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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Proceedings of the National Academy of Sciences - PNAS, 2016-06, Vol.113 (26), p.7124-7129

2016

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Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.583-598

2018

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The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

Cell chemical biology, 2018-01, Vol.25 (1), p.67-77.e3

2018

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Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance

Communications biology, 2018-01, Vol.1 (1), p.100-100, Article 100

2018

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Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin

Molecular cancer therapeutics, 2011-08, Vol.10 (8), p.1394-1406

2011

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

Chemistry & biology, 2015-06, Vol.22 (6), p.755-763

2015

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OSI-930 : A novel selective inhibitor of kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models

Cancer research (Chicago, Ill.), 2006-01, Vol.66 (2), p.1015-1024

2006

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Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: Optimization of kinase selectivity and pharmacokinetics

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (16), p.4511-4516

2013

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Palladium-Catalyzed Direct Heck Arylation of Dual π-Deficient/π-Excessive Heteroaromatics. Synthesis of C-5 Arylated Imidazo[1,5-a]pyrazines

Organic letters, 2008-07, Vol.10 (14), p.2923-2926

2008

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A highly effective one-pot synthesis of quinolines from o-nitroarylcarbaldehydes

Organic & biomolecular chemistry, 2007-01, Vol.5 (1), p.61-64

2007

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Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (4), p.979-984

2013

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The Crystal Structure of a Constitutively Active Mutant RON Kinase Suggests an Intramolecular Autophosphorylation Hypothesis

Biochemistry (Easton), 2010-09, Vol.49 (37), p.7972-7974

2010

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Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (16), p.4517-4522

2013

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One-Pot Friedländer Quinoline Synthesis: Scope and Limitations

Synthesis (Stuttgart), 2010-05, Vol.2010 (10), p.1678-1686

2010

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Novel inhibitors of mTORC1 and mTORC2

Current opinion in investigational drugs (London, England : 2000), 2010-06, Vol.11 (6), p.638

2010

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Imidazo[1,5- a]pyrazines: Orally efficacious inhibitors of mTORC1 and mTORC2

Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (7), p.2092-2097

2011

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Synthesis of Substituted Imidazo[1,5-a]pyrazines via Mono-, Di-, and Directed Remote Metalation Strategies

Organic letters, 2009-11, Vol.11 (22), p.5118-5121

2009

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Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

Leukemia, 2017-09, Vol.31 (9), p.1951-1961

2017

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Abstract 43: Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.43-43

2021

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Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.44-44

2021

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Preclinical Activity of Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) and Their Combination with Venetoclax or CDK4/6 Inhibitor Against Human Mantle Cell Lymphoma (MCL) Cells

Blood, 2017-12, Vol.130, p.1265-1265

2017

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ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer

Journal of clinical oncology, 2019-03, Vol.37 (7_suppl), p.259-259

2019

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Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.5236-5236

2018

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An oral androgen receptor PROTAC degrader for prostate cancer

Journal of clinical oncology, 2018-02, Vol.36 (6_suppl), p.381-381

2018

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Azafulvenium methides: new extended dipolar systems

Chemical communications (Cambridge, England), 2000-01 (8), p.675-676

2000

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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance

Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4

OSI-930 : A novel selective inhibitor of kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models

Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: Optimization of kinase selectivity and pharmacokinetics

Palladium-Catalyzed Direct Heck Arylation of Dual π-Deficient/π-Excessive Heteroaromatics. Synthesis of C-5 Arylated Imidazo[1,5-a]pyrazines

A highly effective one-pot synthesis of quinolines from o-nitroarylcarbaldehydes

Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors

The Crystal Structure of a Constitutively Active Mutant RON Kinase Suggests an Intramolecular Autophosphorylation Hypothesis

Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1

One-Pot Friedländer Quinoline Synthesis: Scope and Limitations

Novel inhibitors of mTORC1 and mTORC2

Imidazo[1,5- a]pyrazines: Orally efficacious inhibitors of mTORC1 and mTORC2

Synthesis of Substituted Imidazo[1,5-a]pyrazines via Mono-, Di-, and Directed Remote Metalation Strategies

Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells

Abstract 43: Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer

Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer

Preclinical Activity of Novel BET Protein Proteolysis Targeting Chimeras (BETP-PROTACs) and Their Combination with Venetoclax or CDK4/6 Inhibitor Against Human Mantle Cell Lymphoma (MCL) Cells

ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer

Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer

An oral androgen receptor PROTAC degrader for prostate cancer

Azafulvenium methides: new extended dipolar systems

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