Articles with "scaffold repurposing" as a keyword



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Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.

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Published in 2021 at "European journal of medicinal chemistry"

DOI: 10.1016/j.ejmech.2021.113381

Abstract: KRAS plays an essential role in regulating cell proliferation, differentiation, migration and survival. Mutated KRAS is a major driver of malignant transformation in multiple human cancers. We showed previously that fendiline (6) is an effective… read more here.

Keywords: membrane localization; localization inhibitors; scaffold repurposing; kras plasma ... See more keywords
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Exploiting ELIOT for Scaffold-Repurposing Opportunities: TRIM33 a Possible Novel E3 Ligase to Expand the Toolbox for PROTAC Design

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Published in 2022 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms232214218

Abstract: The field of targeted protein degradation, through the control of the ubiquitin–proteasome system (UPS), is progressing considerably; to exploit this new therapeutic modality, the proteolysis targeting chimera (PROTAC) technology was born. The opportunity to use… read more here.

Keywords: exploiting eliot; scaffold repurposing; ligase; novel ligase ... See more keywords