Lecture 77 Flashcards
Ligand Binding Domain
Low AA identity. Also involved in receptor dimerization, interaction with other proteins, and nuclear localization
DNA binding domain
High AA identity.
How is AF-1 (transcriptional activation function 1) activated?
Phosphorylation
How is AF-2 (transcriptional activation function 2) activated?
Ligand binding
Name five types of type I nuclear receptors.
Estrogen (ER) Androgen (AR) Glucocorticoid (GR) Progesterone (PR) Mineralocorticoid (MR)
Name seven types of type II nuclear receptors
Thyroid hormone (TR) Vitamin D (VDR) Retinoic acid (RAR) Retinoid X (RXR) Peroxisome proliferator-activated (PPAR) Liver X (LXR) Farnesoid X (FXR)
What is the ligand for RXR?
9cisRA
What is the ligand for PPARa?
Fibrates
What is the ligand for PPARg?
Glitazones
What is the ligand for PXR?
Xenobiotics
What is the ligand for LXR?
Oxysterols
What is the ligand for FXR?
Bile Acids
What is the ligand for VDR?
1,25-dihydroxy vitamin D3
What is the ligand for RAR?
All-trans retinoic acid
What are characteristics of Type I ligands?
- All are derived from cholesterol
- High specificity and affinity
- pM to nM concentrations in serum