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TitlePRT3789 Is a First-in-Human SMARCA2-Selective Degrader That Induces Synthetic Lethality in SMARCA4-Mutated Cancers.
Journal, issue, pagesCancer Res., Vol. 86, Page 213-235, Year 2026
Publish dateOct 2, 2024 (structure data deposition date)
AuthorsHulse, M. / Wang, M. / Xu, C. / Carter, J. / Agarwal, A. / Lu, L. / Pitis, P. / Bhagwat, N. / Rager, J. / Kurian, J. ...Hulse, M. / Wang, M. / Xu, C. / Carter, J. / Agarwal, A. / Lu, L. / Pitis, P. / Bhagwat, N. / Rager, J. / Kurian, J. / Basch, C. / Sivakumar, M. / Burtell, J. / Mondal, A. / Grego, A. / Moore, A. / Bachner, C. / Vykuntam, K. / Reichelderfer, A. / Park, J. / Cote, J. / Cowart, M. / Osinubi, O.P. / Bigot, L. / Da Silva, A. / Nobre, C. / Meteau, M. / Soares, M. / Tang, H.Y. / Bersch, K. / Dai, C. / Cao, G. / Shen, B. / Emm, T. / Ruepp, S. / Xavier, J. / Tankersley, C. / Heiser, D. / Lee, S.H. / Geeganage, S. / Ruggeri, B. / Lin, H. / Novotny, W. / Huang, J. / Vaddi, K. / Combs, A. / Scherle, P. / Ito, K.
External linksCancer Res. / PubMed:40991405
MethodsX-ray diffraction
Resolution2.11 - 3.3 Å
Structure data

PDB-9dtx:
Crystal structure of PRT3789 in complex with the bromodomain of human BRG1 (SMARCA4) and pVHL:ElonginC:ElonginB
Method: X-RAY DIFFRACTION / Resolution: 2.11 Å

PDB-9dty:
Crystal structure of PRT3789 in complex with the bromodomain of human BRM (SMARCA2) and pVHL:ElonginC:ElonginB
Method: X-RAY DIFFRACTION / Resolution: 3.19 Å

PDB-9du0:
Crystal structure of the bromodomain of human BRM (SMARCA2) in complex with a SMARCA-BD binder
Method: X-RAY DIFFRACTION / Resolution: 3 Å

PDB-9mr9:
Crystal structure of AU-15330 in complex with the bromodomain of human BRM (SMARCA2) and pVHL:ElonginC:ElonginB
Method: X-RAY DIFFRACTION / Resolution: 3.3 Å

Chemicals

PDB-1bb4:
HUMAN LYSOZYME DOUBLE MUTANT A96L, W109H

ChemComp-GOL:
GLYCEROL

ChemComp-EDO:
1,2-ETHANEDIOL

ChemComp-CL:
Unknown entry

ChemComp-HOH:
WATER

ChemComp-CIT:
CITRIC ACID

ChemComp-ACT:
ACETATE ION

PDB-1bb5:
HUMAN LYSOZYME MUTANT A96L COMPLEXED WITH CHITOTRIOSE

ChemComp-ZN:
Unknown entry

PDB-1bnt:
CARBONIC ANHYDRASE II INHIBITOR

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / SMARCA2 / Bromodomain / Protein-ligand complex / VHL / PROTAC / ternary complex

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