8EKX
Structure of MBP-Mcl-1 in complex with MIK665
Summary for 8EKX
| Entry DOI | 10.2210/pdb8ekx/pdb |
| Related PRD ID | PRD_900001 |
| Descriptor | Maltose/maltodextrin-binding periplasmic protein,Induced myeloid leukemia cell differentiation protein Mcl-1, alpha-D-glucopyranose-(1-4)-alpha-D-glucopyranose, (2~{R})-2-[5-[3-chloranyl-2-methyl-4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl]-6-(4-fluorophenyl)thieno[2,3-d]pyrimidin-4-yl]oxy-3-[2-[[2-(2-methoxyphenyl)pyrimidin-4-yl]methoxy]phenyl]propanoic acid, ... (4 entities in total) |
| Functional Keywords | mbp-mcl-1 fusion protein, apoptosis, mik665 |
| Biological source | Escherichia coli K-12 More |
| Total number of polymer chains | 1 |
| Total formula weight | 60354.58 |
| Authors | |
| Primary citation | Yuda, J.,Will, C.,Phillips, D.C.,Abraham, L.,Alvey, C.,Avigdor, A.,Buck, W.,Besenhofer, L.,Boghaert, E.,Cheng, D.,Cojocari, D.,Doyle, K.,Hansen, T.M.,Huang, K.,Johnson, E.F.,Judd, A.S.,Judge, R.A.,Kalvass, J.C.,Kunzer, A.,Lam, L.T.,Li, R.,Martin, R.L.,Mastracchio, A.,Mitten, M.,Petrich, A.,Wang, J.,Ward, J.E.,Zhang, H.,Wang, X.,Wolff, J.E.,Bell-McGuinn, K.M.,Souers, A.J. Selective MCL-1 inhibitor ABBV-467 is efficacious in tumor models but is associated with cardiac troponin increases in patients. Commun Med (Lond), 3:154-154, 2023 Cited by PubMed Abstract: MCL-1 is a prosurvival B-cell lymphoma 2 family protein that plays a critical role in tumor maintenance and survival and can act as a resistance factor to multiple anticancer therapies. Herein, we describe the generation and characterization of the highly potent and selective MCL-1 inhibitor ABBV-467 and present findings from a first-in-human trial that included patients with relapsed/refractory multiple myeloma (NCT04178902). PubMed: 37880389DOI: 10.1038/s43856-023-00380-z PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.55 Å) |
Structure validation
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