Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription

M.P. Coghlan; A.A. Culbert; D.A.E. Cross; S.L. Corcoran; J.W. Yates; N.J. Pearce; O.L. Rausch; G.J. Murphy; P.S. Carter; L.R. Cox; D. Mills; M.J. Brown; David Haigh; R.W. Ward; D.G. Smith; K.J. Murray; A.D. Reith; J.C. Holder

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription

M.P. Coghlan, A.A. Culbert, D.A.E. Cross, S.L. Corcoran, J.W. Yates, N.J. Pearce, O.L. Rausch, G.J. Murphy, P.S. Carter, L.R. Cox, D. Mills, M.J. Brown, David Haigh, R.W. Ward, D.G. Smith, K.J. Murray, A.D. Reith, J.C. Holder

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759 Citations (Scopus)

Abstract

Background: Glycogen synthase kinase-3 (GSK-8) is a serine/threonine protein kinase, the activity of which is inhibited by a variety of extracellular stimuli including insulin, growth factors, cell specification factors and cell adhesion. Consequently, inhibition of GSK-3 activity has been proposed to play a role in the regulation of numerous signalling pathways that elicit pleiotropic cellular responses. This report describes the identification and characterisation of potent and selective small molecule inhibitors of GSK-3.

Original language	English
Pages (from-to)	793-803
Number of pages	11
Journal	Chemistry & Biology
Volume	7
Issue number	10
Publication status	Published - 2000

ASJC Scopus subject areas

Organic Chemistry

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Coghlan, M. P., Culbert, A. A., Cross, D. A. E., Corcoran, S. L., Yates, J. W., Pearce, N. J., Rausch, O. L., Murphy, G. J., Carter, P. S., Cox, L. R., Mills, D., Brown, M. J., Haigh, D., Ward, R. W., Smith, D. G., Murray, K. J., Reith, A. D., & Holder, J. C. (2000). Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chemistry & Biology, 7(10), 793-803.

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abstract = "Background: Glycogen synthase kinase-3 (GSK-8) is a serine/threonine protein kinase, the activity of which is inhibited by a variety of extracellular stimuli including insulin, growth factors, cell specification factors and cell adhesion. Consequently, inhibition of GSK-3 activity has been proposed to play a role in the regulation of numerous signalling pathways that elicit pleiotropic cellular responses. This report describes the identification and characterisation of potent and selective small molecule inhibitors of GSK-3.",

author = "M.P. Coghlan and A.A. Culbert and D.A.E. Cross and S.L. Corcoran and J.W. Yates and N.J. Pearce and O.L. Rausch and G.J. Murphy and P.S. Carter and L.R. Cox and D. Mills and M.J. Brown and David Haigh and R.W. Ward and D.G. Smith and K.J. Murray and A.D. Reith and J.C. Holder",

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Coghlan, MP, Culbert, AA, Cross, DAE, Corcoran, SL, Yates, JW, Pearce, NJ, Rausch, OL, Murphy, GJ, Carter, PS, Cox, LR, Mills, D, Brown, MJ, Haigh, D, Ward, RW, Smith, DG, Murray, KJ, Reith, AD & Holder, JC 2000, 'Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription', Chemistry & Biology, vol. 7, no. 10, pp. 793-803.

TY - JOUR

T1 - Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription

AU - Coghlan, M.P.

AU - Culbert, A.A.

AU - Cross, D.A.E.

AU - Corcoran, S.L.

AU - Yates, J.W.

AU - Pearce, N.J.

AU - Rausch, O.L.

AU - Murphy, G.J.

AU - Carter, P.S.

AU - Cox, L.R.

AU - Mills, D.

AU - Brown, M.J.

AU - Haigh, David

AU - Ward, R.W.

AU - Smith, D.G.

AU - Murray, K.J.

AU - Reith, A.D.

AU - Holder, J.C.

PY - 2000

Y1 - 2000

N2 - Background: Glycogen synthase kinase-3 (GSK-8) is a serine/threonine protein kinase, the activity of which is inhibited by a variety of extracellular stimuli including insulin, growth factors, cell specification factors and cell adhesion. Consequently, inhibition of GSK-3 activity has been proposed to play a role in the regulation of numerous signalling pathways that elicit pleiotropic cellular responses. This report describes the identification and characterisation of potent and selective small molecule inhibitors of GSK-3.

AB - Background: Glycogen synthase kinase-3 (GSK-8) is a serine/threonine protein kinase, the activity of which is inhibited by a variety of extracellular stimuli including insulin, growth factors, cell specification factors and cell adhesion. Consequently, inhibition of GSK-3 activity has been proposed to play a role in the regulation of numerous signalling pathways that elicit pleiotropic cellular responses. This report describes the identification and characterisation of potent and selective small molecule inhibitors of GSK-3.

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M3 - Article

VL - 7

SP - 793

EP - 803

JO - Chemistry & Biology

JF - Chemistry & Biology

SN - 1074-5521

IS - 10

ER -

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription

Abstract

ASJC Scopus subject areas

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