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

Molecular cancer therapeutics, 2017-02, Vol.16 (2), p.388-396

2017

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Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075

Molecular cancer research, 2017-01, Vol.15 (1), p.35-44

2017

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PRL-3, a metastasis associated tyrosine phosphatase, is involved in FLT3-ITD signaling and implicated in anti-AML therapy

PloS one, 2011-05, Vol.6 (5), p.e19798-e19798

2011

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Identification of VEGF Signaling Inhibition-Induced Glomerular Injury in Rats through Site-Specific Urinary Biomarkers

International journal of molecular sciences, 2021-11, Vol.22 (23), p.12629

2021

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Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Nature (London), 2020-02, Vol.578 (7794), p.306-310

2020

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Role of Class I and Class II histone deacetylases in carcinoma cells using siRNA

Biochemical and biophysical research communications, 2003-10, Vol.310 (2), p.529-536

2003

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ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside

Journal of hematology and oncology, 2009-07, Vol.2 (1), p.33-33, Article 33

2009

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Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases

Bioorganic & medicinal chemistry letters, 2011-09, Vol.21 (18), p.5620-5624

2011

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Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Journal of medicinal chemistry, 2020-05, Vol.63 (10), p.5585-5623

2020

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Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Journal of medicinal chemistry, 2020-05, Vol.63 (10), p.5585-5623

2020

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Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

Science translational medicine, 2015-03, Vol.7 (279), p.279ra40

2015

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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Cancer research (Chicago, Ill.), 2017-06, Vol.77 (11), p.2976-2989

2017

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A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies

Leukemia, 2020-06, Vol.34 (6), p.1646-1657

2020

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Hypoxia-Inducible Factor-1 Inhibition in Combination with Temozolomide Treatment Exhibits Robust Antitumor Efficacy In vivo

Clinical cancer research, 2006-08, Vol.12 (15), p.4747-4754

2006

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Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Molecular cancer therapeutics, 2017-08, Vol.16 (8), p.1511-1520

2017

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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Molecular cancer therapeutics, 2021-10, Vol.20 (10), p.1809-1819

2021

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Effect of the multitargeted receptor tyrosine kinase inhibitor, ABT-869 [N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea], on blood pressure in conscious rats and mice: reversal with antihypertensive agents and effect on tumor growth inhibition

The Journal of pharmacology and experimental therapeutics, 2009-06, Vol.329 (3), p.928-937

2009

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Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors

Bioorganic & medicinal chemistry, 2008, Vol.18 (1), p.386-390

2008

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Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (14), p.4528-4531

2012

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Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML

Blood, 2009-04, Vol.113 (17), p.4052-4062

2009

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (10), p.1804-1810

2018

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Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML

In vivo (Athens), 2022-07, Vol.36 (4), p.1615-1627

2022

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

Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075

PRL-3, a metastasis associated tyrosine phosphatase, is involved in FLT3-ITD signaling and implicated in anti-AML therapy

Identification of VEGF Signaling Inhibition-Induced Glomerular Injury in Rats through Site-Specific Urinary Biomarkers

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Role of Class I and Class II histone deacetylases in carcinoma cells using siRNA

ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases

Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia

A novel CDK9 inhibitor increases the efficacy of venetoclax (ABT-199) in multiple models of hematologic malignancies

Hypoxia-Inducible Factor-1 Inhibition in Combination with Temozolomide Treatment Exhibits Robust Antitumor Efficacy In vivo

Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors

Effect of the multitargeted receptor tyrosine kinase inhibitor, ABT-869 [N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea], on blood pressure in conscious rats and mice: reversal with antihypertensive agents and effect on tumor growth inhibition

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors

Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML

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