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Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure

EMBO reports, 2015-03, Vol.16 (3), p.280-296

2015

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Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF

Cancer research (Chicago, Ill.), 2018-03, Vol.78 (6), p.1537-1548

2018

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Chromosome-Wide Mapping of Estrogen Receptor Binding Reveals Long-Range Regulation Requiring the Forkhead Protein FoxA1

Cell, 2005-07, Vol.122 (1), p.33-43

2005

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Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor

Journal of medicinal chemistry, 2013-08, Vol.56 (16), p.6495-6511

2013

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Evaluation of Combination Strategies for the A2AR Inhibitor AZD4635 Across Tumor Microenvironment Conditions via a Systems Pharmacology Model

Frontiers in immunology, 2021-03, Vol.12, p.617316-617316

2021

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Inhibiting Tankyrases Sensitizes KRAS-Mutant Cancer Cells to MEK Inhibitors via FGFR2 Feedback Signaling

Cancer research (Chicago, Ill.), 2014-06, Vol.74 (12), p.3294-3305

2014

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Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight

Journal of medicinal chemistry, 2016-05, Vol.59 (10), p.4711-4723

2016

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In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma

Haematologica (Roma), 2010-05, Vol.95 (5), p.794-803

2010

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Coactivator AIB1 Links Estrogen Receptor Transcriptional Activity and Stability

Proceedings of the National Academy of Sciences - PNAS, 2004-08, Vol.101 (32), p.11599-11604

2004

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ERAP140, a Conserved Tissue-Specific Nuclear Receptor Coactivator

Molecular and Cellular Biology, 2002-05, Vol.22 (10), p.3358-3372

2002

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AZD4573 Is a Highly Selective CDK9 Inhibitor That Suppresses MCL-1 and Induces Apoptosis in Hematologic Cancer Cells

Clinical cancer research, 2020-02, Vol.26 (4), p.922-934

2020

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Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer

Clinical cancer research, 2016-02, Vol.22 (3), p.644-656

2016

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Abstract 2500: Transient CDK9 inhibition with AZD4573 modulates Bfl-1 in preclinical lymphoma models

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.2500-2500

2019

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Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies

Journal of medicinal chemistry, 2020-12, Vol.63 (24), p.15564-15590

2020

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Targeting Bfl-1 via acute CDK9 inhibition overcomes intrinsic BH3-mimetic resistance in lymphomas

Blood, 2021-05, Vol.137 (21), p.2947-2957

2021

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Advances in estrogen receptor biology: prospects for improvements in targeted breast cancer therapy

Breast cancer research : BCR, 2004-01, Vol.6 (1), p.39-52, Article 39

2004

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Abstract 1664: Inhibition of arginase in combination with radiation therapy shows increased immune-activation and anti-tumor activity in syngeneic tumor models

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.1664-1664

2021

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Abstract 306: A mechanistic rationale for combining acalabrutinib with CDK9 inhibitor, AZD4573, in ABC-DLBCL

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.306-306

2018

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Abstract CT168: Clinical pharmacology of AZD4635 (A2ARi): Integration of PK data from cancer patients (CP) and healthy volunteer (HV) clinical trials to provide dosing recommendations

Cancer research (Chicago, Ill.), 2020-08, Vol.80 (16_Supplement), p.CT168-CT168

2020

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Abstract 4523: Inhibition of arginase in combination with anti-PDL1 leads to increased infiltration and activation of CD8+ T cells, NK cells, and CD103+ dendritic cells in mouse syngeneic tumor models

Cancer research (Chicago, Ill.), 2020-08, Vol.80 (16_Supplement), p.4523-4523

2020

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Combination of AZD4573, a Selective CDK9 Inhibitor, with Other Cell Death Inducing Agents Can Overcome De Novo Venetoclax Resistance in Preclinical Hematologic Tumor Models

Blood, 2018-11, Vol.132 (Supplement 1), p.3946-3946

2018

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Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity

Journal for immunotherapy of cancer, 2020-07, Vol.8 (2)

2020

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Abstract 297: AZD4573: Mechanistic PKPD model linking CDK9 inhibition to Mcl1 depletion and induction of apoptosis in preclinical AML model

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.297-297

2018

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Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure

Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF

Chromosome-Wide Mapping of Estrogen Receptor Binding Reveals Long-Range Regulation Requiring the Forkhead Protein FoxA1

Identification of NVP-TNKS656: The Use of Structure–Efficiency Relationships To Generate a Highly Potent, Selective, and Orally Active Tankyrase Inhibitor

Evaluation of Combination Strategies for the A2AR Inhibitor AZD4635 Across Tumor Microenvironment Conditions via a Systems Pharmacology Model

Inhibiting Tankyrases Sensitizes KRAS-Mutant Cancer Cells to MEK Inhibitors via FGFR2 Feedback Signaling

Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight

In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma

Coactivator AIB1 Links Estrogen Receptor Transcriptional Activity and Stability

ERAP140, a Conserved Tissue-Specific Nuclear Receptor Coactivator

AZD4573 Is a Highly Selective CDK9 Inhibitor That Suppresses MCL-1 and Induces Apoptosis in Hematologic Cancer Cells

Tankyrase Inhibition Blocks Wnt/β-Catenin Pathway and Reverts Resistance to PI3K and AKT Inhibitors in the Treatment of Colorectal Cancer

Abstract 2500: Transient CDK9 inhibition with AZD4573 modulates Bfl-1 in preclinical lymphoma models

Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies

Targeting Bfl-1 via acute CDK9 inhibition overcomes intrinsic BH3-mimetic resistance in lymphomas

Advances in estrogen receptor biology: prospects for improvements in targeted breast cancer therapy

Abstract 1664: Inhibition of arginase in combination with radiation therapy shows increased immune-activation and anti-tumor activity in syngeneic tumor models

Abstract 306: A mechanistic rationale for combining acalabrutinib with CDK9 inhibitor, AZD4573, in ABC-DLBCL

Abstract CT168: Clinical pharmacology of AZD4635 (A2ARi): Integration of PK data from cancer patients (CP) and healthy volunteer (HV) clinical trials to provide dosing recommendations

Abstract 4523: Inhibition of arginase in combination with anti-PDL1 leads to increased infiltration and activation of CD8+ T cells, NK cells, and CD103+ dendritic cells in mouse syngeneic tumor models

Genomic sequencing of colorectal adenocarcinomas identifies a recurrent VTI1A - TCF7L2 fusion

Combination of AZD4573, a Selective CDK9 Inhibitor, with Other Cell Death Inducing Agents Can Overcome De Novo Venetoclax Resistance in Preclinical Hematologic Tumor Models

Discovery of N‑(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)‑1H‑1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors

Small molecule AZD4635 inhibitor of A2AR signaling rescues immune cell function including CD103+ dendritic cells enhancing anti-tumor immunity

Abstract 297: AZD4573: Mechanistic PKPD model linking CDK9 inhibition to Mcl1 depletion and induction of apoptosis in preclinical AML model

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