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TitleDiscovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
Journal, issue, pagesJ. Med. Chem., Year 2024
Publish dateJun 24, 2024 (structure data deposition date)
AuthorsHudkins, R.L. / Allen, E. / Balcer, A. / Hoffman, I.D. / Iyer, S. / Neal, M. / Nelson, K.J. / Rideout, M. / Ye, Q. / Starrett, J.H. ...Hudkins, R.L. / Allen, E. / Balcer, A. / Hoffman, I.D. / Iyer, S. / Neal, M. / Nelson, K.J. / Rideout, M. / Ye, Q. / Starrett, J.H. / Patel, P. / Harris, T. / Swanson, R.V. / Bensen, D.C.
External linksJ. Med. Chem. / PubMed:39258897
MethodsX-ray diffraction
Resolution2.53 - 2.939 Å
Structure data

PDB-9cd5:
FGFR1 Kinase Domain Soak with Inhibitor TYRA-300
Method: X-RAY DIFFRACTION / Resolution: 2.939 Å

PDB-9cd7:
FGFR3 Kinase Domain with Inhibitor TYRA-300
Method: X-RAY DIFFRACTION / Resolution: 2.53 Å

Chemicals

ChemComp-EDO:
1,2-ETHANEDIOL

PDB-1av2:
Gramicidin A/CsCl complex, active as a dimer

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

ChemComp-GOL:
GLYCEROL

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Kinase / Transferase / Inhibitor / Cancer / Achondroplasia / FGFR3 / FGFR / TRANSFERASE-TRANSFERASE INHIBITOR complex

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