Overview
Prostanoid Receptor Antibody Explorer Kit (#AK-655) is a budget friendly screening package.
Compounds
Scientific Background
Prostanoids, consisting of prostaglandins (PG) and thromboxanes (Tx), are a group of molecules generated by fatty acid metabolism. Prostanoids contain a cyclopentane ring and two side chains, α and ω attached to the ring1.
Prostanoids exert their effects by activating rhodopsin-like seven transmembrane spanning G-protein coupled receptors. The prostanoid receptor subfamily is comprised of eight members: EP1 (E prostanoid receptor 1), EP2, EP3, and EP4 subtypes of the PGE receptor, PGD receptor (DP1), PGF receptor (FP), PGI receptor (IP), and TX receptor (TP)2.
In addition to structural features shared with other GPCRs, particular motifs are specifically conserved among the prostanoid receptors, suggesting they may participate in the construction of binding domains for structures common to prostanoid molecules. For example: the arginine in the seventh transmembrane domain, which is conserved in all of the prostanoid receptors, was proposed to be the binding site of the carboxyl group of prostanoid molecules by analogy to the retinal binding site, Lys-296, of rhodopsin3.
Prostanoids exert a variety of actions in various tissues and cells by interacting with their receptors and activating a signaling cascade. The most typical actions are the relaxation and contraction of various types of smooth muscles. They also modulate neuronal activity by either inhibiting or stimulating neurotransmitter release, sensitizing sensory fibers to noxious stimuli, or inducing central actions such as fever generation and sleep induction. They are involved in apoptosis, cell differentiation, and oncogenesis1.
- Narumiya, S. et al. (1999) Physiol. Rev. 79, 1193.
- Narumiya, S. and Fitzgerald, G.A. (2001) J. Clin. Invest. 108, 25.
- Breyer, R.M. et al. (2001) Annu. Rev. Pharmacol. Toxicol. 41, 661.