Pub. Date : 2021 Mar
PMID : 33483427
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Nelfinavir and its active metabolite M8 are partial agonists and competitive antagonists of the human pregnane X receptor. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 2 | The present study addresses the effects of nelfinavir and its major and pharmacologically active metabolite nelfinavir hydroxy-tert-butylamide (M8) on PXR to elucidate the underlying molecular mechanism. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 3 | Impaired co-activator recruitment by nelfinavir, as compared to the full agonist rifampin, proved to be the underlying mechanism of both effects on PXR. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 4 | Physiological relevance of nelfinavir-dependent modulation of PXR activity was investigated in respectively treated primary human hepatocytes, which showed differential induction of PXR target genes and antagonism of rifampin-induced ABCB1 and CYP3A4 gene expression. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 5 | Physiological relevance of nelfinavir-dependent modulation of PXR activity was investigated in respectively treated primary human hepatocytes, which showed differential induction of PXR target genes and antagonism of rifampin-induced ABCB1 and CYP3A4 gene expression. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 6 | In conclusion, we elucidated here the molecular mechanism of nelfinavir interaction with PXR. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 7 | It is hypothesized that modulation of PXR activity may impact on the anticancer effects of nelfinavir. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |
| 8 | Nelfinavir anticancer activity may partially rely on modulation of PXR, which itself is discussed as a therapeutic target in cancer therapy and for the reversal of chemoresistance. | Nelfinavir | nuclear receptor subfamily 1 group I member 2 | Homo sapiens |