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The landscape of kinase fusions in cancer

Nature communications, 2014-09, Vol.5 (1), p.4846-4846, Article 4846

2014

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Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma

Cancer discovery, 2019-12, Vol.9 (12), p.1686-1695

2019

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Selective and potent Raf inhibitors paradoxically stimulate normal cell proliferation and tumor growth

Molecular cancer therapeutics, 2010-08, Vol.9 (8), p.2399-2410

2010

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First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway

Cancer discovery, 2015-04, Vol.5 (4), p.424-437

2015

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Precision Targeted Therapy with BLU-667 for RET -Driven Cancers

Cancer discovery, 2018-07, Vol.8 (7), p.836-849

2018

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A precision therapy against cancers driven by KIT/PDGFRA mutations

Science translational medicine, 2017-11, Vol.9 (414)

2017

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Targeting kinases with precision

Molecular & cellular oncology, 2018-05, Vol.5 (3), p.e1435183-e1435183

2018

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Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor

Journal of medicinal chemistry, 2007-02, Vol.50 (4), p.611-626

2007

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X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex

Cell, 1995-08, Vol.82 (3), p.507-522

1995

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Co-crystal structure of TBP recognizing the minor groove of a TATA element

Nature (London), 1993-10, Vol.365 (6446), p.520-527

1993

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An ALK2 inhibitor, BLU-782, prevents heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva

Science translational medicine, 2024-05, Vol.16 (749), p.eabp8334

2024

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Evaluation of STK17B as a cancer immunotherapy target utilizing highly potent and selective small molecule inhibitors

Frontiers in immunology, 2024-10, Vol.15

2024

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Selective Inhibitors of the Mutant B-Raf Pathway: Discovery of a Potent and Orally Bioavailable Aminoisoquinoline

Journal of medicinal chemistry, 2009-10, Vol.52 (20), p.6189-6192

2009

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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors

Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (10), p.2886-2889

2007

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Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors

Journal of medicinal chemistry, 2007-09, Vol.50 (18), p.4351-4373

2007

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Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (10), p.2215-2234

2016

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Discovery of Potent and Highly Selective Thienopyridine Janus Kinase 2 Inhibitors

Journal of medicinal chemistry, 2011-12, Vol.54 (24), p.8440-8450

2011

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Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.2641-2641

2016

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Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (15), p.4967-4974

2012

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Hepatitis C virus NS3 RNA helicase domain with a bound oligonucleotide: the crystal structure provides insights into the mode of unwinding

Structure (London), 1998-01, Vol.6 (1), p.89-100

1998

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Corrigendum to “Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling” [Bioorg. Med. Chem. 24 (2016) 2215–2234]

Bioorganic & medicinal chemistry, 2016-07, Vol.24 (13), p.3093-3093

2016

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Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors

Structure (London), 1999-06, Vol.7 (6), p.651-661

1999

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Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

Bioorganic & medicinal chemistry letters, 2009-01, Vol.19 (2), p.424-427

2009

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Discovery of triazine-benzimidazoles as selective inhibitors of mTOR

Bioorganic & medicinal chemistry letters, 2011-04, Vol.21 (7), p.2064-2070

2011

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The landscape of kinase fusions in cancer

Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma

Selective and potent Raf inhibitors paradoxically stimulate normal cell proliferation and tumor growth

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway

Precision Targeted Therapy with BLU-667 for RET -Driven Cancers

A precision therapy against cancers driven by KIT/PDGFRA mutations

Targeting kinases with precision

Evolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor

X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex

Co-crystal structure of TBP recognizing the minor groove of a TATA element

An ALK2 inhibitor, BLU-782, prevents heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva

Evaluation of STK17B as a cancer immunotherapy target utilizing highly potent and selective small molecule inhibitors

Selective Inhibitors of the Mutant B-Raf Pathway: Discovery of a Potent and Orally Bioavailable Aminoisoquinoline

Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors

Design, Synthesis, and Evaluation of Orally Active Benzimidazoles and Benzoxazoles as Vascular Endothelial Growth Factor-2 Receptor Tyrosine Kinase Inhibitors

Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling

Discovery of Potent and Highly Selective Thienopyridine Janus Kinase 2 Inhibitors

Abstract 2641: The development of potent, selective RET inhibitors that target both wild-type RET and prospectively identified resistance mutations to multi-kinase inhibitors

Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors

Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido[5′,4′:5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, SAR, and In Vivo Anti-Inflammatory Activity

Hepatitis C virus NS3 RNA helicase domain with a bound oligonucleotide: the crystal structure provides insights into the mode of unwinding

Corrigendum to “Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling” [Bioorg. Med. Chem. 24 (2016) 2215–2234]

Structural analysis of the lymphocyte-specific kinase Lck in complex with non-selective and Src family selective kinase inhibitors

Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase

Discovery of triazine-benzimidazoles as selective inhibitors of mTOR

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