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RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

PloS one, 2013-12, Vol.8 (12), p.e83190

2013

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RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease

Molecular pharmacology, 2017-12, Vol.92 (6), p.694-706

2017

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Inhibition of integrin-linked kinase (ILK) suppresses activation of protein kinase B/Akt and induces cell cycle arrest and apoptosis of PTEN-mutant prostate cancer cells

Proceedings of the National Academy of Sciences - PNAS, 2000-03, Vol.97 (7), p.3207-3212

2000

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Inhibition of Integrin-Linked Kinase (ILK) Suppresses Activation of Protein Kinase B/Akt and Induces Cell Cycle Arrest and Apoptosis of PTEN-Mutant Prostate Cancer Cells

Proceedings of the National Academy of Sciences - PNAS, 2000-03, Vol.97 (7), p.3207-3212

2000

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Integration of cell attachment, cytoskeletal localization, and signaling by integrin-linked kinase (ILK), CH-ILKBP, and the tumor suppressor PTEN

Molecular biology of the cell, 2003-12, Vol.14 (12), p.4813-4825

2003

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Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2

ACS omega, 2021-08, Vol.6 (33), p.21327-21338

2021

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A Phase Ib/IIa Study of the Pan-BET Inhibitor ZEN-3694 in Combination with Enzalutamide in Patients with Metastatic Castration-resistant Prostate Cancer

Clinical cancer research, 2020-10, Vol.26 (20), p.5338-5347

2020

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

Atherosclerosis, 2014-09, Vol.236 (1), p.91-100

2014

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A randomized mCRPC phase 2b study of the BET bromodomain inhibitor (BETi) zen-3694 and enzalutamide vesus enzalutamide

Journal of clinical oncology, 2022-02, Vol.40 (6_suppl), p.TPS201-TPS201

2022

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A phase 1b/2 study of the BET inhibitor ZEN-3694 in combination with talazoparib for treatment of patients with TNBC without gBRCA1/2 mutations

Journal of clinical oncology, 2022-06, Vol.40 (16_suppl), p.1023-1023

2022

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A Phase 1b/2a Study of the Pan-BET Bromodomain Inhibitor ZEN-3694 in Combination with Enzalutamide in Patients with Metastatic Castration Resistant Prostate Cancer

Clinical cancer research, 2020-07, Vol.26 (20), p.5338-5347

2020

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Abstract PS11-10: A Phase 1b/2 Study of the BET inhibitor ZEN003694 in combination with talazoparib for treatment of patients with TNBC without gBRCA1/2 mutations

Cancer research (Chicago, Ill.), 2021-02, Vol.81 (4_Supplement), p.PS11-10-PS11-10

2021

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The integrin-linked kinase (ILK) suppresses anoikis

Oncogene, 2000-08, Vol.19 (33), p.3811-3815

2000

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Abstract CT095: A Phase Ib/IIa study of the BET bromodomain inhibitor ZEN-3694 in combination with enzalutamide in patients with metastatic castration-resistant prostate cancer (mCRPC)

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.CT095-CT095

2019

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Abstract LB-038: Preclinical development and clinical validation of a whole blood pharmacodynamic marker assay for the BET bromodomain inhibitor ZEN-3694 in metastatic castration-resistant prostate cancer (mCRPC) patients

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.LB-038-LB-038

2017

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Regulation of protein kinase B/Akt-serine 473 phosphorylation by integrin-linked kinase: critical roles for kinase activity and amino acids arginine 211 and serine 343

The Journal of biological chemistry, 2001-07, Vol.276 (29), p.27462-27469

2001

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Integrin-linked kinase activity regulates Rac- and Cdc42-mediated actin cytoskeleton reorganization via α-PIX

Oncogene, 2005-09, Vol.24 (38), p.5837-5849

2005

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Abstract C86: The clinical candidate ZEN-3694, a novel BET bromodomain inhibitor, is efficacious in the treatment of a variety of solid tumor and hematological malignancies, alone or in combination with several standard of care and targeted therapies

Molecular cancer therapeutics, 2015-12, Vol.14 (12_Supplement_2), p.C86-C86

2015

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Abstract LB-207: Preclinical characterization of ZEN-3694, a novel BET bromodomain inhibitor entering phase I studies for metastatic castration-resistant prostate cancer (mCRPC)

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.LB-207-LB-207

2016

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Abstract 338: Effects of RVX-208 a Selective Bromodomain Extra-Terminal Protein Inhibitor Beyond Raising ApoA-I/HDL

Arteriosclerosis, thrombosis, and vascular biology, 2015-05, Vol.35 (suppl_1)

2015

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Recent Doctoral Research

Lymphatic research and biology, 2005-06, Vol.3 (2), p.93-99

2005

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Abstract LB-92: RVX-2135 is a novel, orally bioavailable epigenetic BET inhibitor that synergizes with cytarabine and idarubicin to inhibit proliferation of acute myeloid leukemia cells

Cancer research (Chicago, Ill.), 2013-04, Vol.73 (8_Supplement), p.LB-92-LB-92

2013

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Regulation of Protein Kinase B/Akt-Serine 473 Phosphorylation by Integrin-linked Kinase

The Journal of biological chemistry, 2001-07, Vol.276 (29), p.27462-27469

2001

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Integrin-linked kinase activity regulates Rac- and Cdc42-mediated actin cytoskeleton reorganization via -PIX

Oncogene, 2005-09, Vol.24 (38), p.5837-5849

2005

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RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist

RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease

Inhibition of integrin-linked kinase (ILK) suppresses activation of protein kinase B/Akt and induces cell cycle arrest and apoptosis of PTEN-mutant prostate cancer cells

Inhibition of Integrin-Linked Kinase (ILK) Suppresses Activation of Protein Kinase B/Akt and Induces Cell Cycle Arrest and Apoptosis of PTEN-Mutant Prostate Cancer Cells

Integration of cell attachment, cytoskeletal localization, and signaling by integrin-linked kinase (ILK), CH-ILKBP, and the tumor suppressor PTEN

Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2

A Phase Ib/IIa Study of the Pan-BET Inhibitor ZEN-3694 in Combination with Enzalutamide in Patients with Metastatic Castration-resistant Prostate Cancer

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

BET Bromodomain Inhibition Blocks an AR-Repressed, E2F1-Activated Treatment-Emergent Neuroendocrine Prostate Cancer Lineage Plasticity Program

A randomized mCRPC phase 2b study of the BET bromodomain inhibitor (BETi) zen-3694 and enzalutamide vesus enzalutamide

A phase 1b/2 study of the BET inhibitor ZEN-3694 in combination with talazoparib for treatment of patients with TNBC without gBRCA1/2 mutations

A Phase 1b/2a Study of the Pan-BET Bromodomain Inhibitor ZEN-3694 in Combination with Enzalutamide in Patients with Metastatic Castration Resistant Prostate Cancer

Abstract PS11-10: A Phase 1b/2 Study of the BET inhibitor ZEN003694 in combination with talazoparib for treatment of patients with TNBC without gBRCA1/2 mutations

The integrin-linked kinase (ILK) suppresses anoikis

Abstract CT095: A Phase Ib/IIa study of the BET bromodomain inhibitor ZEN-3694 in combination with enzalutamide in patients with metastatic castration-resistant prostate cancer (mCRPC)

Abstract LB-038: Preclinical development and clinical validation of a whole blood pharmacodynamic marker assay for the BET bromodomain inhibitor ZEN-3694 in metastatic castration-resistant prostate cancer (mCRPC) patients

Regulation of protein kinase B/Akt-serine 473 phosphorylation by integrin-linked kinase: critical roles for kinase activity and amino acids arginine 211 and serine 343

Integrin-linked kinase activity regulates Rac- and Cdc42-mediated actin cytoskeleton reorganization via α-PIX

Abstract C86: The clinical candidate ZEN-3694, a novel BET bromodomain inhibitor, is efficacious in the treatment of a variety of solid tumor and hematological malignancies, alone or in combination with several standard of care and targeted therapies

Abstract LB-207: Preclinical characterization of ZEN-3694, a novel BET bromodomain inhibitor entering phase I studies for metastatic castration-resistant prostate cancer (mCRPC)

Abstract 338: Effects of RVX-208 a Selective Bromodomain Extra-Terminal Protein Inhibitor Beyond Raising ApoA-I/HDL

Recent Doctoral Research

Abstract LB-92: RVX-2135 is a novel, orally bioavailable epigenetic BET inhibitor that synergizes with cytarabine and idarubicin to inhibit proliferation of acute myeloid leukemia cells

Regulation of Protein Kinase B/Akt-Serine 473 Phosphorylation by Integrin-linked Kinase

Integrin-linked kinase activity regulates Rac- and Cdc42-mediated actin cytoskeleton reorganization via -PIX

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