ArticleBioorganic & medicinal chemistry letters2016
Application of oxime-diversification to optimize ligand interactions within a cryptic pocket of the polo-like kinase 1 polo-box domain.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Affinity enhancement of polo-like kinase 1 polo box domain-binding ligands by a bivalent approach using a covalent kinase-binding component.RSC chemical biology · 2024Article
- Solid-Phase Synthesis and Biological Evaluation of Peptides ADP-Ribosylated at Histidine.Angewandte Chemie (Weinheim an der Bergstrasse, Germany) · 2024Article
- Solid-Phase Synthesis and Biological Evaluation of Peptides ADP-Ribosylated at Histidine.Angewandte Chemie (International ed. in English) · 2024Article
- Identification of multidentate tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitors that simultaneously access the DNA, protein and catalytic-binding sites by oxime diversification.RSC chemical biology · 2023Article
- Development of ultra-high affinity bivalent ligands targeting the polo-like kinase 1.RSC chemical biology · 2022Article
- Design and synthesis of a new orthogonally protected glutamic acid analog and its use in the preparation of high affinity polo-like kinase 1 polo-box domain - binding peptide macrocycles.Organic & biomolecular chemistry · 2021Article
- Application of Post Solid-Phase Oxime Ligation to Fine-Tune Peptide-Protein Interactions.Molecules (Basel, Switzerland) · 2020Review
- Development of Highly Selective 1,2,3-Triazole-containing Peptidic Polo-like Kinase 1 Polo-box Domain-binding Inhibitors.Molecules (Basel, Switzerland) · 2019Article
- Targeting Protein-Protein Interactions of Tyrosine Phosphatases with Microarrayed Fragment Libraries Displayed on Phosphopeptide Substrate Scaffolds.ACS combinatorial science · 2019Article
- Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors.Bioorganic & medicinal chemistry letters · 2018Article
- Enhancing polo-like kinase 1 selectivity of polo-box domain-binding peptides.Bioorganic & medicinal chemistry · 2017Article
- Current progress and future perspectives in the development of anti-polo-like kinase 1 therapeutic agents.F1000Research · 2017Review
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
By a process involving initial screening of a set of 87 aldehydes using an oxime ligation-based strategy, we were able to achieve a several-fold affinity enhancement over one of the most potent previously known polo-like kinase 1 (Plk1) polo-box domain (PBD) binding inhibitors. This improved binding may result by accessing a newly identified auxiliary region proximal to a key hydrophobic cryptic pocket on the surface of the protein. Our findings could have general applicability to the design of PBD-binding antagonists.
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