Human Family With Sequence Similarity 83 Member B (FAM83B)The content of this page was edited by SGC and matteoferla on the 2019-10-07 15:59:03.951789.
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FAM83A-H are newly identified oncogenes characterised by a conserved DUF1669 domain. FAM83B can substitute for Ras to promote malignant transformation. Ablation of FAM83B or mutation of Lys230 inhibits malignant phenotypes, implicating FAM83B as potential therapeutic target. As part of this TEP, we solved the first crystal structures from the FAM83 family, including FAM83A and FAM83B. The structures of the DUF1669 domain reveal a phospholipase D-like fold lacking conservation of key catalytic residues. We deorphanise the FAM83 DUF1669 domain as a critical docking scaffold for binding of casein kinase 1 isoforms. Finally, using XChem fragment screening we report chemical fragments that bind to Lys230 in the central pocket of the DUF1669 and form starting points for potential drug development.
Structures available in TEP:
- 2.68 Å structure of FAM83A DUF1669 domain (PDB:4URJ ): ,
- 1.58 Å structure of FAM83B DUF1669 domain (PDB:5LZK ): ,
- 1.78 Å structure of FAM83B with fragment FM001923a (PDB:5QHI ): ,
- 1.76 Å structure of FAM83B with fragment FM002203a (PDB:5QHJ ): ,
- 1.72 Å structure of FAM83B with fragment FM001730a (PDB:5QHK ): ,
- 1.80 Å structure of FAM83B with fragment FM001894a (PDB:5QHL ): ,
- 1.84 Å structure of FAM83B with fragment FM000368b (PDB:5QHM ): ,
- 1.81 Å structure of FAM83B with fragment FM002168a (PDB:5QHN ): ,
- 1.74 Å structure of FAM83B with fragment FM001730a (PDB:5QHO ): ,
- 2.10 Å structure of FAM83B with fragment XS094794b (PDB:5QHP ): ,
- 2.03 Å structure of FAM83B with fragment FM001992a (PDB:5QHQ ): ,
- 1.95 Å structure of FAM83B with fragment FM002208b (PDB:5QHR ): ,
- 1.95 Å structure of FAM83B with fragment FF000014a (PDB:5QHS ): ,