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1998b). These structures indicate that the RHR exhibits La Jolla, California 92093-0359 a tripartite organization. The amino-terminal 180 amino acids fold into an immunoglobulin-like domain. A short (10 amino acids) flexible linker connects this amino-Summary terminal domain to a second immunoglobulin-like domain of approximately 100 amino acids in length.(More)
KRAS and BRAF activating mutations drive tumorigenesis through constitutive activation of the MAPK pathway. As these tumours represent an area of high unmet medical need, multiple allosteric MEK inhibitors, which inhibit MAPK signalling in both genotypes, are being tested in clinical trials. Impressive single-agent activity in BRAF-mutant melanoma has been(More)
Activating mutations within the epidermal growth factor receptor (EGFR) kinase domain, commonly L858R or deletions within exon 19, increase EGFR-driven cell proliferation and survival and are correlated with impressive responses to the EGFR inhibitors erlotinib and gefitinib in nonsmall cell lung cancer patients. Approximately 60% of acquired resistance to(More)
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