Chemical Starting Matter for HNF4? Ligand Discovery and Chemogenomics.
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ABSTRACT:
SUBMITTER: Meijer I
PROVIDER: S-EPMC7660650 | biostudies-literature | 2020 Oct
REPOSITORIES: biostudies-literature
Publications
Chemical Starting Matter for HNF4α Ligand Discovery and Chemogenomics.
Meijer Isabelle I Willems Sabine S Ni Xiaomin X Heering Jan J Chaikuad Apirat A Merk Daniel D
International journal of molecular sciences 20201024 21
Hepatocyte nuclear factor 4α (HNF4α) is a ligand-sensing transcription factor and presents as a potential drug target in metabolic diseases and cancer. In humans, mutations in the HNF4α gene cause maturity-onset diabetes of the young (MODY), and the elevated activity of this protein has been associated with gastrointestinal cancers. Despite the high therapeutic potential, available ligands and structure-activity relationship knowledge for this nuclear receptor are scarce. Here, we disclose a che ...[more]
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