Thursday, February 13, 2014
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signal transducer (IL-6ST;
kinase (JAK); signal
transducer and activator of transcription 3 (STAT3)
In vitro studies suggest two marketed drugs could inform the
design of inhibitors that block the IL-6-CD130 interaction and help treat
cancer. Fragment-based drug design and virtual screening identified raloxifene
as potential inhibitors of the IL-6-CD130 interaction that activates JAK and
STAT3 signaling. In a CD130+ human
pancreatic cancer cell line, both drugs reduced viability at micromolar IC50
values. In an estrogen
receptor-negative human breast cancer cell line, the drugs
reduced viability at micromolar IC50 values. Ongoing work includes
optimizing the two drugs for potency against the IL-6-CD130 interaction.
Eli Lilly and Co. and Takeda
Pharmaceutical Co. Ltd. market Evista
raloxifene, a selective estrogen receptor modulator (SERM), to treat
osteoporosis and breast cancer.
Pharmaceuticals Inc. and Pfizer
Inc. market the SERM Conbriza
bazedoxifene to treat osteoporosis.
Published online Feb. 13, 2014
available for partnering
Li, H. et al. J. Med.
published online Jan. 23, 2014;
Contact: Chenglong Li, The Ohio State University, Columbus, Ohio
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