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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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The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1

Nature (London), 2017-03, Vol.543 (7647), p.733-737

2017

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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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Expansion of Bcr-Abl-Positive Leukemic Stem Cells Is Dependent on Hedgehog Pathway Activation

Cancer cell, 2008-09, Vol.14 (3), p.238-249

2008

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H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma

Cancer research (Chicago, Ill.), 2017-12, Vol.77 (24), p.6999-7013

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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Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators

Nature communications, 2019-01, Vol.10 (1), p.137-137, Article 137

2019

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

Nature communications, 2017-07, Vol.8 (1), p.103-14, Article 103

2017

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Essential role of stromally induced hedgehog signaling in B-cell malignancies

Nature medicine, 2007-08, Vol.13 (8), p.944-951

2007

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Loss of the tumor suppressor Snf5 leads to aberrant activation of the Hedgehog-Gli pathway

Nature medicine, 2010-12, Vol.16 (12), p.1429-1433

2010

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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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Protein Kinase C Inhibitor Sotrastaurin Selectively Inhibits the Growth of CD79 Mutant Diffuse Large B-Cell Lymphomas

Cancer research (Chicago, Ill.), 2011-04, Vol.71 (7), p.2643-2653

2011

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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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NAMPT Is the Cellular Target of STF-31-Like Small-Molecule Probes

ACS chemical biology, 2014-10, Vol.9 (10), p.2247-2254

2014

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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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The Polycomb Group Protein Bmi-1 Is Essential for the Growth of Multiple Myeloma Cells

Cancer research (Chicago, Ill.), 2010-07, Vol.70 (13), p.5528-5538

2010

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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.2043-2059

2003

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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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Novel SF3B1 in-frame deletions result in aberrant RNA splicing in CLL patients

Blood advances, 2017-06, Vol.1 (15), p.995-1000

2017

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Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

Nature (London), 2016-07, Vol.535 (7610), p.148-152

2016

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H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers

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

The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1

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

Expansion of Bcr-Abl-Positive Leukemic Stem Cells Is Dependent on Hedgehog Pathway Activation

H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma

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

Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators

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

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

Essential role of stromally induced hedgehog signaling in B-cell malignancies

Loss of the tumor suppressor Snf5 leads to aberrant activation of the Hedgehog-Gli pathway

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

Protein Kinase C Inhibitor Sotrastaurin Selectively Inhibits the Growth of CD79 Mutant Diffuse Large B-Cell Lymphomas

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

NAMPT Is the Cellular Target of STF-31-Like Small-Molecule Probes

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

The Polycomb Group Protein Bmi-1 Is Essential for the Growth of Multiple Myeloma Cells

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

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

Novel SF3B1 in-frame deletions result in aberrant RNA splicing in CLL patients

Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

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