Zhi-Fu Tao

TL;DR: BCL-XL–selective inhibitors have the potential to enhance the efficacy of docetaxel in solid tumors and avoid the exacerbation of neutropenia observed with navitoclax, and demonstrate the translational utility of this toolkit of selective BCL-2 family inhibitors.

TL;DR: A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses and represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization.

TL;DR: In this paper, compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-APOPotic BCL-2 protein.

TL;DR: A series of MCL-1 inhibitors that emanated from a high throughput screening (HTS) hit and progressed via iterative cycles of structure-guided design exhibited subnanomolar affinity for M CL-1 and excellent selectivity over other BCL-2 family proteins as well as multiple kinases and GPCRs.

TL;DR: It is feasible to achieve a therapeutic window with 1 or more Chk1 inhibitors in potentiation of cancer therapy based on the status of the p53 pathway in a wide spectrum of tumor types, and these results indicate that it is feasible.