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Avapritinib in advanced PDGFRA D842V-mutant gastrointestinal stromal tumour (NAVIGATOR): a multicentre, open-label, phase 1 trial

The lancet oncology, 2020-07, Vol.21 (7), p.935-946

2020

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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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MM-151 overcomes acquired resistance to cetuximab and panitumumab in colorectal cancers harboring EGFR extracellular domain mutations

Science translational medicine, 2016-02, Vol.8 (324), p.324ra14

2016

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Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

Cancer discovery, 2024-02, Vol.14 (2), p.240-257

2024

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Enhanced Targeting of the EGFR Network with MM-151, an Oligoclonal Anti-EGFR Antibody Therapeutic

Molecular cancer therapeutics, 2015-07, Vol.14 (7), p.1625-1636

2015

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Heat-shock protein 70 inhibits apoptosis by preventing recruitment of procaspase-9 to the Apaf-1 apoptosome

Nature cell biology, 2000-08, Vol.2 (8), p.469-475

2000

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Ordering the Cytochrome c-Initiated Caspase Cascade: Hierarchical Activation of Caspases-2, -3, -6, -7, -8, and -10 in a Caspase-9-Dependent Manner

The Journal of cell biology, 1999-01, Vol.144 (2), p.281-292

1999

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On the edge of validation--cancer protease fibroblast activation protein

Mini reviews in medicinal chemistry, 2008-06, Vol.8 (7), p.719-727

2008

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Selective Inhibition of Fibroblast Activation Protein Protease Based on Dipeptide Substrate Specificity

The Journal of biological chemistry, 2006-03, Vol.281 (11), p.7437-7444

2006

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Synthesis and structure–activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP

Bioorganic & medicinal chemistry letters, 2007-03, Vol.17 (5), p.1438-1442

2007

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Caspase-3 Is the Primary Activator of Apoptotic DNA Fragmentation via DNA Fragmentation Factor-45/Inhibitor of Caspase-activated DNase Inactivation

The Journal of biological chemistry, 1999-10, Vol.274 (43), p.30651-30656

1999

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Targeting kinases with precision

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

2018

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Distinct Caspase Cascades Are Initiated in Receptor-mediated and Chemical-induced Apoptosis

The Journal of biological chemistry, 1999-02, Vol.274 (8), p.5053-5060

1999

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Pro-caspase-3 Is a Major Physiologic Target of Caspase-8

The Journal of biological chemistry, 1998-10, Vol.273 (42), p.27084-27090

1998

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Apoptosis: Letting Slip The Dogs Of War

Current biology, 2002-03, Vol.12 (5), p.R177-R179

2002

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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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Granzyme B-mediated Apoptosis Proceeds Predominantly through a Bcl-2-inhibitable Mitochondrial Pathway

The Journal of biological chemistry, 2001-04, Vol.276 (15), p.12060-12067

2001

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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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Defective Cytochrome c-dependent Caspase Activation in Ovarian Cancer Cell Lines due to Diminished or Absent Apoptotic Protease Activating Factor-1 Activity

The Journal of biological chemistry, 2001-09, Vol.276 (36), p.34244-34251

2001

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Ala657 and Conserved Active Site Residues Promote Fibroblast Activation Protein Endopeptidase Activity via Distinct Mechanisms of Transition State Stabilization

Biochemistry (Easton), 2007-04, Vol.46 (15), p.4598-4605

2007

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First-in-human global multi-center study of RLY-2608, a pan-mutant and isoform-selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer

Journal of clinical oncology, 2022-06, Vol.40 (16_suppl), p.TPS1124-TPS1124

2022

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Suicidal tendencies: apoptotic cell death by caspase family proteinases

The Journal of biological chemistry, 1999-07, Vol.274 (29), p.20049-20052

1999

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First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant FGF19 Signaling as a Driver Event in Hepatocellular Carcinoma

Avapritinib in advanced PDGFRA D842V-mutant gastrointestinal stromal tumour (NAVIGATOR): a multicentre, open-label, phase 1 trial

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

MM-151 overcomes acquired resistance to cetuximab and panitumumab in colorectal cancers harboring EGFR extracellular domain mutations

RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations

Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

Enhanced Targeting of the EGFR Network with MM-151, an Oligoclonal Anti-EGFR Antibody Therapeutic

Heat-shock protein 70 inhibits apoptosis by preventing recruitment of procaspase-9 to the Apaf-1 apoptosome

Ordering the Cytochrome c-Initiated Caspase Cascade: Hierarchical Activation of Caspases-2, -3, -6, -7, -8, and -10 in a Caspase-9-Dependent Manner

On the edge of validation--cancer protease fibroblast activation protein

Selective Inhibition of Fibroblast Activation Protein Protease Based on Dipeptide Substrate Specificity

Synthesis and structure–activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP

Caspase-3 Is the Primary Activator of Apoptotic DNA Fragmentation via DNA Fragmentation Factor-45/Inhibitor of Caspase-activated DNase Inactivation

Targeting kinases with precision

Distinct Caspase Cascades Are Initiated in Receptor-mediated and Chemical-induced Apoptosis

Pro-caspase-3 Is a Major Physiologic Target of Caspase-8

Apoptosis: Letting Slip The Dogs Of War

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

Landscape of Acquired Resistance to Osimertinib in EGFR -Mutant NSCLC and Clinical Validation of Combined EGFR and RET Inhibition with Osimertinib and BLU-667 for Acquired RET Fusion

Granzyme B-mediated Apoptosis Proceeds Predominantly through a Bcl-2-inhibitable Mitochondrial Pathway

A precision therapy against cancers driven by KIT/PDGFRA mutations

Defective Cytochrome c-dependent Caspase Activation in Ovarian Cancer Cell Lines due to Diminished or Absent Apoptotic Protease Activating Factor-1 Activity

Ala657 and Conserved Active Site Residues Promote Fibroblast Activation Protein Endopeptidase Activity via Distinct Mechanisms of Transition State Stabilization

First-in-human global multi-center study of RLY-2608, a pan-mutant and isoform-selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer

Suicidal tendencies: apoptotic cell death by caspase family proteinases

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