Publications
71 results found
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S2. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Analysis of ICEC0942 treatment of MCF7 cells.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S7. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Combinatorial inhibition of breast cancer cells with a combination of ICEC0942 and anti-estrogens.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S2. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Analysis of ICEC0942 treatment of MCF7 cells.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S1. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>In vitro kinase assays demonstrate selectivity of ICEC0942 for CDK7.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S4. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>ADME analysis, oral bioavailability and distribution of ICEC0942.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S1. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>In vitro kinase assays demonstrate selectivity of ICEC0942 for CDK7.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S4. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>ADME analysis, oral bioavailability and distribution of ICEC0942.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S6. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Pharmacokinetic determination of ICEC0942 plasma and tumor concentrations at different doses and over time.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Information from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Figure legends for supplementary Figures</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S3. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Cell Cycle analysis of MCF7 cells treated with ICEC0942.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S6. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Pharmacokinetic determination of ICEC0942 plasma and tumor concentrations at different doses and over time.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S5. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Oral administration of ICEC0942 inhibits cyclin-dependent kinase substrate phosphorylation in mouse peripheral blood mononuclear cells.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S3. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Cell Cycle analysis of MCF7 cells treated with ICEC0942.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S5. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Oral administration of ICEC0942 inhibits cyclin-dependent kinase substrate phosphorylation in mouse peripheral blood mononuclear cells.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Information from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Figure legends for supplementary Figures</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Supplementary Figure S7. from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><p>Combinatorial inhibition of breast cancer cells with a combination of ICEC0942 and anti-estrogens.</p></jats:p>
Patel H, Periyasamy M, Sava GP, et al., 2023, Data from ICEC0942, an Orally Bioavailable Selective Inhibitor of CDK7 for Cancer Treatment
<jats:p><div>Abstract<p>Recent reports indicate that some cancer types are especially sensitive to transcription inhibition, suggesting that targeting the transcriptional machinery provides new approaches to cancer treatment. Cyclin-dependent kinase (CDK)7 is necessary for transcription, and acts by phosphorylating the C-terminal domain (CTD) of RNA polymerase II (PolII) to enable transcription initiation. CDK7 additionally regulates the activities of a number of transcription factors, including estrogen receptor (ER)-α. Here we describe a new, orally bioavailable CDK7 inhibitor, ICEC0942. It selectively inhibits CDK7, with an IC<sub>50</sub> of 40 nmol/L; IC<sub>50</sub> values for CDK1, CDK2, CDK5, and CDK9 were 45-, 15-, 230-, and 30-fold higher. <i>In vitro</i> studies show that a wide range of cancer types are sensitive to CDK7 inhibition with GI<sub>50</sub> values ranging between 0.2 and 0.3 μmol/L. In xenografts of both breast and colorectal cancers, the drug has substantial antitumor effects. In addition, combination therapy with tamoxifen showed complete growth arrest of ER-positive tumor xenografts. Our findings reveal that CDK7 inhibition provides a new approach, especially for ER-positive breast cancer and identify ICEC0942 as a prototype drug with potential utility as a single agent or in combination with hormone therapies for breast cancer. ICEC0942 may also be effective in other cancers that display characteristics of transcription factor addiction, such as acute leukaemia and small-cell lung cancer. <i>Mol Cancer Ther; 17(6); 1156–66. ©2018 AACR</i>.</p></div></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S4 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Significant CHART-seq SCIRT peaks identified using HOMER</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S8 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Sequence of primers used in the study</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S4 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Significant CHART-seq SCIRT peaks identified using HOMER</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Supplementary Data from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Supplementary material and methods</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S6 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Significant marker genes of cluster 3 after scRNA-seq analysis of Breast Cancer primary samples</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S6 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Significant marker genes of cluster 3 after scRNA-seq analysis of Breast Cancer primary samples</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Supplementary Data from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Supplementary Figures 1-15</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S7 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Top 100 gene significantly up-regulated upon siSCIRT treatment (Overlap between siSCIRT #1 and siSCIRT #2). Genes are ranked from the most up-regulated to the least up-regulated.</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Supplementary Data from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Supplementary Figures 1-15</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S8 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Sequence of primers used in the study</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Supplementary Data from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Supplementary material and methods</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S1 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Differential gene expression DESeq2 analysis for 16h Spheres vs Adh (Sheet #1) and 5d Spheres vs Adh</p></jats:p>
Zagorac S, de Giorgio A, Dabrowska A, et al., 2023, Table S5 from SCIRT lncRNA Restrains Tumorigenesis by Opposing Transcriptional Programs of Tumor-Initiating Cells
<jats:p><p>Differential gene expression DESeq2 analysis for siEZH2 vs siNC.</p></jats:p>
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