Success examples
Fast-acting chemical tools to delineate causality in transcriptional control

Jaeger M. G., Winter G. E.

Mol Cell 2021, S1097-2765(21)00125-8.

BRD9 inhibitor
DOI
PUBMED
Success examples
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface

Teng M., Ficarro S. B., Yoon H., Che J., Zhou J., Fischer E. S., Marto J. A., Zhang T., Gray N. S.

ACS Med Chem Lett. 2020, 11(6):1269-1273.

BCL6 degrader BCL6 inhibitor BCL6 degrader
DOI
PUBMED
Success examples
Suppression of the HBP Function Increases Pancreatic Cancer Cell Sensitivity to a Pan-RAS Inhibitor

Ricciardiello F., Bergamaschi L., De Vitto H., Gang Y.,Zhang T., Palorini R., Chiaradonna F.

Cells 2021, 10(2), 431.

KRAS switch I/II pocket inhibitor
DOI
PUBMED
Success examples
Small-molecule-induced polymerization triggers degradation of BCL6

Słabicki M., Yoon H., Koeppel J., Nitsch L., Roy Burman S. S., Di Genua C., Donovan K. A., Sperling A. S., Hunkeler M., Tsai J. M., Sharma R., Guirguis A., Zou C., Chudasama P., Gasser J. A., Miller P. G., Scholl C., Fröhling S., Nowak R. P., Fischer E. S., Ebert B. L.

Nature 2020, 588, 164–168.

BCL6 degrader BCL6 inhibitor BCL6 degrader
DOI
PUBMED
Success examples
In Vitro and In Vivo Behaviors of KinetiSol and Spray-Dried Amorphous Solid Dispersions of a Weakly Basic Drug and Ionic Polymer

Jermain S. V., Lowinger M. B., Ellenberger D. J., Miller D. A., Su Y., Williams III R. O.

Mol. Pharmaceutics 2020, 17, 8, 2789-2808.

CCR1 antagonist
DOI
PUBMED