Leirdal Marianne, Sioud Mouldy
Avdeling for immunologi Gruppe for molekylaer medisin Institutt for Kreftforskning Det Norske Radiumhospital Montebello 0310 Oslo.
Tidsskr Nor Laegeforen. 2002 Jan 20;122(2):178-82.
Experimental evidence indicates that various intracellular signalling cascades are altered in tumour cells. Among these, the receptor tyrosine kinase ras-ERK signalling pathway was found to be constitutively active in a significant percentage of human tumours; hence, considerable effort has been directed at finding compounds that inhibit its activation.
We review the recent progress in establishing novel approaches to interference with the constitutive activation of the receptor tyrosine kinase ras-ERK signalling pathway in cancer.
Inhibition of the receptor tyrosine kinase ras-ERK signalling pathway activation by various novel agents (e.g. small molecule tyrosine kinase inhibitors, antibodies, FTase inhibitors, SH2/SH3 directed agents, antisense, ribozymes) impaired tumour growth. Some of the developed agents have been tested in clinical trials; promising results were obtained.
Inactivation of the receptor tyrosine kinase ras-ERK signalling pathway by small molecular inhibitors has confirmed its involvement in tumour growth. Thus, molecular and/or pharmacological modulation of the components that are critically involved in the constitutive activation of this pathway are expected to improve the treatment of human malignancies.
