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Ailanthone targets p23 to overcome MDV3100 resistance in castration-resistant prostate cancer
The small molecule Ailanthone (AIL) is identified as a potent inhibitor of both full-length AR ( AR-FL) and constitutively active truncated AR splice variants (AR-Vs) and is a potential candidate for the treatment of CRPC.
Evaluation of the inhibition potential of plumbagin against cytochrome P450 using LC-MS/MS and cocktail approach
Plumbagin presented non-time-dependent inhibition of CYP activities in both human and rat liver and the relatively low Ki values of plumbagin in humans would have a high potential to cause the toxicity and drug interactions involving CYP enzymes.
Reprogramming immunosuppressive myeloid cells facilitates immunotherapy for colorectal cancer
It is demonstrated that inhibition of EP4‐expressing IMCs may offer a potential strategy for enhancing the efficacy of immunotherapy for colorectal cancer.
Design and optimization of novel hydroxamate-based histone deacetylase inhibitors of Bis-substituted aromatic amides bearing potent activities against tumor growth and metastasis.
Compound 11b, one of the most potent leads, exhibited nanomolar IC50 values toward inhibition of class I and IIb HDACs as well as sub-micromolar activity against proliferation and migration of breast cancer cells in vitro, and significantly suppressed tumor growth in a breast tumor xenograft mouse model.