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• W3204016418 startingPage "113871" @default.
• W3204016418 abstract "The ubiquitination of the hypoxia-inducible factor-1α (HIF-1α) is mediated by interacting with the von Hippel-Lindau protein (VHL), and is associated with cancer, chronic anemia, and ischemia. VHL, an E3 ligase, has been reported to degrade HIF-1 for decades, however, there are few successful inhibitors currently. Poor understanding of the binding pocket and a lack of in-depth exploration of the interactions between two proteins are the main reasons. Hence, we developed an effective strategy to identify and design new inhibitors for protein-protein interaction targets. The hydroxyproline (Hyp564) of HIF-1α contributed the key interaction between HIF-1α and VHL. In this study, detailed information of the binding pocket were explored by alanine scanning, site-directed mutagenesis and molecular dynamics simulations. Interestingly, we found the interaction(s) between Y565 and H110 played a key role in the binding of VHL/HIF-1α. Based on the interactions, 8 derivates of VH032, 16a-h, were synthesized by introducing various groups bounded to H110. Further assay on protein and cellular level exhibited that 16a-h accessed higher binding affinity to VHL and markable or modest improvement in stabilization of HIF-1α or HIF-1α-OH in HeLa cells. Our work provides a new orientation for the modification or design of VHL/HIF-1α protein-protein interaction inhibitors." @default.
• W3204016418 created "2021-10-11" @default.
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• W3204016418 date "2022-01-01" @default.
• W3204016418 modified "2023-10-16" @default.
• W3204016418 title "An efficient strategy for digging protein-protein interactions for rational drug design - A case study with HIF-1α/VHL" @default.
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• W3204016418 doi "https://doi.org/10.1016/j.ejmech.2021.113871" @default.
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• W3204016418 hasPublicationYear "2022" @default.
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