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View article: Supplementary Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer
Supplementary Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer Open
Supplementary Tables (S1-6) and Figures (S1-6)
View article: Supplementary Table 1 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Supplementary Table 1 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
PDF file - 73K
View article: Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer
Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer Open
Most EGFR exon 20 insertion (EGFRex20ins) driver mutations in non–small cell lung cancer (NSCLC) are insensitive to approved EGFR tyrosine kinase inhibitors (TKI). To address the limitations of existing therapies targeting
View article: Supplementary Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer
Supplementary Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer Open
Supplementary Tables (S1-6) and Figures (S1-6)
View article: Supplementary Figures 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Supplementary Figures 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
PDF file - 457K
View article: Data from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Data from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
Members of the fibroblast growth factor receptor family of kinases (FGFR1–4) are dysregulated in multiple cancers. Ponatinib (AP24534) is an oral multitargeted tyrosine kinase inhibitor being explored in a pivotal phase II trial in patient…
View article: Supplementary Methods, Figure Legends 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Supplementary Methods, Figure Legends 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
PDF file - 89K
View article: Data from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Data from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
Members of the fibroblast growth factor receptor family of kinases (FGFR1–4) are dysregulated in multiple cancers. Ponatinib (AP24534) is an oral multitargeted tyrosine kinase inhibitor being explored in a pivotal phase II trial in patient…
View article: Supplementary Methods, Figure Legends 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Supplementary Methods, Figure Legends 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
PDF file - 89K
View article: Supplementary Table 1 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Supplementary Table 1 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
PDF file - 73K
View article: Supplementary Figures 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models
Supplementary Figures 1-6 from Ponatinib (AP24534), a Multitargeted Pan-FGFR Inhibitor with Activity in Multiple FGFR-Amplified or Mutated Cancer Models Open
PDF file - 457K
View article: Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer
Data from Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer Open
Most EGFR exon 20 insertion (EGFRex20ins) driver mutations in non–small cell lung cancer (NSCLC) are insensitive to approved EGFR tyrosine kinase inhibitors (TKI). To address the limitations of existing therapies targeting
View article: Data from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
Data from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models Open
Purpose: Non–small cell lung cancers (NSCLCs) harboring ALK gene rearrangements (ALK+) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) crizotinib …
View article: Supplementary Methods, Supplementary Results, Supplementary Table 1, Supplementary Figures 1-8 from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
Supplementary Methods, Supplementary Results, Supplementary Table 1, Supplementary Figures 1-8 from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models Open
Supplementary Table 1. Brigatinib in vitro activity (IC50s) in a kinase panel (N=289); Supplementary Figure 1. Chemical structures of brigatinib, crizotinib, ceritinib, and alectinib; Supplementary Figure 2. Brigatinib-mediated inhibition …
View article: Supplementary Methods, Supplementary Results, Supplementary Table 1, Supplementary Figures 1-8 from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
Supplementary Methods, Supplementary Results, Supplementary Table 1, Supplementary Figures 1-8 from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models Open
Supplementary Table 1. Brigatinib in vitro activity (IC50s) in a kinase panel (N=289); Supplementary Figure 1. Chemical structures of brigatinib, crizotinib, ceritinib, and alectinib; Supplementary Figure 2. Brigatinib-mediated inhibition …
View article: Data from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
Data from The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models Open
Purpose: Non–small cell lung cancers (NSCLCs) harboring ALK gene rearrangements (ALK+) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) crizotinib …
View article: Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non–small cell lung cancer
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non–small cell lung cancer Open
In the treatment of non-small cell lung cancer (NSCLC), patients harboring exon 20 insertion mutations in the epidermal growth factor receptor (EGFR) gene (EGFR) have few effective therapies because this subset of mutants is generally resi…
View article: Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer
Mobocertinib (TAK-788): A Targeted Inhibitor of <i>EGFR</i> Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer Open
Most EGFR exon 20 insertion (EGFRex20ins) driver mutations in non–small cell lung cancer (NSCLC) are insensitive to approved EGFR tyrosine kinase inhibitors (TKI). To address the limitations of existing therapies targeting EGFR-mutated NSC…
View article: The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models Open
Purpose: Non–small cell lung cancers (NSCLCs) harboring ALK gene rearrangements (ALK+) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) crizotinib through development of se…
View article: Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase Open
In the treatment of echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase positive (ALK+) non-small-cell lung cancer (NSCLC), secondary mutations within the ALK kinase domain have emerged as a major resistance …
View article: Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery Open
Choline kinase α (ChoKα) is an enzyme involved in the synthesis of phospholipids and thereby plays key roles in regulation of cell proliferation, oncogenic transformation, and human carcinogenesis. Since several inhibitors of ChoKα display…