Siva K. Kolluri
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View article: Distinct 2-phenyl-imidazo[1, 2α] pyridine derivatives drive ER degradation and selectively impair proliferation of ER<sup>+</sup> breast cancer cells via the aryl hydrocarbon receptor
Distinct 2-phenyl-imidazo[1, 2α] pyridine derivatives drive ER degradation and selectively impair proliferation of ER<sup>+</sup> breast cancer cells via the aryl hydrocarbon receptor Open
X15695 is a 2-phenyl-imidazo[1, 2α] pyridine derivative identified as an orally active, selective oestrogen receptor (ER) degrader that inhibits the proliferation of ER + breast cancer cells. Here, we show that X15695 is an aryl hydrocarbo…
View article: Ruxolitinib mediated paradoxical JAK2 hyperphosphorylation is due to the protection of activation loop tyrosines from phosphatases
Ruxolitinib mediated paradoxical JAK2 hyperphosphorylation is due to the protection of activation loop tyrosines from phosphatases Open
Myelofibrosis (MF) in 50% of cases is driven by an activating JAK2 mutation, mostly V617F. Ruxolinitib is approved for the treatment of MF. Responses to ruxolitinib in MF are of limited duration. Unexpectedly, treatment of JAK2-V617F expre…
View article: Small Molecule Functional Converter of B-Cell Lymphoma-2 (Bcl-2) Suppresses Breast Cancer Lung Metastasis
Small Molecule Functional Converter of B-Cell Lymphoma-2 (Bcl-2) Suppresses Breast Cancer Lung Metastasis Open
The B-cell lymphoma-2 (Bcl-2) family of proteins plays a vital role in tumorigenesis. Cancer cells utilize the expression of Bcl-2 to evade therapy and develop resistance. Bcl-2 overexpression also causes cancer cells to be more invasive a…
View article: FIGURE 6 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 6 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Antitumor effects of BFC1108 in an orthotopic breast cancer model. A, BFC1108 inhibits growth of high Bcl-2–expressing MDA-MB-231 TNBC cells in vivo. A total of 106 MDA-MB-231/Bcl-2 cells were implanted in the mamm…
View article: FIGURE 3 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 3 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
BFC1108 activates intrinsic mitochondrial death pathway. A, BFC1108 suppresses the colony-forming ability of MEF cells in a Bcl-2–dependent manner. WT and Bcl-2−/− MEF cells were treated for 48 hours in a medium containin…
View article: FIGURE 4 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 4 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Interaction of BFC1108 with Bcl-2. A, Limited proteolysis of Bcl-2 loop domain in the presence of BFC1108. Purified GST-tagged Bcl-2 loop domain and GST only control were incubated with 50 µmol/L BFC1108. The proteolysis pattern of …
View article: FIGURE 3 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 3 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
BFC1108 activates intrinsic mitochondrial death pathway. A, BFC1108 suppresses the colony-forming ability of MEF cells in a Bcl-2–dependent manner. WT and Bcl-2−/− MEF cells were treated for 48 hours in a medium containin…
View article: FIGURE 6 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 6 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Antitumor effects of BFC1108 in an orthotopic breast cancer model. A, BFC1108 inhibits growth of high Bcl-2–expressing MDA-MB-231 TNBC cells in vivo. A total of 106 MDA-MB-231/Bcl-2 cells were implanted in the mamm…
View article: FIGURE 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
BFC1108 suppresses viability of multiple cancer cell types. A, Bcl-2–selective inhibition of clonogenic survival of MDA-MB-231 cells. MDA-MB-231/Vector and MDA-MB-231/Bcl-2 cells were exposed to 10 µmol/L concentration in medium con…
View article: FIGURE 4 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 4 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Interaction of BFC1108 with Bcl-2. A, Limited proteolysis of Bcl-2 loop domain in the presence of BFC1108. Purified GST-tagged Bcl-2 loop domain and GST only control were incubated with 50 µmol/L BFC1108. The proteolysis pattern of …
View article: FIGURE 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
BFC1108 suppresses viability of multiple cancer cell types. A, Bcl-2–selective inhibition of clonogenic survival of MDA-MB-231 cells. MDA-MB-231/Vector and MDA-MB-231/Bcl-2 cells were exposed to 10 µmol/L concentration in medium con…
View article: Supplemental Figure 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Supplemental Figure 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Bioluminescent imaging of data in Figure 7 for individual mouse treated with vehicle or BFC1108 is shown.
View article: FIGURE 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Bcl-2–dependent effects of BFC1108. A, Structure of BFC1108 (5-chloro-N-(2-ethoxyphenyl)-2-[(4-methoxybenzyol)amino]benzamide). B, Left: Bcl-2 expression in MDA-MB-231 cells transfected with pcDNA control vector (MDA-MB-231/V…
View article: Data from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Data from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Cancer cells exploit the expression of anti-apoptotic protein Bcl-2 to evade apoptosis and develop resistance to therapeutics. High levels of Bcl-2 leads to sequestration of pro-apoptotic proteins causing the apoptotic machinery to halt. I…
View article: Supplemental Figure 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Supplemental Figure 2 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Bioluminescent imaging of data in Figure 7 for individual mouse treated with vehicle or BFC1108 is shown.
View article: FIGURE 5 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 5 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
BFC1108 induces cell death across multiple Bcl-2–expressing TNBC cell lines to a greater extent than ABT199. Cell death percentage is calculated based upon viability assay after 72 hours treatment at the indicated BFC1108 concentrations.
View article: Data from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Data from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Cancer cells exploit the expression of anti-apoptotic protein Bcl-2 to evade apoptosis and develop resistance to therapeutics. High levels of Bcl-2 leads to sequestration of pro-apoptotic proteins causing the apoptotic machinery to halt. I…
View article: FIGURE 5 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 5 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
BFC1108 induces cell death across multiple Bcl-2–expressing TNBC cell lines to a greater extent than ABT199. Cell death percentage is calculated based upon viability assay after 72 hours treatment at the indicated BFC1108 concentrations.
View article: FIGURE 7 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 7 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Inhibition of breast cancer lung metastasis by BFC1108. A, BFC1108 suppresses the growth of lung metastasis in vivo. LMD-231 cells (200,000) stably expressing luciferase were injected into the tail vein of 6-week-old nude mic…
View article: Supplemental Figure 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Supplemental Figure 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Bcl-2 dependent apoptotic effects of BFC1108. Independent experimental replicates of data in Figure 2C are shown.
View article: FIGURE 7 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 7 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Inhibition of breast cancer lung metastasis by BFC1108. A, BFC1108 suppresses the growth of lung metastasis in vivo. LMD-231 cells (200,000) stably expressing luciferase were injected into the tail vein of 6-week-old nude mic…
View article: FIGURE 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
FIGURE 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Bcl-2–dependent effects of BFC1108. A, Structure of BFC1108 (5-chloro-N-(2-ethoxyphenyl)-2-[(4-methoxybenzyol)amino]benzamide). B, Left: Bcl-2 expression in MDA-MB-231 cells transfected with pcDNA control vector (MDA-MB-231/V…
View article: Supplemental Figure 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Supplemental Figure 1 from Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Bcl-2 dependent apoptotic effects of BFC1108. Independent experimental replicates of data in Figure 2C are shown.
View article: Identification and Characterization of a Small Molecule Bcl-2 Functional Converter
Identification and Characterization of a Small Molecule Bcl-2 Functional Converter Open
Cancer cells exploit the expression of anti-apoptotic protein Bcl-2 to evade apoptosis and develop resistance to therapeutics. High levels of Bcl-2 leads to sequestration of pro-apoptotic proteins causing the apoptotic machinery to halt. I…
View article: The Aryl Hydrocarbon Receptor-Dependent Mechanisms of 4,11-Dichloro-Bbq in Suppressing Hepatocellular Carcinoma Cell Growth
The Aryl Hydrocarbon Receptor-Dependent Mechanisms of 4,11-Dichloro-Bbq in Suppressing Hepatocellular Carcinoma Cell Growth Open
View article: Induction of Aryl Hydrocarbon Receptor-Mediated Cancer Cell-Selective Apoptosis in Triple-Negative Breast Cancer Cells by a High-Affinity Benzimidazoisoquinoline
Induction of Aryl Hydrocarbon Receptor-Mediated Cancer Cell-Selective Apoptosis in Triple-Negative Breast Cancer Cells by a High-Affinity Benzimidazoisoquinoline Open
Triple-negative breast cancer (TNBC) remains a disease with a paucity of targeted treatment opportunities. The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that is involved in a wide range of physiological pro…
View article: Tumor-Suppressive Functions of the Aryl Hydrocarbon Receptor (AhR) and AhR as a Therapeutic Target in Cancer
Tumor-Suppressive Functions of the Aryl Hydrocarbon Receptor (AhR) and AhR as a Therapeutic Target in Cancer Open
The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor involved in regulating a wide range of biological responses. A diverse array of xenobiotics and endogenous small molecules bind to the receptor and drive unique…
View article: <scp>11‐Cl‐BBQ</scp> , a select modulator of <scp>AhR</scp> ‐regulated transcription, suppresses lung cancer cell growth via activation of p53 and <scp> p27 <sup>Kip1</sup> </scp>
<span>11‐Cl‐BBQ</span> , a select modulator of <span>AhR</span> ‐regulated transcription, suppresses lung cancer cell growth via activation of p53 and <span> p27 <sup>Kip1</sup> </span> Open
Aryl hydrocarbon receptor (AhR) is a ligand‐activated transcription factor and functions as a tumour suppressor in different cancer models. In the present study, we report detailed characterization of 11‐chloro‐7H‐benzimidazo[2,1‐a]benzo[d…
View article: Leveraging a High-Throughput Screening Method to Identify Mechanisms of Individual Susceptibility Differences in a Genetically Diverse Zebrafish Model
Leveraging a High-Throughput Screening Method to Identify Mechanisms of Individual Susceptibility Differences in a Genetically Diverse Zebrafish Model Open
Understanding the mechanisms behind chemical susceptibility differences is key to protecting sensitive populations. However, elucidating gene-environment interactions (GxE) presents a daunting challenge. While mammalian models have proven …
View article: 3,3′-Diindolylmethane Exhibits Significant Metabolism after Oral Dosing in Humans
3,3′-Diindolylmethane Exhibits Significant Metabolism after Oral Dosing in Humans Open