Ligand-dependent regulation

Sex steroid receptors are members of the steroid hormone receptor (SHR) family that ligand-dependently regulate functions of the sexual organs. Sex steroid receptors are the androgen receptor [1] (AR), the estrogen receptor a [2] and (3 [3] (ERa, ER 3), and the progesterone receptor [4] (PR). 

Abruzzese, R.V., D. Godin, M. Burcin, V. Mehta, M. French, Y. Li, B.W. O Malley, and J.L. Nordstrom, Ligand-dependent regulation of plasmid-based transgene expression in vivo. Hum Gene Ther, 1999. 10(9) 1499-507. 

Ronne H, Ocklind C, Wiman K, Rask L, Obrink B, Peterson PA. Ligand dependent regulation of intracellular protein transport effect of vitamin A on the secretion of retinol-binding protein. J Cell Biol 1983 96 907-10. 

Miao J, Choi SE, Seok SM, Yang L, Zuercher WJ, Xu Y Willson TM, Xu HE, Kemper JK (2011) Ligand-dependent regulation of the activity of the orphan nuclear receptor, small heterodimer partner (SHP), in the repression of bile acid biosynthetic CYP7A1 and CYP8B1 genes. Mol Endocrinol 25 1159-1169... 

Ca2+ can enter cells via voltage- or ligand-dependent channels and by capacitative entry. These three fundamental mechanisms of regulated calcium ion entry across the plasma membrane involve, respectively, voltage-dependent Ca2+ channels, ligand-gated Ca2+ channels and capacitative Ca2+ entry associated with phospholipase C-coupled receptors. 

PPAR is a nuclear receptor-transcription factor and is ligand-dependent and expressed in several tissues. It is initially involved in adipocyte differentiation and fatty acid synthesis. Fatty acid and eicosanoids bind to PPAR and regulate transcription. PPAR activation inhibits monocyte differentiation and expression of several pro-inflammatory genes such as iNOS, TNF, etc. PPAR activation inhibits tumor cell proliferation (epithelial, colon, prostate). PPAR is involved in angiogenesis. 

PCA can be used for quantitative pharmocological analysis of protein-protein and protein—small molecule binding in vivo. However, if the mDHFR domains are swapped for complementary fragments of another enzyme, then perhaps a PCA with ligand-dependent interacting domains such as FKBP and FRB can be used to regulate the activity of this enzyme. 

Vitamin A acts to regulate gene expression through interactions with its specific ligand-dependent transcription factors, which are sometimes referred to as nuclear receptors (Chambon, 1994 Chawla et al., 2001 Mangels-... 

Fujita Aand Mitsuhashi T (1999) Differential regulation of ligand-dependent and ligand-independent functions of the mouse retinoid X receptor beta by alternative splicing. Biochemical and Biophysical Research Communications 255, 625-30. 

Kawada T, Kamei Y, and Sugimoto E (1996) The possibility of active form of vitamins A and Das suppressors on adipocyte development via ligand-dependent transcriptional regulators. International Journal of Obesity and Related Metabolic Disorders 20(Suppl 3),S52-7. 

---