TCID | Name | Domain | Kingdom/Phylum | Protein(s) |
---|---|---|---|---|
9.B.208.1.1 | The Vitamin D3 Receptor, VDR of 427 aas and 0 - 1 TMS. Possibly can insert into the plasma membrane and form a large channel (see family description) (Morrill et al. 2016). It is a dimer with two transmembrane half helices (264K - N276) and 16 cholesterol binding (CRAC/CARC) domains. May function with importin-4 (TC# 1.I.1.1.3) which may also be able to form a transmembrane channel (Morrill et al. 2016). | Eukaryota |
Metazoa, Chordata | VDR of Homo sapiens |
9.B.208.1.2 | The bile acid farnesoid receptor, FXR, of 472 or 486 aas but 0 TMSs. The farnesoid X receptor is an important target for the treatment of disorders of bile acid and fatty acid metabolism in mice with nonalcoholic fatty liver disease combined with cholestasis (Liu et al. 2023). FXR, MRP-1 and SLC7A5 are new targets for the treatment of hepatocellular carcinoma (Zhang et al. 2024). SLC7A11, a key protein involved in ferroptosis, and it has been identified as a potential target for drug development. Through screening efforts, novel inhibitors of SLC7A11 have been designed with the aim of promoting ferroptosis and ultimately eliminating cancer cells. Small molecules 42711 and 27363 have been identified as lead compounds with strong inhibitory activity against SLC7A11. Further optimization resulted in the development of a new inhibitor structure (42711_11) (Zhang et al. 2024). FXR-deficiency induces ferroptosis via modulation of CBP-dependent p53 acetylation to suppress breast cancer growth and metastasis (Huang et al. 2024). FXR was first reported as a tumor promoter that enhanced the proliferation and metastasis of breast cancer cells by regulating CBP-dependent p53 K382 acetylation. FXR may serve as a therapeutic target for the treatment of breast cancer. | Eukaryota |
Metazoa, Chordata | Farnesoid receptor of Homo sapiens |
9.B.208.1.3 | Nuclear receptor subfamily 1 group I member 2, or the pregnane X recpetor, of 434 aas and 0 TMSs. It binds and is activated by a variety of endogenous and xenobiotic compounds and is a transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. It is activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones in a species-specific fashion. It is also activated by naturally occurring steroids, such as pregnenolone and progesterone (Lehmann et al. 1998; Geick et al. 2001; Watkins et al. 2003; Li et al. 2009). | Eukaryota |
Metazoa, Chordata | Pregnane X recpetor of Homo sapiens |
9.B.208.1.4 | Nuclear receptor subfamily 5 group A member 2 of 541 aas. It functions as a key regulator of cholesterol 7-alpha-hydroxylase gene (CYP7A) expression in liver and may also contribute to the regulation of pancreas-specific genes while playing important roles in embryonic development (Wang et al. 2005). | Metazoa, Chordata | ||
9.B.208.1.5 | Progesterone receptor, PGR, of 933 aas; it is a transcriptional regulatory protein responding to steroids such as progesterone. It has various isoforms of differing functions; isoform 4 increases the mitochondrial membrane potential and cellular respiration upon stimulation by progesterone (Grimm et al. 2016). | Eukaryota |
Metazoa, Chordata | PGR of Homo sapiens |
9.B.208.1.6 | Peroxisome proliferator-activated receptor alpha, PPARa or PPARα, of 468 aas. It is a ligand-activated transcription factor that is a key regulator of lipid metabolism.The expression of it structural gene is influenced by emodin (Cheng et al. 2021). | Eukaryota |
Metazoa, Chordata | PPARα of Homo sapiens |
9.B.208.1.7 | Oxysterol receptor, LXR-allpha (LXRα) of 447 aas and 0 - 2 TMSs. The effect of liver X receptor agonist TO901317 on cognitive function in APP/PS1 double transgenic mice with Alzheimer's disease and the underlying mechanism have been determined (Luo et al. 2022). Soyasapogenol C is a liver X receptor α agonist that mitigates cholesterol accumulation in diabetic kidney disease (Zhang et al. 2025). | Eukaryota |
Metazoa, Chordata | LXRα of Homo sapiens |