Activation of IP3 receptors by synthetic bisphosphate ligands

Kana M. Sureshan, Andrew M. Riley, Ana M. Rossi, Stephen C. Tovey, Skarlatos G. Dedos, Colin W. Taylor, Barry V. L. Potter

Research output: Contribution to journalArticle

22 Citations (Scopus)

Abstract

Ca2+ release by D-myo-inositol 1,4,5-trisphosphate receptors (IP(3)Rs) is widely considered to require the vicinal 4,5-bisphosphate motif of IP3, with P-5 and P-4 engaging the alpha and beta domains of the binding site; using synthesis and mutagenesis we show that the adenine of synthetic glyconucleotides, through an interaction with Arg504, can replace the interaction of either P-1 or P-5 with the alpha-domain producing, respectively, the most potent bisphosphate agonist yet synthesised and the first agonist of IP3R without a vicinal bisphosphate motif; this will stimulate new approaches to IP3R ligand design.
Original languageEnglish
Pages (from-to)1204-1206
JournalChemical Communications
Volume2009
Issue number10
Early online date4 Feb 2009
DOIs
Publication statusPublished - 14 Mar 2009

Fingerprint

Artificial Receptors
Inositol 1,4,5-Trisphosphate Receptors
Mutagenesis
Inositol 1,4,5-Trisphosphate
Adenine
Binding sites
Chemical activation
Binding Sites
Ligands

Cite this

Sureshan, K. M., Riley, A. M., Rossi, A. M., Tovey, S. C., Dedos, S. G., Taylor, C. W., & Potter, B. V. L. (2009). Activation of IP3 receptors by synthetic bisphosphate ligands. Chemical Communications, 2009(10), 1204-1206. https://doi.org/10.1039/b819328b

Activation of IP3 receptors by synthetic bisphosphate ligands. / Sureshan, Kana M.; Riley, Andrew M.; Rossi, Ana M.; Tovey, Stephen C.; Dedos, Skarlatos G.; Taylor, Colin W.; Potter, Barry V. L.

In: Chemical Communications, Vol. 2009, No. 10, 14.03.2009, p. 1204-1206.

Research output: Contribution to journalArticle

Sureshan, KM, Riley, AM, Rossi, AM, Tovey, SC, Dedos, SG, Taylor, CW & Potter, BVL 2009, 'Activation of IP3 receptors by synthetic bisphosphate ligands', Chemical Communications, vol. 2009, no. 10, pp. 1204-1206. https://doi.org/10.1039/b819328b
Sureshan KM, Riley AM, Rossi AM, Tovey SC, Dedos SG, Taylor CW et al. Activation of IP3 receptors by synthetic bisphosphate ligands. Chemical Communications. 2009 Mar 14;2009(10):1204-1206. https://doi.org/10.1039/b819328b
Sureshan, Kana M. ; Riley, Andrew M. ; Rossi, Ana M. ; Tovey, Stephen C. ; Dedos, Skarlatos G. ; Taylor, Colin W. ; Potter, Barry V. L. / Activation of IP3 receptors by synthetic bisphosphate ligands. In: Chemical Communications. 2009 ; Vol. 2009, No. 10. pp. 1204-1206.
@article{d7a374de805a43d98d9e6768d100d34d,
title = "Activation of IP3 receptors by synthetic bisphosphate ligands",
abstract = "Ca2+ release by D-myo-inositol 1,4,5-trisphosphate receptors (IP(3)Rs) is widely considered to require the vicinal 4,5-bisphosphate motif of IP3, with P-5 and P-4 engaging the alpha and beta domains of the binding site; using synthesis and mutagenesis we show that the adenine of synthetic glyconucleotides, through an interaction with Arg504, can replace the interaction of either P-1 or P-5 with the alpha-domain producing, respectively, the most potent bisphosphate agonist yet synthesised and the first agonist of IP3R without a vicinal bisphosphate motif; this will stimulate new approaches to IP3R ligand design.",
author = "Sureshan, {Kana M.} and Riley, {Andrew M.} and Rossi, {Ana M.} and Tovey, {Stephen C.} and Dedos, {Skarlatos G.} and Taylor, {Colin W.} and Potter, {Barry V. L.}",
year = "2009",
month = "3",
day = "14",
doi = "10.1039/b819328b",
language = "English",
volume = "2009",
pages = "1204--1206",
journal = "Chemical communications (Cambridge, England)",
issn = "1359-7345",
publisher = "Royal Society of Chemistry",
number = "10",

}

TY - JOUR

T1 - Activation of IP3 receptors by synthetic bisphosphate ligands

AU - Sureshan, Kana M.

AU - Riley, Andrew M.

AU - Rossi, Ana M.

AU - Tovey, Stephen C.

AU - Dedos, Skarlatos G.

AU - Taylor, Colin W.

AU - Potter, Barry V. L.

PY - 2009/3/14

Y1 - 2009/3/14

N2 - Ca2+ release by D-myo-inositol 1,4,5-trisphosphate receptors (IP(3)Rs) is widely considered to require the vicinal 4,5-bisphosphate motif of IP3, with P-5 and P-4 engaging the alpha and beta domains of the binding site; using synthesis and mutagenesis we show that the adenine of synthetic glyconucleotides, through an interaction with Arg504, can replace the interaction of either P-1 or P-5 with the alpha-domain producing, respectively, the most potent bisphosphate agonist yet synthesised and the first agonist of IP3R without a vicinal bisphosphate motif; this will stimulate new approaches to IP3R ligand design.

AB - Ca2+ release by D-myo-inositol 1,4,5-trisphosphate receptors (IP(3)Rs) is widely considered to require the vicinal 4,5-bisphosphate motif of IP3, with P-5 and P-4 engaging the alpha and beta domains of the binding site; using synthesis and mutagenesis we show that the adenine of synthetic glyconucleotides, through an interaction with Arg504, can replace the interaction of either P-1 or P-5 with the alpha-domain producing, respectively, the most potent bisphosphate agonist yet synthesised and the first agonist of IP3R without a vicinal bisphosphate motif; this will stimulate new approaches to IP3R ligand design.

UR - http://www.scopus.com/inward/record.url?scp=60849109525&partnerID=8YFLogxK

UR - http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2898634/

UR - http://dx.doi.org/10.1039/b819328b

U2 - 10.1039/b819328b

DO - 10.1039/b819328b

M3 - Article

VL - 2009

SP - 1204

EP - 1206

JO - Chemical communications (Cambridge, England)

JF - Chemical communications (Cambridge, England)

SN - 1359-7345

IS - 10

ER -