Abstract:Introduction: Gain-of-function mutations in the ErbB4 receptor tyrosine kinase have been found in a significant fraction of melanoma cell lines that are dependent on ErbB4 for proliferation. However, there is a scarcity of therapeutics for treating these ErbB4-dependent tumors. Consequently, we have developed high-throughput screening assays to identify small molecule ErbB4 antagonists that may hold promise as targeted melanoma therapeutics. Our approach is based on the observation that the Q43L mutant of the … Show more
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