Search Results - "COLEMAN, Kevin G"
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PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
Published in Proceedings of the National Academy of Sciences - PNAS (28-06-2016)“…Prostate cancer has the second highest incidence among cancers in men worldwide and is the second leading cause of cancer deaths of men in the United States…”
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Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Published in Journal of medicinal chemistry (25-01-2018)“…Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent…”
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PARP inhibitor synthetic lethality in ATM biallelic mutant cancer cell lines is associated with BRCA1/2 and RAD51 downregulation
Published in Frontiers in oncology (14-05-2024)“…Ataxia telangiectasia-mutated (ATM) kinase is a central regulator of the DNA damage response (DDR) signaling pathway, and its function is critical for the…”
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Proteolysis-Targeting Chimeras: Harnessing the Ubiquitin-Proteasome System to Induce Degradation of Specific Target Proteins
Published in Annual review of cancer biology (04-03-2018)“…The ubiquitin-proteasome system plays a central role in regulating protein homeostasis in mammalian cells. It is a multistep process involving the…”
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Dwarfism, impaired skin development, skeletal muscle atrophy, delayed bone development, and impeded adipogenesis in mice lacking Akt1 and Akt2
Published in Genes & development (01-06-2003)“…To elucidate the functions of the serine/threonine kinase Akt/PKB in vivo, we generated mice lacking both akt1 and akt2 genes. Akt1/Akt2 double-knockout (DKO)…”
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Protein targeting chimeric molecules specific for bromodomain and extra-terminal motif family proteins are active against pre-clinical models of multiple myeloma
Published in Leukemia (01-10-2018)“…Bromodomain and extraterminal (BET) domain containing protein (BRD)-4 modulates the expression of oncogenes such as c-myc , and is a promising therapeutic…”
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Biochemical and pharmacological characterization of human c-Met neutralizing monoclonal antibody CE-355621
Published in mAbs (01-11-2012)“…The c-Met proto-oncogene is a multifunctional receptor tyrosine kinase that is stimulated by its ligand, hepatocyte growth factor (HGF), to induce cell growth,…”
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Severe diabetes, age-dependent loss of adipose tissue, and mild growth deficiency in mice lacking Akt2/PKB beta
Published in The Journal of clinical investigation (01-07-2003)“…The serine/threonine kinase Akt/PKB plays key roles in the regulation of cell growth, survival, and metabolism. It remains unclear, however, whether the…”
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Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor
Published in Cancer research (Chicago, Ill.) (15-10-2007)“…Amplification and overexpression of erbB2 (Her-2/neu) proto-oncogene has been linked to human malignancies including tumors of the breast, ovary, and stomach…”
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Abstract 2379: Elaborating the mechanism of PARP synthetic lethality in ATM loss
Published in Cancer research (Chicago, Ill.) (15-08-2020)“…PARP inhibitors have transformed the treatment for ovarian cancer, which is known to have high incidence of homologous recombination (HR) deficiency through…”
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Expression of engrailed proteins in arthropods, annelids, and chordates
Published in Cell (08-09-1989)“…engrailed is a homeobox gene that has an important role in Drosophila segmentation. Genes homologous to engrailed have been identified in several other…”
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Phosphorylation of serine residues in histidine-tag sequences attached to recombinant protein kinases: A cause of heterogeneity in mass and complications in function
Published in Protein expression and purification (01-12-2005)“…High-level recombinant expression of protein kinases in eukaryotic cells or Escherichia coli commonly gives products that are phosphorylated by autocatalysis…”
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Identification of CDK4 Sequences Involved in Cyclin D1 and p16 Binding
Published in The Journal of biological chemistry (25-07-1997)“…Activation of CDK4 is regulated, in part, by its association with a D-type cyclin. Conversely, CDK4 activity is inhibited when it is bound to the…”
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Abstract A091: Targeting homologous recombination repair defects in lung cancer
Published in Molecular cancer therapeutics (01-12-2019)“…Non-Small Cell Lung Cancer (NSCLC) is the leading cause of cancer related mortality worldwide, and accounts for 80-85% of all lung cancer diagnoses. While…”
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Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells
Published in Leukemia (01-09-2017)“…The PROTAC (proteolysis-targeting chimera) ARV-825 recruits bromodomain and extraterminal (BET) proteins to the E3 ubiquitin ligase cereblon, leading to…”
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Abstract 3242: Triple checkpoint blockade targeting PD-1, TIM-3, and LAG-3 reinvigorates ovarian cancer-infiltrating T cells by increasing T cell polyfunctionality and effector function
Published in Cancer research (Chicago, Ill.) (01-07-2019)“…Co-expression of immune checkpoint receptors (ICRs) PD-1, TIM-3, and LAG-3 characterizes chronically activated and exhausted tumor-infiltrating T cells (TILs),…”
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Abstract 6175: CDK8 inhibition potentiates the efficacy of niraparib in homologous recombination proficient cancer cell lines
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…While cyclin dependent kinases (CDKs) were originally implicated in cell cycle regulation, several CDKs including CDK7, CDK8, and CDK9 play critical roles in…”
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Severe diabetes, age-dependent loss of adipose tissue, and mild growth deficiency in mice lacking Akt2/PKB beta
Published in The Journal of clinical investigation (01-07-2003)“…The serine/threonine kinase Akt/PKB plays key roles in the regulation of cell growth, survival, and metabolism. It remains unclear, however, whether the…”
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Abstract 5067: BET protein proteolysis targeting chimera (BETP-PROTACs) exert more potent activity than BETP bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm (MPN) secondary (s) AML cells
Published in Cancer research (Chicago, Ill.) (01-07-2017)“…In BCR-ABL1-negative myeloproliferative neoplasms with myelofibrosis (MPN-MF) transformation to AML (sAML) occurs in up to 20% of patients. Ruxolitinib (R) is…”
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Temperature-sensitive lethal mutations on yeast chromosome I appear to define only a small number of genes [Saccharomyces cerevisiae]
Published in Genetics (Austin) (01-09-1984)“…A method was developed for isolating large numbers of mutations on chromosome I of the yeast Saccharomyces cerevisiae. A strain monosomic for chromosome I…”
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