognosis, especially in aggressive types of cancer. Hence, there is a need to identify novel drug targets to enhance cancer drug development.

As malignant tumors tend to be heterogeneous, it is challenging to identify targets that could successfully be targeted by small-molecule drugs.

The highly conserved protein-protein interaction BTB domain, present in a number of oncogenic transcription factors, shows to be a promising target for newly synthesized small-molecule drugs.

Our aim is to elucidate the interaction between the BTB domain of the oncogenic transcription factors and newly developed inhibitors, ensuring specificity and potency.

To do so, we focus on the druggable BTB domains of the oncogenic transcription factors to characterize the interaction with ligands and enhance drug development.

We employed methods such as NMR to characterize the BTB domain of MIZ1 protein; ITC and circular dichroism to determine ligand affinity and to validate the interaction with ligands.

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