Kinases' role in Alzheimer's .
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ActivX has launched a new profiling platform, which the company claims allows the functional analysis of twice the number of protein kinases than competing systems.
The KiNativ platform has been launched to address the problem of designing safe and effective kinase inhibitors by allowing the screening of over 450 kinases. The technique will find applications in drug target discovery, lead optimisation, toxicology and clinical development. Protein kinases represent the largest family of mammalian enzymes and regulate cellular signalling pathways by modifying the activity of specific proteins by phosphorylation. There are over 500 human protein kinases which all share striking structural similarities.
The kinase inhibitor market has been predicted by Pharmaprojects to grow to $58.6bn by 2010, with GlaxoSmithKline's Tykerb (lapatinib) the latest inhibitor to have been approved by the US Food and Drug Administration (FDA).
While the majority of kinase inhibitors such as Tykerb, AstraZeneca's Iressa (gefitinib) and Bristol-Myers Squibb's Sprycel (dasatinib) all focus on various different cancer indications, other drug candidates have targeted kinases' role in Alzheimer's, diabetes and arthritis.
The new platform uses biotinylated acyl phosphates of ATP or ADP that irreversibly react with the kinases. The labelled fragments can then be sequenced and analysed by LC-MS/MS (liquid chromatography - tandem mass spectrometry). This allows not only the determination of which kinases are present in the biological sample and their relative abundance, but also competition studies between probes and inhibitors to determine inhibitor potency.
Alzheimer's Donation
Donate Online Now
.
ActivX has launched a new profiling platform, which the company claims allows the functional analysis of twice the number of protein kinases than competing systems.
The KiNativ platform has been launched to address the problem of designing safe and effective kinase inhibitors by allowing the screening of over 450 kinases. The technique will find applications in drug target discovery, lead optimisation, toxicology and clinical development. Protein kinases represent the largest family of mammalian enzymes and regulate cellular signalling pathways by modifying the activity of specific proteins by phosphorylation. There are over 500 human protein kinases which all share striking structural similarities.
The kinase inhibitor market has been predicted by Pharmaprojects to grow to $58.6bn by 2010, with GlaxoSmithKline's Tykerb (lapatinib) the latest inhibitor to have been approved by the US Food and Drug Administration (FDA).
While the majority of kinase inhibitors such as Tykerb, AstraZeneca's Iressa (gefitinib) and Bristol-Myers Squibb's Sprycel (dasatinib) all focus on various different cancer indications, other drug candidates have targeted kinases' role in Alzheimer's, diabetes and arthritis.
The new platform uses biotinylated acyl phosphates of ATP or ADP that irreversibly react with the kinases. The labelled fragments can then be sequenced and analysed by LC-MS/MS (liquid chromatography - tandem mass spectrometry). This allows not only the determination of which kinases are present in the biological sample and their relative abundance, but also competition studies between probes and inhibitors to determine inhibitor potency.
posted by Valery Yermalitsky at
6:24 AM
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