Michael D. Shultz
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View article: Transaminases Provide Key Chiral Building Blocks for the Synthesis of Selective M1/M4 Agonists
Transaminases Provide Key Chiral Building Blocks for the Synthesis of Selective M1/M4 Agonists Open
We have developed a chiral route toward the synthesis of muscarinic M4 agonists that was enabled by the biocatalytic synthesis of the key spirocyclic diamine building blocks 10 and 12. Using these bifunctional compounds we were able to opt…
View article: Data from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Data from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
Two splice variants derived from the Bcl-x gene via alternative 5′ splice site selection (5′SS) are proapoptotic Bcl-x(s) and antiapoptotic Bcl-x(L). Previously, our laboratory showed that apoptotic signaling pathways regulated the alterna…
View article: Supplementary Table 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Table 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Table 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Table 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Table 3 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Table 3 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Table 3 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Table 3 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Figure 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Figure 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Figure 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Figure 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Figure 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Figure 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
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View article: Supplementary Table 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Table 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
PDF file - 1.1MB
View article: Supplementary Table 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Table 1 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
PDF file - 1.7MB
View article: Data from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Data from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
Two splice variants derived from the Bcl-x gene via alternative 5′ splice site selection (5′SS) are proapoptotic Bcl-x(s) and antiapoptotic Bcl-x(L). Previously, our laboratory showed that apoptotic signaling pathways regulated the alterna…
View article: Supplementary Figure 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA
Supplementary Figure 2 from The Proto-oncogene PKCι Regulates the Alternative Splicing of Bcl-x Pre-mRNA Open
PDF file - 188K
View article: Supplemental Figure Legends from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Supplemental Figure Legends from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Supplemental Figure Legends for Supplemental Figures 1 through 12.
View article: Data from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Data from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Alternate RNA processing of caspase-9 generates the splice variants caspase 9a (C9a) and caspase 9b (C9b). C9b lacks a domain present in C9a, revealing a tumorigenic function that drives the phenotype of non–small cell lung cancer (NSCLC) …
View article: Data from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Data from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Alternate RNA processing of caspase-9 generates the splice variants caspase 9a (C9a) and caspase 9b (C9b). C9b lacks a domain present in C9a, revealing a tumorigenic function that drives the phenotype of non–small cell lung cancer (NSCLC) …
View article: Supplemental Methods from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Supplemental Methods from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Methods used for Supplemental Data only: WST-1 cell proliferation assay, Ki-67 mmunohistochemical analysis
View article: Supplemental Figures and Tables from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Supplemental Figures and Tables from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Supplemental Figure 1: Larger legend table for symbols in fig 1A. Supplemental Figure 2: The expression of BIRC5, CDKN1A, CXCL1 and IER3 correlates with expression of C9b, but not C9a, in human NSCLC tissues. Supplemental Figure 3: Down-re…
View article: Supplemental Figures and Tables from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Supplemental Figures and Tables from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Supplemental Figure 1: Larger legend table for symbols in fig 1A. Supplemental Figure 2: The expression of BIRC5, CDKN1A, CXCL1 and IER3 correlates with expression of C9b, but not C9a, in human NSCLC tissues. Supplemental Figure 3: Down-re…
View article: Supplemental Methods from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Supplemental Methods from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Methods used for Supplemental Data only: WST-1 cell proliferation assay, Ki-67 mmunohistochemical analysis
View article: Supplemental Figure Legends from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis
Supplemental Figure Legends from Caspase-9b Interacts Directly with cIAP1 to Drive Agonist-Independent Activation of NF-κB and Lung Tumorigenesis Open
Supplemental Figure Legends for Supplemental Figures 1 through 12.
View article: The effects of stress on employee tendency to paticipate in safety under three cognitive biases
The effects of stress on employee tendency to paticipate in safety under three cognitive biases Open
This study's overarching goal was to explore the effect stress has on employee safety decision-making under three safety participation hindering cognitive biases. Safety research often involves analysis on injuries and illnesses after occu…
View article: Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer
Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer Open
SHP2 is a nonreceptor protein tyrosine phosphatase encoded by the PTPN11 gene and is involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also plays an important role in the programed cell death pathway (PD-1/PD…
View article: Correction to Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors
Correction to Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors Open
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to Optimization of Fused Bicyclic Allosteric SHP2 InhibitorsJeffrey T. BagdanoffJeffrey T. BagdanoffMore by Jeffrey T. Bagdanoff,…
View article: Correction to 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors
Correction to 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors Open
ADVERTISEMENT RETURN TO ISSUEPREVAddition/CorrectionNEXTORIGINAL ARTICLEThis notice is a correctionCorrection to 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 InhibitorsPatrick SarverPatrick SarverMore by …
View article: Dual Allosteric Inhibition of SHP2 Phosphatase
Dual Allosteric Inhibition of SHP2 Phosphatase Open
SHP2 is a cytoplasmic protein tyrosine phosphatase encoded by the PTPN11 gene and is involved in cell proliferation, differentiation, and survival. Recently, we reported an allosteric mechanism of inhibition that stabilizes the auto-inhibi…
View article: Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor
Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor Open
Inhibition of mutant IDH1 is being evaluated clinically as a promising treatment option for various cancers with hotspot mutation at Arg132. Having identified an allosteric, induced pocket of IDH1R132H, we have explored 3-pyrimidin-4-yl-ox…
View article: Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy Open
Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2), are associated with several tumor types. EZH2 inhibitor, EPZ-6438 (tazemetostat), demonstrated clinical efficacy in p…
View article: Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase Open
PRC2 is a multisubunit methyltransferase involved in epigenetic regulation of early embryonic development and cell growth. The catalytic subunit EZH2 methylates primarily lysine 27 of histone H3, leading to chromatin compaction and repress…