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View article: Supplementary Table S4 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S4 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S4: Potency against resistant clones from the ENU mutagenesis screen
View article: Supplementary Table S2 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S2 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S2: Determining Ceff,u (efficacious unbound concentration)
View article: Supplementary Figure S11 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S11 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S11: Structural basis for TRK selectivity
View article: Supplementary Figure S6 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S6 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S6: Preclinical measurements of brain penetration potential
View article: Supplementary Table S7 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S7 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S7: Crystallographic and refinement statistics
View article: Supplementary Figure S8 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S8 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S8: Similarities between wild-type ROS1 and ROS1 G2032R
View article: Supplementary Figure S9 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S9 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S9: P-loop differences between wild-type ROS1 and ROS1 G2032R
View article: Supplementary Figure S1 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S1 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S1: Determining efficacious unbound concentration (Ceff,u)
View article: Supplementary Figure S4 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S4 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S4: Bioinformatic analyses of starting cell pools from ENU mutagenesis screens
View article: Supplementary Figure S3 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S3 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S3: Residues with mutations identified in mutagenesis screens
View article: Supplementary Table S3 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S3 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S3: Number of resistant wells and distribution of ROS1 kinase-domain mutations identified in ENU mutagenesis screens
View article: Supplementary Table S5 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S5 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S5: Quantification of brain BLI from intracranial Ba/F3 CD74-ROS1 G2032R luciferase study
View article: Data from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Data from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Zidesamtinib (NVL-520) is a ROS1-selective macrocyclic tyrosine kinase inhibitor designed with the aim to address clinical challenges for patients with non–small cell lung or other cancers that are ROS1 fusion–positive. These challenges in…
View article: Supplementary Figure S5 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S5 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S5: Pharmacokinetics measurements from the intracranial study
View article: Supplementary Figure S7 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S7 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S7: ROS1 G2032R protein purification
View article: Supplementary Figure S2 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S2 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S2: Dose-response curves for 6 TKIs
View article: Supplementary Figure S12 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S12 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S12: Free-energy perturbation (FEP) workflow
View article: Supplementary Figure S10 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Figure S10 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Figure S10: Structural impact of ROS1 G2032R mutation on TKI binding
View article: Supplementary Table S6 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S6 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S6: Pharmacokinetics measurements from intracranial Ba/F3 CD74-ROS1 G2032R luciferase study
View article: Supplementary Table S1 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Supplementary Table S1 from Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Supplementary Table S1: Determining Cavg,u (clinical average unbound plasma exposure)
View article: Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations
Zidesamtinib Selective Targeting of Diverse ROS1 Drug-Resistant Mutations Open
Zidesamtinib (NVL-520) is a ROS1-selective macrocyclic tyrosine kinase inhibitor designed with the aim to address clinical challenges for patients with non–small cell lung or other cancers that are ROS1 fusion–positive. These challenges in…
View article: Data from NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations
Data from NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations Open
Three generations of tyrosine kinase inhibitors (TKI) have been approved for anaplastic lymphoma kinase (ALK) fusion–positive non–small cell lung cancer. However, none address the combined need for broad resistance coverage, brain activity…
View article: Supplementary Figures S1-S17 from NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations
Supplementary Figures S1-S17 from NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations Open
Supplementary Figure S1. Chemistry/X-ray. Supplementary Figure S2. Biochemical activity of ALK TKIs. Supplementary Figure S3. Kinome profiling of NVL-655. Supplementary Figure S4. Potency in cell viability assay. Supplementary Figure S5. M…
View article: NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations
NVL-655 Is a Selective and Brain-Penetrant Inhibitor of Diverse ALK-Mutant Oncoproteins, Including Lorlatinib-Resistant Compound Mutations Open
Three generations of tyrosine kinase inhibitors (TKI) have been approved for anaplastic lymphoma kinase (ALK) fusion–positive non–small cell lung cancer. However, none address the combined need for broad resistance coverage, brain activity…
View article: Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M<sub>4</sub> Muscarinic Acetylcholine Receptor
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M<sub>4</sub> Muscarinic Acetylcholine Receptor Open
Selective activation of the M4 muscarinic acetylcholine receptor subtype offers a novel strategy for the treatment of psychosis in multiple neurological disorders. Although the development of traditional muscarinic activators has been stym…
View article: Supplementary Figures S1-S16 from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
Supplementary Figures S1-S16 from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations Open
NVL-520 Modeling, Properties, Biochemical Activity, Cellular Activity, and In Vivo Activity
View article: Data from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
Data from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations Open
ROS1 tyrosine kinase inhibitors (TKI) have been approved (crizotinib and entrectinib) or explored (lorlatinib, taletrectinib, and repotrectinib) for the treatment of ROS1 fusion–positive cancers, although none of them simultaneously addres…
View article: Supplementary Figures S1-S16 from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
Supplementary Figures S1-S16 from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations Open
NVL-520 Modeling, Properties, Biochemical Activity, Cellular Activity, and In Vivo Activity
View article: Data from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
Data from NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations Open
ROS1 tyrosine kinase inhibitors (TKI) have been approved (crizotinib and entrectinib) or explored (lorlatinib, taletrectinib, and repotrectinib) for the treatment of ROS1 fusion–positive cancers, although none of them simultaneously addres…
View article: NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations
NVL-520 Is a Selective, TRK-Sparing, and Brain-Penetrant Inhibitor of ROS1 Fusions and Secondary Resistance Mutations Open
ROS1 tyrosine kinase inhibitors (TKI) have been approved (crizotinib and entrectinib) or explored (lorlatinib, taletrectinib, and repotrectinib) for the treatment of ROS1 fusion–positive cancers, although none of them simultaneously addres…