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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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Loss of function JAK1 mutations occur at high frequency in cancers with microsatellite instability and are suggestive of immune evasion

PloS one, 2017-11, Vol.12 (11), p.e0176181-e0176181

2017

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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‑N2‑(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)‑N4‑(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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Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex

Nature communications, 2017-05, Vol.8 (1), p.15522-15522, Article 15522

2017

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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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Trisomy 12 and elevated GLI1 and PTCH1 transcript levels are biomarkers for Hedgehog-inhibitor responsiveness in CLL

Blood, 2012-01, Vol.119 (4), p.997-1007

2012

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

Nature communications, 2019-06, Vol.10 (1), p.2527-2527, Article 2527

2019

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Allosteric inhibition of BCR-ABL

Cell cycle (Georgetown, Tex.), 2010-09, Vol.9 (18), p.3734-3738

2010

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SRC family kinases: potential targets for the treatment of human cancer and leukemia

Current pharmaceutical design, 2003-01, Vol.9 (25), p.2043

2003

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

Nature (London), 2012-03, Vol.483 (7391), p.603-607

2012

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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 Src Family Kinase Hck Interacts with Bcr-Abl by a Kinase-independent Mechanism and Phosphorylates the Grb2-binding Site of Bcr

The Journal of biological chemistry, 1997-12, Vol.272 (52), p.33260-33270

1997

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The R882H DNMT3A hot spot mutation stabilizes the formation of large DNMT3A oligomers with low DNA methyltransferase activity

The Journal of biological chemistry, 2019-11, Vol.294 (45), p.16966-16977

2019

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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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Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA)

Cancer chemotherapy and pharmacology, 2019-01, Vol.83 (1), p.151-160

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

Loss of function JAK1 mutations occur at high frequency in cancers with microsatellite instability and are suggestive of immune evasion

Cancer-Associated SF3B1 Hotspot Mutations Induce Cryptic 3′ Splice Site Selection through Use of a Different Branch Point

Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex

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

Trisomy 12 and elevated GLI1 and PTCH1 transcript levels are biomarkers for Hedgehog-inhibitor responsiveness in CLL

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

Allosteric inhibition of BCR-ABL

SRC family kinases: potential targets for the treatment of human cancer and leukemia

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

The Src Family Kinase Hck Interacts with Bcr-Abl by a Kinase-independent Mechanism and Phosphorylates the Grb2-binding Site of Bcr

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

The R882H DNMT3A hot spot mutation stabilizes the formation of large DNMT3A oligomers with low DNA methyltransferase activity

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

Nonclinical pharmacokinetics and in vitro metabolism of H3B-6545, a novel selective ERα covalent antagonist (SERCA)

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)

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