Human Family With Sequence Similarity 83 Member B (FAM83B); A Target Enabling Package
| العنوان: | Human Family With Sequence Similarity 83 Member B (FAM83B); A Target Enabling Package |
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| المؤلفون: | Daniel M. Pinkas, Joshua C. Bufton, Alice E. Fox, Gian Filippo Ruda, Romain Talon, Tobias Krojer, Anthony R. Bradley, Frank von Delft, Paul E. Brennan, Luke J. Fulcher, Polyxeni Bozatzi, Theresa Tachi-Menson, Kevin Z. L. Wu, Timothy D. Cummins, Karen Dunbar, Sabin Shrestha, Nicola T. Wood, Simone Weidlich, Thomas J. Macartney, Joby Varghese, Robert Gourlay, David G. Campbell, Luke D. Hutchinson, Janis Vogt, Fay Cooper, Kevin S. Dingwell, James C. Smith, Gopal P. Sapkota, Alex N. Bullock |
| سنة النشر: | 2018 |
| المجموعة: | Zenodo |
| مصطلحات موضوعية: | Protein, Target Enabling Package, Disease, Structure, Cancer, Neuropsychiatry, Neuro, Neurological Genetic Disorders, Metabolic Diseases, Oncology, Infectious Disease, Malaria, Structural Genomics, Drug Discovery, Orphan Disease, Drug Target, Chemical Biology, Probe, Structure Discovery, FAM83B |
| الوصف: | 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. ; Further versions of this document will contain experimental data about the FAM83 TEP. |
| نوع الوثيقة: | dataset |
| اللغة: | unknown |
| العلاقة: | info:eu-repo/grantAgreement/WT/Molecular Basis of Cell Function/106169/; https://www.thesgc.org/tepTest; https://zenodo.org/communities/sgctepsTest; https://zenodo.org/record/1342541Test; https://doi.org/10.5281/zenodo.1342541Test; oai:zenodo.org:1342541 |
| DOI: | 10.5281/zenodo.1342541 |
| الإتاحة: | https://doi.org/10.5281/zenodo.1342541Test https://doi.org/10.5281/zenodo.1342540Test https://zenodo.org/record/1342541Test |
| حقوق: | info:eu-repo/semantics/openAccess ; https://creativecommons.org/licenses/by/4.0/legalcodeTest |
| رقم الانضمام: | edsbas.1A7E203D |
| قاعدة البيانات: | BASE |
| DOI: | 10.5281/zenodo.1342541 |
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