Title : Proof of target for SU11654: inhibition of KIT phosphorylation in canine mast cell tumors.

Pub. Date : 2003 Nov 15

PMID : 14654558






6 Functional Relationships(s)
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1 Proof of target for SU11654: inhibition of KIT phosphorylation in canine mast cell tumors. toceranib phosphate KIT proto-oncogene, receptor tyrosine kinase Canis lupus familiaris
2 PURPOSE: The purpose of this study was to evaluate the effect of the receptor tyrosine kinase inhibitor SU11654 on the activity of its molecular target KIT in canine mast cell tumors (MCT) and correlate target inhibition with mutational status of the c-kit juxtamembrane domain and SU11654 plasma concentration. toceranib phosphate KIT proto-oncogene, receptor tyrosine kinase Canis lupus familiaris
3 PURPOSE: The purpose of this study was to evaluate the effect of the receptor tyrosine kinase inhibitor SU11654 on the activity of its molecular target KIT in canine mast cell tumors (MCT) and correlate target inhibition with mutational status of the c-kit juxtamembrane domain and SU11654 plasma concentration. toceranib phosphate KIT proto-oncogene, receptor tyrosine kinase Canis lupus familiaris
4 Of these, eight MCTs showed reduced levels of phosphorylated KIT relative to total KIT after treatment with SU11654, compared with pretreatment biopsies. toceranib phosphate KIT proto-oncogene, receptor tyrosine kinase Canis lupus familiaris
5 Phosphorylated ERK1/2 was modulated in seven tumors; this did not correlate with inhibition of KIT phosphorylation CONCLUSION: SU11654 treatment at the efficacious dose results in inhibition of KIT phosphorylation in canine MCTs. toceranib phosphate mitogen-activated protein kinase 1 Canis lupus familiaris
6 Phosphorylated ERK1/2 was modulated in seven tumors; this did not correlate with inhibition of KIT phosphorylation CONCLUSION: SU11654 treatment at the efficacious dose results in inhibition of KIT phosphorylation in canine MCTs. toceranib phosphate KIT proto-oncogene, receptor tyrosine kinase Canis lupus familiaris