Louis V. LaFrance

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

Michael T. McCabe, Heidi M. Ott, Gopinath Ganji et al. · Nature · 2012 · 1.8K citations

Ezh2 Inhibition, Lymphoid Neoplasia, Hematological Malignancy +10

Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells

Bruce Grasberger, Tianbao Lu, Carsten J. Schubert et al. · Journal of Medicinal Chemistry · 2005 · 425 citations · Full text

Molecular Biology, Chemical Biology, Pharmaceutical Chemistry +20

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2

Sharad K. Verma, Xinrong Tian, Louis V. LaFrance et al. · ACS Medicinal Chemistry Letters · 2012 · 373 citations · Full text

Histone Modifications, Drug Discovery Program, Engineering +18

1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2–p53 interaction: discovery and SAR

Daniel J. Parks, Louis V. LaFrance, Raul R. Calvo et al. · Bioorganic & Medicinal Chemistry Letters · 2004 · 166 citations

Molecular Pharmacology, Drug Target, Small Molecule Antagonists +11

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation <i>in vitro</i> and sensitize tumors to doxorubicin <i>in vivo</i>

Holly K. Koblish, Shuyuan Zhao, Carol F. Franks et al. · Molecular Cancer Therapeutics · 2006 · 162 citations · Full text

P53 Interaction, Chemoprevention Strategy, P53 Complex +18