… Evalaution of Enzyme Inhibitors in Drug Discovery by Robert A. Copeland has been an
invaluable guide to the community of scientists devoted to finding new drugs in all therapeutic …

Much of drug discovery today is predicated on the concept of selective targeting of particular
bioactive macromolecules by low-molecular-mass drugs. The binding of drugs to their …

Chemical probes are powerful reagents with increasing impacts on biomedical research.
However, probes of poor quality or that are used incorrectly generate misleading results. To …

The compound U0126 (1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene) was
identified as an inhibitor of AP-1 transactivation in a cell-based reporter assay. U0126 was …

… The right of author Robert A. Copeland to be identified as the author of this work has been
… I thank June Davis, Petra Marchand, Diane Lombardo, Robert Lombardo, John Giannaras, …

The drug–target residence time model was first introduced in 2006 and has been broadly
adopted across the chemical biology, biotechnology and pharmaceutical communities. While …

Mislocated enzymatic activity of DOT1L has been proposed as a driver of leukemogenesis
in mixed lineage leukemia (MLL). The characterization of EPZ004777, a potent, selective …

EZH2 catalyzes trimethylation of histone H3 lysine 27 (H3K27). Point mutations of EZH2 at
Tyr641 and Ala677 occur in subpopulations of non-Hodgkin's lymphoma, where they drive …

EZH2, the catalytic subunit of the PRC2 complex, catalyzes the mono- through trimethylation
of lysine 27 on histone H3 (H3K27). Histone H3K27 trimethylation is a mechanism for …

Inactivation of the switch/sucrose nonfermentable complex component SMARCB1 is extremely
prevalent in pediatric malignant rhabdoid tumors (MRTs) or atypical teratoid rhabdoid …