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Crystal structures of human NSDHL
and development of its novel inhibitor…
Crystal structures of human NSDHL
and development of its novel inhibitor with the potential to suppress EGFR activity
Introduction
NSDHL
- NAD(P)-dependent steroid dehydrogenase-like(NSDHL)
- essential enzyme in downstream of human cholesterol synthesis pathway
- Also, strongly related to cancer growth and the signaling of proto-oncogenes
- NSDHL regulates the expression and signaling of EGFR
- Loss of Nsdhl gene --> sensitizes cancer cells to EGFR-targeting inhibitor
Purpose of this study
- To elucidate the crystal structures of NSDHL
- To identify a structure-based inhibitor of NSDHL for novel and effective treatment against cholesterol imbalance and cancers
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Conclusion
- Novel NSDHL inhibitor, Compound 9, was the most potent inhibitor among the analogs included in this study
- Compound 9 can suppress EGFR expression and EGFR-dependent signaling and sensitization to Erlotinib
- Provides valuable insights into the therapeutic potential of targeting NSDHL