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TitleNovel, potent, and orally bioavailable LSD1 inhibitors induce fetal hemoglobin synthesis in a sickle cell disease mouse model.
Journal, issue, pagesBlood, Vol. 146, Page 356-368, Year 2025
Publish dateAug 23, 2024 (structure data deposition date)
AuthorsWang, Y. / Yu, L. / Deng, K. / Packiarajan, M. / Aguilar, A. / An, S. / Liu, X. / Myers, G. / Oh, H. / Singh, S.A. ...Wang, Y. / Yu, L. / Deng, K. / Packiarajan, M. / Aguilar, A. / An, S. / Liu, X. / Myers, G. / Oh, H. / Singh, S.A. / Cho, U.S. / Wang, S. / Guan, Y. / White, A.D. / Khoriaty, R. / Engel, J.D.
External linksBlood / PubMed:40332031
MethodsX-ray diffraction
Resolution2.66 Å
Structure data

PDB-9dbp:
Crystal structure of the LSD1/CoREST histone demethylase in complex with the cofactor FAD and the inhibitor GSK690
Method: X-RAY DIFFRACTION / Resolution: 2.66 Å

Chemicals

ChemComp-FAD:
FLAVIN-ADENINE DINUCLEOTIDE / FAD*YM

ChemComp-GOL:
GLYCEROL

PDB-1a5u:
PYRUVATE KINASE COMPLEX WITH BIS MG-ATP-NA-OXALATE

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsGENE REGULATION / LSD1-CoREST / Histone methyltransferase inhibitor

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