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β2-Adrenoceptor Phosphorylation Assays

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OD signals in pS355/pS356-β2 Phosphorylation Assay
pS355/pS356-β2 Phosphorylation Assay Kit
The pS355/pS356-β2 Phosphorylation Assay Kit allows determination of ß2 Phosphorylation in 96-well plates without the need for Western blot analysis.
$ 600.00 *
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OD signals in pT360/pS364-β2 Phosphorylation Assay
pT360/pS364-β2 Phosphorylation Assay Kit
The pS355/pS356-β2 Phosphorylation Assay Kit allows determination of ß2 Phosphorylation in 96-well plates without the need for Western blot analysis.
$ 600.00 *

2

The β2-adrenoceptor is responsible for relaxation of vascular, uterine, and airway smooth muscle. The β2-adrenoceptor is much less sensitive to noradrenaline then to adrenaline. Many potent and selective β2-adrenoceptor agonists have been developed, which are used in the treatment of asthma. β2-adrenoceptor desensitization, β-arrestin recruitment and internalization are regulated by phosphorylation of carboxyl-terminal serine355/serine356 (pS355/pS356-ß2) and threonine360/serine364 (pT360/pS364-ß2) residues. Agonist-induced phosphorylation of S355/S356 is predominantly mediated by GRK5/6, whereas phosphorylation of T360/S364 is predominantly mediated by GRK2/3. This nomenclature refers to the human β2. For more information on β2-adrenoceptor pharmacology please refer to the IUPHAR database. For further reading refer to:

Nobles KN, Xiao K, Ahn S, Shukla AK, Lam CM, Rajagopal S, Strachan RT, Huang TY, Bressler EA, Hara MR, Shenoy SK, Gygi SP, Lefkowitz RJ. Distinct phosphorylation sites on the β(2)-adrenergic receptor establish a barcode that encodes differential functions of β-arrestin. Sci Signal. 2011 Aug 9;4(185):ra51. doi: 10.1126/scisignal.2001707. PMID: 21868357; PMCID: PMC3415961.

Kobilka BK. Structural insights into adrenergic receptor function and pharmacology. Trends Pharmacol Sci. 2011 Apr;32(4):213-8. doi: 10.1016/j.tips.2011.02.005. Epub 2011 Mar 15. PMID: 21414670; PMCID: PMC3090711.

Benkel T, Zimmermann M, Zeiner J, Bravo S, Merten N, Lim VJY, Matthees ESF, Drube J, Miess-Tanneberg E, Malan D, Szpakowska M, Monteleone S, Grimes J, Koszegi Z, Lanoiselée Y, O'Brien S, Pavlaki N, Dobberstein N, Inoue A, Nikolaev V, Calebiro D, Chevigné A, Sasse P, Schulz S, Hoffmann C, Kolb P, Waldhoer M, Simon K, Gomeza J, Kostenis E. How Carvedilol activates β2-adrenoceptors. Nat Commun. 2022 Nov 19;13(1):7109. doi: 10.1038/s41467-022-34765-w. PMID: 36402762; PMCID: PMC9675828.

Burghi V, Paradis JS, Officer A, Adame-Garcia SR, Wu X, Matthees ESF, Barsi-Rhyne B, Ramms DJ, Clubb L, Acosta M, Tamayo P, Bouvier M, Inoue A, von Zastrow
M, Hoffmann C, Gutkind JS. Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by
β2-adrenergic receptor. J Biol Chem. 2023 Nov;299(11):105293. doi:10.1016/j.jbc.2023.105293. Epub 2023 Sep 27. PMID: 37774973; PMCID: PMC10641165.

Radoux-Mergault A, Oberhauser L, Aureli S, Gervasio FL, Stoeber M.Subcellular location defines GPCR signal transduction. Sci Adv. 2023 Apr 21;9(16):eadf6059. doi: 10.1126/sciadv.adf6059. Epub 2023 Apr 19. PMID: 37075112; PMCID: PMC10115417.

The β2-adrenoceptor is responsible for relaxation of vascular, uterine, and airway smooth muscle. The β2-adrenoceptor is much less sensitive to noradrenaline then to adrenaline. Many potent... read more »
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β2-Adrenoceptor Phosphorylation Assays

2

The β2-adrenoceptor is responsible for relaxation of vascular, uterine, and airway smooth muscle. The β2-adrenoceptor is much less sensitive to noradrenaline then to adrenaline. Many potent and selective β2-adrenoceptor agonists have been developed, which are used in the treatment of asthma. β2-adrenoceptor desensitization, β-arrestin recruitment and internalization are regulated by phosphorylation of carboxyl-terminal serine355/serine356 (pS355/pS356-ß2) and threonine360/serine364 (pT360/pS364-ß2) residues. Agonist-induced phosphorylation of S355/S356 is predominantly mediated by GRK5/6, whereas phosphorylation of T360/S364 is predominantly mediated by GRK2/3. This nomenclature refers to the human β2. For more information on β2-adrenoceptor pharmacology please refer to the IUPHAR database. For further reading refer to:

Nobles KN, Xiao K, Ahn S, Shukla AK, Lam CM, Rajagopal S, Strachan RT, Huang TY, Bressler EA, Hara MR, Shenoy SK, Gygi SP, Lefkowitz RJ. Distinct phosphorylation sites on the β(2)-adrenergic receptor establish a barcode that encodes differential functions of β-arrestin. Sci Signal. 2011 Aug 9;4(185):ra51. doi: 10.1126/scisignal.2001707. PMID: 21868357; PMCID: PMC3415961.

Kobilka BK. Structural insights into adrenergic receptor function and pharmacology. Trends Pharmacol Sci. 2011 Apr;32(4):213-8. doi: 10.1016/j.tips.2011.02.005. Epub 2011 Mar 15. PMID: 21414670; PMCID: PMC3090711.

Benkel T, Zimmermann M, Zeiner J, Bravo S, Merten N, Lim VJY, Matthees ESF, Drube J, Miess-Tanneberg E, Malan D, Szpakowska M, Monteleone S, Grimes J, Koszegi Z, Lanoiselée Y, O'Brien S, Pavlaki N, Dobberstein N, Inoue A, Nikolaev V, Calebiro D, Chevigné A, Sasse P, Schulz S, Hoffmann C, Kolb P, Waldhoer M, Simon K, Gomeza J, Kostenis E. How Carvedilol activates β2-adrenoceptors. Nat Commun. 2022 Nov 19;13(1):7109. doi: 10.1038/s41467-022-34765-w. PMID: 36402762; PMCID: PMC9675828.

Burghi V, Paradis JS, Officer A, Adame-Garcia SR, Wu X, Matthees ESF, Barsi-Rhyne B, Ramms DJ, Clubb L, Acosta M, Tamayo P, Bouvier M, Inoue A, von Zastrow
M, Hoffmann C, Gutkind JS. Gαs is dispensable for β-arrestin coupling but dictates GRK selectivity and is predominant for gene expression regulation by
β2-adrenergic receptor. J Biol Chem. 2023 Nov;299(11):105293. doi:10.1016/j.jbc.2023.105293. Epub 2023 Sep 27. PMID: 37774973; PMCID: PMC10641165.

Radoux-Mergault A, Oberhauser L, Aureli S, Gervasio FL, Stoeber M.Subcellular location defines GPCR signal transduction. Sci Adv. 2023 Apr 21;9(16):eadf6059. doi: 10.1126/sciadv.adf6059. Epub 2023 Apr 19. PMID: 37075112; PMCID: PMC10115417.

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