Tarang Gaur, Ramulu Poddutoori, Leena Khare, Bhausaheb Bagal, Sonal Rashmi, Nikhil Patkar, Prashant Tembhare, Subramanian Pg, Dhanlaxmi Shetty, Amit Dutt, Qi Zhang, Marina Konopleva, Uwe Platzbeckar, Sudeep Gupta, Susanta Samajdar, Murali Ramchandra, Navin Khattry, Syed K Hasan
INTRODUCTION: The emergence of resistance to the highly successful BCL2-directed therapy is a major unmet need in acute myeloid leukemia (AML), an aggressive malignancy with poor survival rates. Towards identifying therapeutic options for AML patients who progress on BCL2-directed therapy, we studied a clinical-stage CDK7 inhibitor XL102, which is being evaluated in solid tumors (NCT04726332). MATERIALS AND METHODS: To determine the anti-proliferative effects of XL102, we performed experiments including time-resolved fluorescence resonance energy transfer, target occupancy, cell cycle and apoptosis-based assays...
July 29, 2023: Journal of Experimental & Clinical Cancer Research: CR