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Endothelin Receptors
The endothelin family consists of highly potent vasoconstrictive peptides. Three endogenous isoforms are known to exist - ET-1, ET-2 and ET-3. Due to their physiological role as vasoactive peptides, endothelins have been linked to certain cardiac, vascular and renal diseases; endothelin antagonists may therefore play an important role in the treatment of these conditions. Two distinct endothelin receptors have so far been cloned in mammals, classified as ETA and ETB receptors.
Endothelin Receptor Target Files
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Endothelin receptors are widely expressed in all tissues. They are also localized to non-vascular structures including epithelial cells, glia and neurons. The principal physiological role of endothelin receptors is the maintenance of vascular tone. They also have comitogenic activity, potentiating the effects of other growth factors such as PDGF.
| Receptor Subtype | ETA Receptors | ETB Receptors |
|---|
| Transduction Mechanism | 7-TM, ↑ PI turnover → ↑ Ca2+i.c., ↑ Ca2+ influx | 7-TM, ↑ PI turnover → ↑ Ca2+i.c., ↑ Ca2+ influx |
| Primary Locations | Vascular smooth muscle | Vascular endothelial cells |
| Tissue Functions | Vasoconstriction, positive ionotrope, cell proliferation | Vasodilatation, bronchoconstriction, vasoconstriction, cell proliferation |
| Endogenous Ligand Potency | ET-1 = ET-2 > ET-3 | ET-1 = ET-2 = ET-3 |
| Key Compounds | Ki Values (nM) |
|---|
| Selective ETB Agonists |
IRL-1620 (1196) Sarafotoxin S6c (1175) BQ-3020 (1189) [Ala1,3,11,15]-Endothelin (1197) |
1190 2800 970 2200* |
0.016 0.29 0.18 0.33* |
| ETA Antagonists |
BQ-123 (1188) FR 139317 (1210) BMS 182874 (1441) Sulfisoxazole (0731) CI 1020 (2942) |
1.4 1 48 600* 0.3* |
1500 7300 > 50000 2200* 480* |
* IC50 values
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7-TM Receptor Signaling
Written by T. Kenakin et al
'Seven Transmembrane Receptor Signaling' highlights the multiple behaviors of 7-TMs including G-protein-dependent and -independent signaling as well as the concept of collateral efficacy
VEGF Pathway & Anti-Angiogenic Therapy
Written by N. Ferrara & Y. Crawford
A summary of antiangiogenic therapies targeting the VEGF pathway and the mechanisms of therapy resistance.
Gut Hormones and the Regulation of Appetite
Written by V.J. Taylor et al
'Gut Hormones and the Regulation of Appetite' summarizes the neuropeptide modulators and gut hormones that influence appetite
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