Concepedia

The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia

Eytan M. Stein, Guillermo Garcia‐Manero, David A. Rizzieri, Raoul Tibes, Jesús G. Berdeja, Michael R. Savona, Mojca Jongen-Lavrenic, Jessica K. Altman, Blythe Thomson, Stephen J. Blakemore,

Blood · 2018 · 457 citations · 27 references

DOIFull text

Open access

Concepts

Abstract

Key Points Pinometostat demonstrates first evidence of DOT1L target inhibition and clinical responses in a subset of MLL-r advanced leukemia patients. The observed safety profile of pinometostat shows potential for exploration of combination therapies in leukemia.

References

27

Molecular Classification of Cancer: Class Discovery and Class Prediction by Gene Expression Monitoring

Todd R. Golub, Donna K. Slonim, Pablo Tamayo et al. · Science · 1999 · 11.6K citations

, , +16

Pretreatment cytogenetic abnormalities are predictive of induction success, cumulative incidence of relapse, and overall survival in adult patients with de novo acute myeloid leukemia: results from Cancer and Leukemia Group B (CALGB 8461)

John C. Byrd · Blood · 2002 · 1.6K citations

, , +16

Transformation from committed progenitor to leukaemia stem cell initiated by MLL–AF9

Andrei V. Krivtsov, David Twomey, Zhaohui Feng et al. · Nature · 2006 · 1.5K citations

, , +14

MLL Targets SET Domain Methyltransferase Activity to Hox Gene Promoters

Thomas A. Milne, Scott Briggs, Hugh W. Brock et al. · Molecular Cell · 2002 · 1.1K citations · Full text

, , +12

Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor

Scott R. Daigle, Edward J. Olhava, Carly A. Therkelsen et al. · Cancer Cell · 2011 · 934 citations · Full text

, , +10