ArticlePloS one2015
A Maltose-Binding Protein Fusion Construct Yields a Robust Crystallography Platform for MCL1.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Deciphering molecular specificity in MCL-1/BAK interaction and its implications for designing potent MCL-1 inhibitors.Cell death and differentiation · 2025Article
- Structural basis of BAK sequestration by MCL-1 in apoptosis.Molecular cell · 2025Article
- BRD-810 is a highly selective MCL1 inhibitor with optimized in vivo clearance and robust efficacy in solid and hematological tumor models.Nature cancer · 2024Article
- Interaction between moxifloxacin and Mcl-1 and MITF proteins: the effect on growth inhibition and apoptosis in MDA-MB-231 human triple-negative breast cancer cells.Pharmacological reports : PR · 2022Article
- Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment.Bioorganic & medicinal chemistry · 2021Article
- Novel Insights into the Roles of Bcl-2 Homolog Nr-13 (vNr-13) Encoded by Herpesvirus of Turkeys in the Virus Replication Cycle, Mitochondrial Networks, and Apoptosis Inhibition.Journal of virology · 2020Article
- Antibody fragments structurally enable a drug-discovery campaign on the cancer target Mcl-1.Acta crystallographica. Section D, Structural biology · 2019Article
- Establishing Drug Discovery and Identification of Hit Series for the Anti-apoptotic Proteins, Bcl-2 and Mcl-1.ACS omega · 2019Article
- MBP-binding DARPins facilitate the crystallization of an MBP fusion protein.Acta crystallographica. Section F, Structural biology communications · 2018Article
- Crystal Structures of Anti-apoptotic BFL-1 and Its Complex with a Covalent Stapled Peptide Inhibitor.Structure (London, England : 1993) · 2018Article
- Guidelines for the successful generation of protein-ligand complex crystals.Acta crystallographica. Section D, Structural biology · 2017Review
- Design of an expression system to enhance MBP-mediated crystallization.Scientific reports · 2017Article
- Pentameric quaternary structure of the intracellular domain of serotonin type 3A receptors.Scientific reports · 2016Article
- Crystal structures of MBP fusion proteins.Protein science : a publication of the Protein Society · 2016Review
- Protein stability: a crystallographer's perspective.Acta crystallographica. Section F, Structural biology communications · 2016Review
- Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1).ACS medicinal chemistry letters · 2014Article
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Authors and funding
18 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Crystallization of a maltose-binding protein MCL1 fusion has yielded a robust crystallography platform that generated the first apo MCL1 crystal structure, as well as five ligand-bound structures. The ability to obtain fragment-bound structures advances structure-based drug design efforts that, despite considerable effort, had previously been intractable by crystallography. In the ligand-independent crystal form we identify inhibitor binding modes not observed in earlier crystallographic systems. This MBP-MCL1 construct dramatically improves the structural understanding of well-validated MCL1 ligands, and will likely catalyze the structure-based optimization of high affinity MCL1 inhibitors.
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