The Screen to Lead Program (SLP) supports academic laboratories for drug discovery support specifically directed towards medicinal chemistry and/or drug target screening in hematological malignancies. LLS recognizes a significant need for investigators to receive resources for high-throughput screening and/or optimization of small molecules into drug-like compounds suitable for in vivo testing in a disease-relevant model.
Ash1L represents a novel attractive therapeutic target in AML. In this project, we propose to screen for new small molecule inhibitors of ASH1L to block its catalytic activity. We will pursue high throughput screening followed by chemistry optimization and biological evaluations of selected compounds in AML models. This project should result in new targeted therapy for AML and possibly other tumors associated with overexpression of ASH1L.
Jolanta Grembecka, PhD
University of Michigan
Screening for inhibitors of ASH1L as a new treatment for Acute Myeloid Leukemia