Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials

(2016) Brian K. Albrecht et al.   JOURNAL OF MEDICINAL CHEMISTRY

Immunomodulatory drugs target IKZF1-IRF4-MYC axis in primary effusion lymphoma in a cereblon-dependent manner and display synergistic cytotoxicity with BRD4 inhibitors

(2015) R Gopalakrishnan et al.   ONCOGENE

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Targeting bromodomains: epigenetic readers of lysine acetylation

(2014) Panagis Filippakopoulos et al.   NATURE REVIEWS DRUG DISCOVERY

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

(2013) A. Chaidos et al.   BLOOD

PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains

(2013) S. Picaud et al.   CANCER RESEARCH

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs

(2013) D Cirstea et al.   LEUKEMIA

Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors

(2013) B Tolani et al.   ONCOGENE

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

(2013) J. Kronke et al.   SCIENCE

The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins

(2013) G. Lu et al.   SCIENCE

MYC addiction: a potential therapeutic target in MM

(2012) W. M. Kuehl et al.   BLOOD

Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma

(2012) L. Santo et al.   BLOOD

BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia

(2012) C. J. Ott et al.   BLOOD

MYC on the Path to Cancer

(2012) Chi V. Dang   CELL

The Era of Combination Therapy in Myeloma

(2012) Sagar Lonial et al.   JOURNAL OF CLINICAL ONCOLOGY

Pathogenesis of Myeloma

(2011) Kenneth C. Anderson et al.   Annual Review of Pathology-Mechanisms of Disease

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc

(2011) Jake E. Delmore et al.   CELL

Antimyeloma Activity of a Multitargeted Kinase Inhibitor, AT9283, via Potent Aurora Kinase and STAT3 Inhibition Either Alone or in Combination with Lenalidomide

(2011) L. Santo et al.   CLINICAL CANCER RESEARCH

Clinical and biological implications of MYC activation: a common difference between MGUS and newly diagnosed multiple myeloma

(2011) W-J Chng et al.   LEUKEMIA

The Brd4 Extraterminal Domain Confers Transcription Activation Independent of pTEFb by Recruiting Multiple Proteins, Including NSD3

(2011) S. Rahman et al.   MOLECULAR AND CELLULAR BIOLOGY

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

(2011) Johannes Zuber et al.   NATURE

Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

(2011) Mark A. Dawson et al.   NATURE

Targeting MYC dependence in cancer by inhibiting BET bromodomains

(2011) J. A. Mertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

AT7519, A novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3β activation and RNA polymerase II inhibition

(2010) L Santo et al.   ONCOGENE

The ups and downs of Myc biology

(2009) Laura Soucek et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Preclinical activity of P276-00, a novel small-molecule cyclin-dependent kinase inhibitor in the therapy of multiple myeloma

(2009) N Raje et al.   LEUKEMIA

IRF4 addiction in multiple myeloma

(2008) Arthur L. Shaffer et al.   NATURE