LITERATURE · PEER REVIEWED

Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity

Nature Communications · 2021 · Peer reviewed

COMPLETE CITATION

Citation and identifiers

Rogawski DS, et al.. “Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity.” Nature Communications. 12:2792 · doi:10.1038/s41467-021-23152-6.

PubMed ID
33990599

RESEARCH QUESTION

Can first-in-class chemical probes inhibit ASH1L catalytic activity and produce anti-leukemic effects in leukemia models?

The study establishes catalytic inhibition in leukemia models, a direction that does not supply a treatment rationale for an ASH1L reduced-dosage neurodevelopmental disorder.

INTERPRETATION BOUNDARY

Read the finding and limit together.

What this study supports

Develops chemical probes that inhibit ASH1L catalytic activity in leukemia models.

What it cannot establish

ASH1L-related NDD is primarily a reduced-dosage disorder; an ASH1L inhibitor is not a therapeutic rationale for haploinsufficiency.

OPEN THE STUDY