Anti-ET-A

Anti-ET-A

Product#:

AER-001

Sizes:

50 ml

0.2 ml

Host:

Rabbit.

Epitope:

Peptide (C)NHNT ERSSH KDSMN, corresponding to amino acid residues 413-426 of rat ET-A (Accession P26684).

Putative epitope location:

Intracellular, C-terminus.

Homology:

Human, swine, bovine -13/14 residues identical; chicken - 12/14 residues identical.

Reactivity Confirmed:

Rat.

Applications:

Western Blotting:

Western blotting of rat brain membranes: 1.  Anti-ET-A antibody (1:200). 2.  Anti-ET-A antibody, preincubated with the control peptide antigen.

Immunohistochemistry:

Immunohistochemical staining of rat cerebellum using Anti-ET-A antibody (#AER-001) (A), or Anti-ET-A antibody preincubated with the control peptide antigen (B).  Counterstained with cresyl violet.  The specific staining is black.

References:

1. Davenport, A.P. (2002) Pharmacol. Rev. 54, 219.

2. Boivin, B. et al. (2003) J. Biol.Chem. 278, 29153.

3. Grant, K. et al. (2003) Br. J. Cancer. 88, 163.

4. Asham, E. et al. (2001) Br. J. Cancer. 85, 1759.

5. Kopetz, E.S. et al. (2002) Invest. New Drugs. 20, 173.

6. Rosano, L. et al. (2003) Am. J. Pathol. 163, 753.

7. Rosano, L. et al. (2003) Cancer Res. 63, 2447.

8. Wulfing, P. et al. (2003) Clin. Cancer Res. 9, 4125.

9. Nelson, J.B. (2003) J. Urol. 170, S65.

The endothelin system is comprised of three active peptides, ET-1, 2, and 3, which are considered to be very powerful vasoconstrictive substances. In humans, endothelins mediate their actions via two specific G-Protein Coupled Receptors, ET_AR and ET_BR. Both ET_AR and ET_BR are present in heart and in human myocardium at similar levels.^1,2

The endothelin receptors differ in their ligand specificity. While ET_AR has varying affinities for the endothelin isoforms (ET-1 >ET-2>ET-3), ET_BR shows no selective affinity.^2,3 Subsequent studies have demonstrated the presence of endothelins in vascular as well as in non-vascular cells and tissues, having multiple biological activities.

Currently, there is increasing evidence that ET-1 may modulate mitogenesis, apoptosis, angiogenesis tumor invasion and the development of metastases.³

Overexpression of ET-1 and ET_AR was reported in different malignancies including prostate cancer human Kaposiî–¸ sarcoma, ovarian and breast carcinomas.^4-9

In breast carcinomas overexpression of ET-1 and ET_A receptors correlated with parameters that characterize aggressive types of breast cancer¹⁵ suggesting that analysis of ET_AR expression might be used as a diagnostic marker for evaluating the progression of the disease and effectiveness of treatment. These and other findings have made ET receptors, and especially ET_AR, promising therapeutic targets for pharmacological intervention.