The BET inhibitor GS-5829 targets chronic lymphocytic leukemia cells and their supportive microenvironment

Depth and durability of response to ibrutinib in CLL: 5-year follow-up of a phase 2 study

(2018) Inhye E. Ahn et al.   BLOOD

Single-agent ibrutinib in treatment-naïve and relapsed/refractory chronic lymphocytic leukemia: a 5-year experience

(2018) Susan O’Brien et al.   BLOOD

Evolution of CLL treatment — from chemoimmunotherapy to targeted and individualized therapy

(2018) Jan A. Burger et al.   Nature Reviews Clinical Oncology

BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor

(2018) Hatice Gulcin Ozer et al.   Cancer Discovery

Ibrutinib plus obinutuzumab versus chlorambucil plus obinutuzumab in first-line treatment of chronic lymphocytic leukaemia (iLLUMINATE): a multicentre, randomised, open-label, phase 3 trial

(2018) Carol Moreno et al.   LANCET ONCOLOGY

Ibrutinib Regimens versus Chemoimmunotherapy in Older Patients with Untreated CLL

(2018) Jennifer A. Woyach et al.   NEW ENGLAND JOURNAL OF MEDICINE

Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor

(2018) David Sperandio et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Calreticulin as a novel B-cell receptor antigen in chronic lymphocytic leukemia

(2017) Elisa ten Hacken et al.   HAEMATOLOGICA

Ibrutinib modulates the immunosuppressive CLL microenvironment through STAT3-mediated suppression of regulatory B-cell function and inhibition of the PD-1/PD-L1 pathway

(2017) K Kondo et al.   LEUKEMIA

Direct in vivo evidence for increased proliferation of CLL cells in lymph nodes compared to bone marrow and peripheral blood

(2017) T M Herndon et al.   LEUKEMIA

Myc enhances B-cell receptor signaling in precancerous B cells and confers resistance to Btk inhibition

(2017) T K Moyo et al.   ONCOGENE

Unification of de novo and acquired ibrutinib resistance in mantle cell lymphoma

(2017) Xiaohong Zhao et al.   Nature Communications

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

(2017) Xiaochuan Shan et al.   eLife

Calreticulin as a novel B-cell receptor antigen in chronic lymphocytic leukemia

(2017) Elisa ten Hacken et al.   HAEMATOLOGICA

Chronic lymphocytic leukaemia

(2017) Thomas J. Kipps et al.   Nature Reviews Disease Primers

Ibrutinib inhibits pre-BCR+B-cell acute lymphoblastic leukemia progression by targeting BTK and BLK

(2016) Ekaterina Kim et al.   BLOOD

HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues

(2016) Xiaoyu Lin et al.   MOLECULAR CANCER THERAPEUTICS

Nurse-like cells impact on disease progression in chronic lymphocytic leukemia

(2016) F Boissard et al.   Blood Cancer Journal

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

(2016) Sandy Amorim et al.   Lancet Haematology

Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib

(2015) B. Sun et al.   BLOOD

The BET Bromodomain Inhibitor OTX015 Affects Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes with Targeted Drugs

(2015) M. Boi et al.   CLINICAL CANCER RESEARCH

Extracellular HMGB1 promotes differentiation of nurse-like cells in chronic lymphocytic leukemia

(2014) L. Jia et al.   BLOOD

Ibrutinib inhibits BCR and NF- B signaling and reduces tumor proliferation in tissue-resident cells of patients with CLL

(2014) S. E. M. Herman et al.   BLOOD

Prolonged lymphocytosis during ibrutinib therapy is associated with distinct molecular characteristics and does not indicate a suboptimal response to therapy

(2014) J. A. Woyach et al.   BLOOD

Characterization of ibrutinib-sensitive and -resistant mantle lymphoma cells

(2014) Jiao Ma et al.   BRITISH JOURNAL OF HAEMATOLOGY

Inhibition of Bromodomain Proteins for the Treatment of Human Diffuse Large B-cell Lymphoma

(2014) S. E. Trabucco et al.   CLINICAL CANCER RESEARCH

Lenalidomide interferes with tumor-promoting properties of nurse-like cells in chronic lymphocytic leukemia

(2014) S. Fiorcari et al.   HAEMATOLOGICA

Ibrutinib-induced lymphocytosis in patients with chronic lymphocytic leukemia: correlative analyses from a phase II study

(2014) S E M Herman et al.   LEUKEMIA

The Mechanisms behind the Therapeutic Activity of BET Bromodomain Inhibition

(2014) Junwei Shi et al.   MOLECULAR CELL

Blockade of oncogenic I B kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors

(2014) M. Ceribelli et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Lenalidomide reduces survival of chronic lymphocytic leukemia cells in primary cocultures by altering the myeloid microenvironment

(2013) A. Schulz et al.   BLOOD

Discovery and Characterization of Super-Enhancer-Associated Dependencies in Diffuse Large B Cell Lymphoma

(2013) Bjoern Chapuy et al.   CANCER CELL

Selective Inhibition of Tumor Oncogenes by Disruption of Super-Enhancers

(2013) Jakob Lovén et al.   CELL

Super-Enhancers in the Control of Cell Identity and Disease

(2013) Denes Hnisz et al.   CELL

BTK inhibition targets in vivo CLL proliferation through its effects on B-cell receptor signaling activity

(2013) S Cheng et al.   LEUKEMIA

Pharmacological and genomic profiling identifies NF-κB–targeted treatment strategies for mantle cell lymphoma

(2013) Rami Rahal et al.   NATURE MEDICINE

Coming full circle: 70 years of chronic lymphocytic leukemia cell redistribution, from glucocorticoids to inhibitors of B-cell receptor signaling

(2012) J. A. Burger et al.   BLOOD

The clinically active BTK inhibitor PCI-32765 targets B-cell receptor- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemia

(2012) M. F. M. de Rooij et al.   BLOOD

The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo

(2011) S. Ponader et al.   BLOOD

Genomic and phenotypic characterization of nurse-like cells that promote drug resistance in chronic lymphocytic leukemia

(2011) Loic Ysebaert et al.   LEUKEMIA & LYMPHOMA

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

(2011) Mark A. Dawson et al.   NATURE

The lymph node microenvironment promotes B-cell receptor signaling, NF- B activation, and tumor proliferation in chronic lymphocytic leukemia

(2010) Y. Herishanu et al.   BLOOD

High-level expression of the T-cell chemokines CCL3 and CCL4 by chronic lymphocytic leukemia B cells in nurselike cell cocultures and after BCR stimulation

(2008) J. A. Burger et al.   BLOOD