ArticleACS medicinal chemistry letters2014
Single Diastereomer of a Macrolactam Core Binds Specifically to Myeloid Cell Leukemia 1 (MCL1).
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed.
- Identification of small molecule inhibitors of PPM1D using an integrated drug discovery platform.iScience · 2025Article
- Identification of Small Molecule Inhibitors of PPM1D Using a Novel Drug Discovery Platform.bioRxiv : the preprint server for biology · 2024Article
- Practical Considerations and Guidelines for Spectral Referencing for Fluorine NMR Ligand Screening.ACS omega · 2022Article
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- Structure Based Design of Non-Natural Peptidic Macrocyclic Mcl-1 Inhibitors.ACS medicinal chemistry letters · 2017Article
- DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.Journal of medicinal chemistry · 2016Article
- Targeting BCL-2 to enhance vulnerability to therapy in estrogen receptor-positive breast cancer.Oncogene · 2016Review
- Crystal structures of MBP fusion proteins.Protein science : a publication of the Protein Society · 2016Review
- An Intriguing Correlation Based on the Superimposition of Residue Pairs with Inhibitors that Target Protein-Protein Interfaces.Scientific reports · 2016Article
- Clinical implications of molecular heterogeneity in triple negative breast cancer.Breast (Edinburgh, Scotland) · 2015Review
- New dimension in therapeutic targeting of BCL-2 family proteins.Oncotarget · 2015Review
Corrections and comments
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Authors and funding
17 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A direct binding screen of 100 000 sp(3)-rich molecules identified a single diastereomer of a macrolactam core that binds specifically to myeloid cell leukemia 1 (MCL1). A comprehensive toolbox of biophysical methods was applied to validate the original hit and subsequent analogues and also established a binding mode competitive with NOXA BH3 peptide. X-ray crystallography of ligand bound to MCL1 reveals a remarkable ligand/protein shape complementarity that diverges from previously disclosed MCL1 inhibitor costructures.
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Registered trials
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