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Amplification of the CCNE1 locus on chromosome 19q12 is prevalent in multiple tumour types, particularly high-grade serous ovarian cancer, uterine tumours and gastro-oesophageal cancers, where high cyclin E levels are associated with genome instability, whole-genome doubling resistance to cytotoxic targeted therapies
PKMYT1 is a regulator of CDK1 phosphorylation and compelling therapeutic target for the treatment certain types DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification. To date, no selective inhibitors have been reported this kinase that would allow investigation pharmacological role PKMYT1. address need compound 1 was identified as weak inhibitor. Introduction dimethylphenol increased potency on These analogs were found exist atropisomers...
PKMYT1 is an important regulator of CDK1 phosphorylation and a compelling therapeutic target for the treatment certain types DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification. To date, no selective inhibitors have been reported this kinase that would allow investigation pharmacological role in cancer. address need we conducted focused screening effort identified compound 1 as weak inhibitor. Introduction dimethylphenol dramatically...