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Selective kinase inhibitors as tools for neuroscience research

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Selective kinase inhibitors as tools for neuroscience research. / Martin, K.J.; Arthur, J. Simon C.

In: Neuropharmacology, Vol. 63, No. 7, 12.2012, p. 1227-1237.

Research output: Contribution to journalArticle

Harvard

Martin, KJ & Arthur, JSC 2012, 'Selective kinase inhibitors as tools for neuroscience research' Neuropharmacology, vol 63, no. 7, pp. 1227-1237., 10.1016/j.neuropharm.2012.07.024

APA

Martin, K. J., & Arthur, J. S. C. (2012). Selective kinase inhibitors as tools for neuroscience research. Neuropharmacology, 63(7), 1227-1237. 10.1016/j.neuropharm.2012.07.024

Vancouver

Martin KJ, Arthur JSC. Selective kinase inhibitors as tools for neuroscience research. Neuropharmacology. 2012 Dec;63(7):1227-1237. Available from: 10.1016/j.neuropharm.2012.07.024

Author

Martin, K.J.; Arthur, J. Simon C. / Selective kinase inhibitors as tools for neuroscience research.

In: Neuropharmacology, Vol. 63, No. 7, 12.2012, p. 1227-1237.

Research output: Contribution to journalArticle

Bibtex - Download

@article{d680d011946f4bd48775c24f475cb45e,
title = "Selective kinase inhibitors as tools for neuroscience research",
author = "K.J. Martin and Arthur, {J. Simon C.}",
year = "2012",
doi = "10.1016/j.neuropharm.2012.07.024",
volume = "63",
number = "7",
pages = "1227--1237",
journal = "Neuropharmacology",
issn = "0028-3908",

}

RIS (suitable for import to EndNote) - Download

TY - JOUR

T1 - Selective kinase inhibitors as tools for neuroscience research

A1 - Martin,K.J.

A1 - Arthur,J. Simon C.

AU - Martin,K.J.

AU - Arthur,J. Simon C.

PY - 2012/12

Y1 - 2012/12

N2 - Signal transduction cascades, including the MAPK, PI3 kinase, Ca and PKC pathways, play important roles in neurons downstream of multiple signals including neurotrophins and neurotransmitters. Small molecule kinase inhibitors that block these pathways provide a powerful way of studying the in vivo or cellular roles of these signaling systems. Over the last 15 years there has been a major effort by the pharmaceutical industry to develop kinase inhibitors as potential drugs for a variety of diseases including cancer and auto-immunity. As a result of this there are now many compounds available that can be used as research tools. One major drawback is however that many of these compounds are not truly selective for a single kinase, and therefore the possibility that their cellular effects may be due to an off target activity must be considered. This problem has been brought into sharp relief by modern in vitro screening methods that allow an inhibitor to be screened against a significant proportion of the kinome. In this review we discuss the advantages and problems with the use of kinase inhibitors as research tools and describe some of the available compounds that target pathways important to neurons. © 2012 Elsevier Ltd. All rights reserved.

AB - Signal transduction cascades, including the MAPK, PI3 kinase, Ca and PKC pathways, play important roles in neurons downstream of multiple signals including neurotrophins and neurotransmitters. Small molecule kinase inhibitors that block these pathways provide a powerful way of studying the in vivo or cellular roles of these signaling systems. Over the last 15 years there has been a major effort by the pharmaceutical industry to develop kinase inhibitors as potential drugs for a variety of diseases including cancer and auto-immunity. As a result of this there are now many compounds available that can be used as research tools. One major drawback is however that many of these compounds are not truly selective for a single kinase, and therefore the possibility that their cellular effects may be due to an off target activity must be considered. This problem has been brought into sharp relief by modern in vitro screening methods that allow an inhibitor to be screened against a significant proportion of the kinome. In this review we discuss the advantages and problems with the use of kinase inhibitors as research tools and describe some of the available compounds that target pathways important to neurons. © 2012 Elsevier Ltd. All rights reserved.

UR - http://www.scopus.com/inward/record.url?scp=84866038981&partnerID=8YFLogxK

U2 - 10.1016/j.neuropharm.2012.07.024

DO - 10.1016/j.neuropharm.2012.07.024

M1 - Article

JO - Neuropharmacology

JF - Neuropharmacology

SN - 0028-3908

IS - 7

VL - 63

SP - 1227

EP - 1237

ER -

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