A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

Helai P. Mohammad, Kimberly N. Smitheman, Chandrashekhar D. Kamat, +30

Cancer Cell

Oncogenic AgentMedicineEpigenetic ChangePharmacologyLsd1 Inhibitors +7

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27)

Michael T. McCabe, Alan P. Graves, Gopinath Ganji, +18

Proceedings of the National Academy of Sciences

Histone ModificationsEpigenetic ChangePathologyMolecular BiologyEpigenetics +18

Combinations of BRAF, MEK, and PI3K/mTOR Inhibitors Overcome Acquired Resistance to the BRAF Inhibitor GSK2118436 Dabrafenib, Mediated by <i>NRAS</i> or <i>MEK</i> Mutations

James Greger, Stephen D. Eastman, Vivian Zhang, +7

Molecular Cancer Therapeutics

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

Tara Rheault, John Stellwagen, George M. Adjabeng, +15

ACS Medicinal Chemistry Letters

B-raf-driven TumorsAntitumor ActivityHyperactive SignalingTumor BiologyMedicinal Chemistry +14

Dabrafenib; Preclinical Characterization, Increased Efficacy when Combined with Trametinib, while BRAF/MEK Tool Combination Reduced Skin Lesions

Alastair J. King, Marc R. Arnone, Maureen R. Bleam, +12

PLoS ONE

DermatologyTumor BiologySignaling PathwayReceptor Tyrosine KinasePreclinical Characterization +15

BET Inhibition Silences Expression of MYCN and BCL2 and Induces Cytotoxicity in Neuroblastoma Tumor Models

Anastasia Wyce, Gopinath Ganji, Kimberly N. Smitheman, +16

PLoS ONE

Mycn Copy NumberBet Family ProteinsCell RegulationOncogenic AgentMedicine +12

LSD1 inhibition exerts its antileukemic effect by recommissioning PU.1- and C/EBPα-dependent enhancers in AML

Monica Cusan, Sheng F. Cai, Helai P. Mohammad, +14

Blood

Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-<i>trans</i> retinoic acid in acute myeloid leukemia across subtypes

Kimberly N. Smitheman, Tesa Severson, Satyajit Rajapurkar, +17

Haematologica

Abstract B88: A selective Raf kinase inhibitor induces cell death and tumor regression of human cancer cell lines encoding B-RafV600E mutation

Sylvie Laquerre, Marc R. Arnone, Katherine G. Moss, +15

Molecular Cancer Therapeutics

Tumor RegressionB-rafv600e MutationCell DeathSelectivity Towards B-rafCancer Biology +17

Rational Targeting of Cooperating Layers of the Epigenome Yields Enhanced Therapeutic Efficacy against AML

Cihangir Duy, Matt Teater, Francine E. Garrett-Bakelman, +20

Cancer Discovery