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IKK-α selective compound_Prostate Cancer
CRUK
Small molecule
Oncology
Hit To Lead or Lead Optimization
Reports suggest intestinal and liver toxicity has been an issue in clinical trials of IKKβ inhibitors. Given the growing evidence that IKKα has an important role in a number of cancers, the development of selective IKKα inhibitors is an attractive approach and selectivity over IKKβ will facilitate the use of such compounds clinically. Recent data has indicated that Lymphotoxin B, which activates the alternative NF-κβ pathway via IKKα, is an important driver of castrate resistant prostate cancer and may stimulate tumour progression/proliferation following androgen deprivation therapy.