- 1/26/2021Identification and characterization of 2nd generation EZH2 inhibitors with extended residence times and improved biological activity
- 5/6/2020Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors
- 4/13/2020Merkel Cell Polyomavirus Activates LSD1-Mediated Blockade of Non-Canonical BAF to Regulate Transformation and Tumorigenesis
- 3/26/2020Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time
- 6/3/2019A Phase 2 Study of CPI-0610, a Bromodomain and Extraterminal Protein Inhibitor (BETi) Alone or With Ruxolitinib (RUX) in Patients with Myelofibrosis (MF)
- 5/16/2019CPI-0610, a Bromodomain and Extraterminal Domain (BET) Inhibitor, Reduces Pro-Inflammatory Cytokines, Bone Marrow Fibrosis and the Number of Transfusions in …
- 5/15/2019A Phase 2 Study of CPI-0610, a Bromodomain and Extraterminal Protein Inhibitor (BETi) alone or with Ruxolitinib (RUX), in Patients with Myelofibrosis (MF)
- 4/2/2019Single-cell RNA sequencing reveals transcriptomic heterogeneity in response to epigenetic inhibitors
- 4/1/2019ProSTAR: A phase 1b/2 study of CPI-1205, a small molecule inhibitor of EZH2, combined with enzalutamide (E) or abiraterone/prednisone (A/P) in patients with metastatic …
- 11/16/2018EZH2 inhibition as an effective treatment for metastatic castration-resistant prostate cancer
- 11/22/2016An alternative approach to ChIP-Seq normalization enables detection of genome-wide changes in histone H3 lysine 27 trimethylation upon EZH2 inhibition
- 10/10/2016Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide …
- 04/05/2016Pharmacological Inhibition of the Histone Lysine Demethylase KDM1A Suppresses the Growth of Multiple Acute Myeloid Leukemia Subtypes
- 03/15/2016Preclinical anticancer efficacy of BET bromodomain inhibitors is determined by the apoptotic response
- 02/25/2016Identification of a benzoisoxazoloazepine inhibitor (CPI-0610) of the bromodomain and extra-terminal (BET) family as a candidate for human clinical trials
- 04/17/2015Development of methyl isoxazoleazepines as inhibitors of BET
- 03/25/2015Discovery of benzotriazolo[4,3-d][1,4]diazepines as orally active inhibitors of BET bromodomains
- 12/16/2014The bromodomain and extra-terminal inhibitor CPI203 enhances the antiproliferative effects of rapamycin on human neuroendocrine tumors
- 12/16/2014Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma
- 11/14/2014EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation
- 09/05/2014A Practical Synthesis of Indoles via a Pd-Catalyzed C-N Ring Formation
- 07/24/2014Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors
- 04/02/2014Constellation Pharmaceuticals will give a presentation on EZH2 and exhibit posters on EZH2 and BET at the AACR Annual Meeting, April 5-9 in San Diego, CA.
- 01/14/2014Discovery and optimization of tetramethylpiperidinyl benzamides as inhibitors of EZH2
- 11/06/2013Identification of EZH2 and EZH1 Small Molecule Inhibitors with Selective Impact on Diffuse Large B Cell Lymphoma Cell Growth
- 06/16/2013Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors
- 10/04/2011Targeting MYC dependence in cancer by inhibiting BET bromodomains