8UAK
Crystal structure of the catalytic domain of human PKC alpha (D463N, V568I, S657E) in complex with Darovasertib (NVP-LXS196) at 2.82-A resolution
Summary for 8UAK
Entry DOI | 10.2210/pdb8uak/pdb |
Related | 8u37 |
Descriptor | Protein kinase C alpha type, (6M)-3-amino-N-[3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl]-6-[3-(trifluoromethyl)pyridin-2-yl]pyrazine-2-carboxamide (3 entities in total) |
Functional Keywords | inhibitor, complex, darovasertib, nvp-lxs196, nvp-cjl037, 8u37, transferase-inhibitor complex, transferase/inhibitor |
Biological source | Homo sapiens (human) |
Total number of polymer chains | 1 |
Total formula weight | 41153.88 |
Authors | Romanowski, M.J.,Lam, J.,Visser, M. (deposition date: 2023-09-21, release date: 2024-01-24, Last modification date: 2024-01-31) |
Primary citation | Visser, M.,Papillon, J.P.N.,Luzzio, M.,LaMarche, M.J.,Fan, J.,Michael, W.,Wang, D.,Zhang, A.,Straub, C.,Mathieu, S.,Kato, M.,Palermo, M.,Chen, C.,Ramsey, T.,Joud, C.,Barrett, R.,Vattay, A.,Guo, R.,Bric, A.,Chung, F.,Liang, G.,Romanowski, M.J.,Lam, J.,Thohan, S.,Atassi, F.,Wylie, A.,Cooke, V.G. Discovery of Darovasertib (NVP-LXS196), a Pan-PKC Inhibitor for the Treatment of Metastatic Uveal Melanoma. J.Med.Chem., 67:1447-1459, 2024 Cited by PubMed: 38198520DOI: 10.1021/acs.jmedchem.3c02002 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.82 Å) |
Structure validation
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