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Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1

Journal of medicinal chemistry, 2018-09, Vol.61 (18), p.8120-8135

2018

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Hedgehog pathway activation in chronic myeloid leukemia: A promise for a novel combination therapeutic approach?

Cell cycle (Georgetown, Tex.), 2010-09, Vol.9 (17), p.3449-3456

2010

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Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist

ACS medicinal chemistry letters, 2010-06, Vol.1 (3), p.130-134

2010

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An Efficient Rapid System for Profiling the Cellular Activities of Molecular Libraries

Proceedings of the National Academy of Sciences - PNAS, 2006-02, Vol.103 (9), p.3153-3158

2006

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A Conserved Salt Bridge in the G Loop of Multiple Protein Kinases Is Important for Catalysis and for In Vivo Lyn Function

Molecular cell, 2009-01, Vol.33 (1), p.43-52

2009

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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials

Journal of medicinal chemistry, 2013-07, Vol.56 (14), p.5675-5690

2013

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The effects of Bcr-Abl on C/EBP transcription-factor regulation and neutrophilic differentiation are reversed by the Abl kinase inhibitor imatinib mesylate

Blood, 2003-01, Vol.101 (2), p.655-663

2003

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Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma

Science translational medicine, 2010-09, Vol.2 (51), p.51ra70

2010

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Ba/F3 cells and their use in kinase drug discovery

Current opinion in oncology, 2007-01, Vol.19 (1), p.55-60

2007

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Addendum: The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

Nature (London), 2012-12, Vol.492 (7428), p.290-290

2012

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Abstract 3406: Comprehensive genomic profiling of hematologic malignancies identifies recurrent somatic splicing factor mutations in non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM)

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.3406-3406

2018

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H3B-6545, a selective estrogen receptor covalent antagonist, prevents bone loss in ovariectomized Sprague-Dawley rats

Journal of pharmacological and toxicological methods, 2019-09, Vol.99, p.106595, Article 106595

2019

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Effect of a high-fat meal on the relative bioavailability of H3B-6527, a novel FGFR4 inhibitor, in healthy volunteers

Cancer chemotherapy and pharmacology, 2019-01, Vol.83 (1), p.91-96

2019

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Role of p21WAF1/CIP1 as an attenuator of both proliferative and drug-induced apoptotic signals in BCR-ABL-transformed hematopoietic cells

Annals of hematology, 2008-03, Vol.87 (3), p.183-193

2008

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Abstract PS12-23: Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERaWT and ERaMUT breast cancer

Cancer research (Chicago, Ill.), 2021-02, Vol.81 (4_Supplement), p.PS12-23-PS12-23

2021

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Abstract 281: Sensitivity to splicing modulation of BCL2 family genes reveals cancer therapeutic strategies for splicing modulators

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.281-281

2019

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In vitro-in vivo correlation of clearance for H3B-5942, a novel selective erα covalent antagonist (SERCA)

Drug metabolism and pharmacokinetics, 2019-01, Vol.34 (1), p.S22-S22

2019

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Abstract 4269: Exome sequencing of tumor cell lines: Optimizing for cancer variants

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.4269-4269

2014

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Abstract 3013: Identification of PHF5A as a common cellular target of splicing-modulating chemical probes

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.3013-3013

2016

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Abstract 3126: H3B6527, a selective and potent FGFR4 inhibitor for FGF19-driven hepatocellular carcinoma

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.3126-3126

2017

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Abstract 126: A chemogenomic approach reveals the action of splicing modulators at the branch point adenosine binding pocket defined by the PHF5A/SF3b complex

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.126-126

2017

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Abstract ND10: Discovery of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for MYC-driven cancers

Cancer research (Chicago, Ill.), 2023-05, Vol.83 (7_Supplement), p.ND10-ND10

2023

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H3B-8800-G0001-101: A first in human phase I study of a splicing modulator in patients with advanced myeloid malignancies

Journal of clinical oncology, 2017-05, Vol.35 (15_suppl), p.TPS7075-TPS7075

2017

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Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1

Hedgehog pathway activation in chronic myeloid leukemia: A promise for a novel combination therapeutic approach?

Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist

Author Correction: Evasion of immunosurveillance by genomic alterations of PPARγ/RXRα in bladder cancer

An Efficient Rapid System for Profiling the Cellular Activities of Molecular Libraries

A Conserved Salt Bridge in the G Loop of Multiple Protein Kinases Is Important for Catalysis and for In Vivo Lyn Function

The effects of Bcr-Abl on C/EBP transcription-factor regulation and neutrophilic differentiation are reversed by the Abl kinase inhibitor imatinib mesylate

Interfering with resistance to smoothened antagonists by inhibition of the PI3K pathway in medulloblastoma

Ba/F3 cells and their use in kinase drug discovery

Addendum: The Cancer Cell Line Encyclopedia enables predictive modelling of anticancer drug sensitivity

Abstract 3406: Comprehensive genomic profiling of hematologic malignancies identifies recurrent somatic splicing factor mutations in non-Hodgkin's lymphoma (NHL) and multiple myeloma (MM)

H3B-6545, a selective estrogen receptor covalent antagonist, prevents bone loss in ovariectomized Sprague-Dawley rats

Effect of a high-fat meal on the relative bioavailability of H3B-6527, a novel FGFR4 inhibitor, in healthy volunteers

Role of p21WAF1/CIP1 as an attenuator of both proliferative and drug-induced apoptotic signals in BCR-ABL-transformed hematopoietic cells

Abstract PS12-23: Development of H3B-6545, a first-in-class oral selective ER covalent antagonist (SERCA), for the treatment of ERaWT and ERaMUT breast cancer

Abstract 281: Sensitivity to splicing modulation of BCL2 family genes reveals cancer therapeutic strategies for splicing modulators

In vitro-in vivo correlation of clearance for H3B-5942, a novel selective erα covalent antagonist (SERCA)

Abstract 4269: Exome sequencing of tumor cell lines: Optimizing for cancer variants

Abstract 3013: Identification of PHF5A as a common cellular target of splicing-modulating chemical probes

Abstract 3126: H3B6527, a selective and potent FGFR4 inhibitor for FGF19-driven hepatocellular carcinoma

Abstract 126: A chemogenomic approach reveals the action of splicing modulators at the branch point adenosine binding pocket defined by the PHF5A/SF3b complex

Abstract ND10: Discovery of MRT-2359, an orally bioavailable GSPT1 molecular glue degrader, for MYC-driven cancers

H3B-8800-G0001-101: A first in human phase I study of a splicing modulator in patients with advanced myeloid malignancies

The allosteric inhibitor ABL001 enables dual targeting of BCRABL1

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