Henri Colyn Harry Bwanika
Publikasjoner
Targeting autophagy as a therapeutic strategy in pediatric acute lymphoblastic leukemia
In the present study, we used global proteomics, transcriptomics-based approaches and drug profiling, to identify autophagy/lysosomal pathways as valid therapeutic targets in a subgroup of pediatric ALL.
Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel
Highlights
•Report a rigorous SAMHD1 chemical probe discovery pipeline
•Identified a series of low micromolar SAMHD1 inhibitors, exemplified by TH6342
•TH6342 deterred SAMHD1 dimerization in vitro, a prerequisite for catalysis
The drug efficacy testing in 3D cultures platform identifies effective drugs for ovarian cancer patients
The 3D DET3Ct platform can rapidly define potential, clinically relevant data on efficacy of existing drugs in Ovarian Cancer for precision medicine purposes, as well as provide insights on emerging drugs and drug combinations.
The N-terminal SAM domain of the dNTPase SAMHD1 is not required for inhibition by small molecule TH6342
TH6342 is a recently reported small molecule inhibitor of SAMHD1. The binding site of TH6342 on SAMHD1 is currently unknown. In the present study we demonstrate that the N-terminal SAM domain of SAMHD1 is not required for inhibition by TH6342.