Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208)

RVX-208, a BET-inhibitor for treating atherosclerotic cardiovascular disease, raises ApoA-I/HDL and represses pathways that contribute to cardiovascular disease

(2016) Dean Gilham et al.   ATHEROSCLEROSIS

Effect of the BET Protein Inhibitor, RVX-208, on Progression of Coronary Atherosclerosis: Results of the Phase 2b, Randomized, Double-Blind, Multicenter, ASSURE Trial

(2015) Stephen J. Nicholls et al.   American Journal of Cardiovascular Drugs

BET Bromodomain Inhibition Suppresses the Function of Hematopoietic Transcription Factors in Acute Myeloid Leukemia

(2015) Jae-Seok Roe et al.   MOLECULAR CELL

Complement System Part II: Role in Immunity

(2015) Nicolas S. Merle et al.   Frontiers in Immunology

Complement System Part I – Molecular Mechanisms of Activation and Regulation

(2015) Nicolas S. Merle et al.   Frontiers in Immunology

A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice

(2014) Ravi Jahagirdar et al.   ATHEROSCLEROSIS

C3 and C4 are strongly related to adipose tissue variables and cardiovascular risk factors

(2014) Bo Nilsson et al.   EUROPEAN JOURNAL OF CLINICAL INVESTIGATION

BET bromodomain inhibition suppresses transcriptional responses to cytokine-Jak-STAT signaling in a gene-specific manner in human monocytes

(2014) Chun Hin Chan et al.   EUROPEAN JOURNAL OF IMMUNOLOGY

Complement activation products C5a and sC5b-9 are associated with low-grade inflammation and endothelial dysfunction, but not with atherosclerosis in a cross-sectional analysis: The CODAM study

(2014) E. Hertle et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

NF-κB Directs Dynamic Super Enhancer Formation in Inflammation and Atherogenesis

(2014) Jonathan D. Brown et al.   MOLECULAR CELL

The complement system in human cardiometabolic disease

(2014) E. Hertle et al.   MOLECULAR IMMUNOLOGY

RVX-208, an Inducer of ApoA-I in Humans, Is a BET Bromodomain Antagonist

(2014) Kevin G. McLure et al.   PLoS One

Hepatic nuclear factor 4α positively regulates complement C3 expression and does not interfere with TNFα-mediated stimulation of C3 expression in HepG2 cells

(2013) Vladimir S. Shavva et al.   GENE

Mice Lacking C1q Are Protected from High Fat Diet-induced Hepatic Insulin Resistance and Impaired Glucose Homeostasis

(2013) Antoinette D. Hillian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

BET Protein Function Is Required for Inflammation: Brd2 Genetic Disruption and BET Inhibitor JQ1 Impair Mouse Macrophage Inflammatory Responses

(2013) A. C. Belkina et al.   JOURNAL OF IMMUNOLOGY

Brd4 maintains constitutively active NF-κB in cancer cells by binding to acetylated RelA

(2013) Z Zou et al.   ONCOGENE

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

(2013) S. Picaud et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Soluble form of membrane attack complex independently predicts mortality and cardiovascular events in patients with ST-elevation myocardial infarction treated with primary percutaneous coronary intervention

(2012) Søren Lindberg et al.   AMERICAN HEART JOURNAL

ApoA-I Induction as a Potential Cardioprotective Strategy: Rationale for the SUSTAIN and ASSURE Studies

(2012) Stephen J. Nicholls et al.   CARDIOVASCULAR DRUGS AND THERAPY

Complement anaphylatoxin C3a as a novel independent prognostic marker in heart failure

(2012) Tímea Gombos et al.   Clinical Research in Cardiology

Down-regulation of NF-κB Transcriptional Activity in HIV-associated Kidney Disease by BRD4 Inhibition

(2012) Guangtao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Peroxisome Proliferator-activated Receptor α Positively Regulates Complement C3 Expression but Inhibits Tumor Necrosis Factor α-mediated Activation ofC3Gene in Mammalian Hepatic-derived Cells

(2012) Denis A. Mogilenko et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors

(2012) H. S. Bandukwala et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Complement C3 and cleavage products in cardiometabolic risk

(2011) Altan Onat et al.   CLINICA CHIMICA ACTA

Hepatic acute phase proteins – Regulation by IL-6- and IL-1-type cytokines involving STAT3 and its crosstalk with NF-κB-dependent signaling

(2011) Johannes G. Bode et al.   EUROPEAN JOURNAL OF CELL BIOLOGY

Efficacy and Safety of a Novel Oral Inducer of Apolipoprotein A-I Synthesis in Statin-Treated Patients With Stable Coronary Artery Disease

(2011) Stephen J. Nicholls et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Aptamer-Based Multiplexed Proteomic Technology for Biomarker Discovery

(2011) Larry Gold et al.   PLoS One

Pentraxins (CRP, SAP) in the process of complement activation and clearance of apoptotic bodies through Fcγ receptors

(2010) Terry W Du Clos et al.   Current Opinion in Organ Transplantation

Molecular Intercommunication between the Complement and Coagulation Systems

(2010) U. Amara et al.   JOURNAL OF IMMUNOLOGY

Suppression of inflammation by a synthetic histone mimic

(2010) Edwige Nicodeme et al.   NATURE

Coronary late lumen loss of drug eluting stents is associated with increased serum levels of the complement components C3a and C5a

(2009) Walter S. Speidl et al.   ATHEROSCLEROSIS

The C3a Anaphylatoxin Receptor Is a Key Mediator of Insulin Resistance and Functions by Modulating Adipose Tissue Macrophage Infiltration and Activation

(2009) Y. Mamane et al.   DIABETES