Search Results - "Liu, Phillip C."
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INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models
Published in PloS one (21-04-2020)“…Alterations in fibroblast growth factor receptor (FGFR) genes have been identified as potential driver oncogenes. Pharmacological targeting of FGFRs may…”
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Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor
Published in Journal of medicinal chemistry (12-08-2021)“…Aberrant activation of FGFR has been linked to the pathogenesis of many tumor types. Selective inhibition of FGFR has emerged as a promising approach for…”
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Deciphering human heat shock transcription factor 1 regulation via post-translational modification in yeast
Published in PloS one (06-01-2011)“…Heat shock transcription factor 1 (HSF1) plays an important role in the cellular response to proteotoxic stresses. Under normal growth conditions HSF1 is…”
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Potent Benzimidazole Sulfonamide Protein Tyrosine Phosphatase 1B Inhibitors Containing the Heterocyclic (S)-Isothiazolidinone Phosphotyrosine Mimetic
Published in Journal of medicinal chemistry (29-06-2006)“…Potent nonpeptidic benzimidazole sulfonamide inhibitors of protein tyrosine phosphatase 1B (PTP1B) were derived from the optimization of a tripeptide…”
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Benzothiazole benzimidazole ( S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors
Published in Bioorganic & medicinal chemistry letters (01-02-2007)“…Benzothiazole benzimidazole ( S)-isothiazolidinone (( S)-IZD) derivatives 5 were discovered through a peptidomimetic modification of the tripeptide ( S)-IZD…”
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Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines
Published in Bioorganic & medicinal chemistry letters (2008)“…The structure-based design and synthesis of isothiazolidinone (IZD) inhibitors of PTP1B containing imidazoles and imidazolines and their modification to…”
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Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: Synthesis and structure–activity relationships of a peptide scaffold
Published in Bioorganic & medicinal chemistry (01-09-2006)“…The structure-based design and discovery of the isothiazolidinone (IZD) heterocycle as a mimic of phosphotyrosine (pTyr) has led to the identification of novel…”
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Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor
Published in Cancer discovery (02-06-2022)“…Blocking the activity of the programmed cell death protein 1 (PD-1) inhibitory receptor with therapeutic antibodies against either the ligand (PD-L1) or PD-1…”
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Targeting MYCN-expressing triple-negative breast cancer with BET and MEK inhibitors
Published in Science translational medicine (11-03-2020)“…Triple-negative breast cancer (TNBC) is an aggressive form of breast cancer that does not respond to endocrine therapy or human epidermal growth factor…”
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The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies
Published in Clinical cancer research (01-01-2019)“…Bromodomain and extraterminal domain (BET) proteins regulate the expression of many cancer-associated genes and pathways; BET inhibitors have demonstrated…”
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Novel stress-responsive genes EMG1 and NOP14 encode conserved, interacting proteins required for 40S ribosome biogenesis
Published in Molecular biology of the cell (01-11-2001)“…Under stressful conditions organisms adjust the synthesis, processing, and trafficking of molecules to allow survival from and recovery after stress. In…”
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Validation of standards for quantitative assessment of JAK2 c.1849G>T (p.V617F) allele burden analysis in clinical samples
Published in Genetic testing and molecular biomarkers (01-05-2013)“…The substitution of valine with phenylalanine at amino acid 617 of the Janus kinase 2 (JAK2) gene (JAK2 p.V617F) occurs in a high proportion of patients with…”
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BET Inhibition Enhances the Antileukemic Activity of Low-dose Venetoclax in Acute Myeloid Leukemia
Published in Clinical cancer research (15-01-2021)“…The BCL2 inhibitor, venetoclax, has transformed clinical care in acute myeloid leukemia (AML). However, subsets of patients do not respond or eventually…”
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High-throughput determination of mode of inhibition in lead identification and optimization
Published in Journal of biomolecular screening (01-03-2007)“…After finishing the primary high-throughput screening, the screening team is often faced with thousands of hits to be evaluated further. Effective filtering of…”
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Efficacy of Novel Bromodomain and Extraterminal Inhibitors in Combination with Chemotherapy for Castration-Resistant Prostate Cancer
Published in European urology oncology (01-06-2021)“…Chemotherapy is the treatment of choice for metastatic castration-resistant prostate cancer (mCRPC) nonresponsive to androgen receptor–targeted therapies…”
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Identification of ADAM10 as a major source of HER2 ectodomain sheddase activity in HER2 overexpressing breast cancer cells
Published in Cancer biology & therapy (01-06-2006)“…ALL AUTHORS: Phillip C.C. Liu, Xiangdong Liu, Yanlong Li, Maryanne Covington, Richard Wynn, Reid Huber, Milton Hillman, Gengjie Yang, Dawn Ellis, Cindy…”
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Combined Inhibition of Janus Kinase 1/2 for the Treatment of JAK2V617F-Driven Neoplasms: Selective Effects on Mutant Cells and Improvements in Measures of Disease Severity
Published in Clinical cancer research (15-11-2009)“…Purpose: Deregulation of the Janus kinase-signal transducers and activators of transcription (JAK-STAT) pathway is a hallmark for the Philadelphia…”
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Abstract 3780: Activity of the BET inhibitor INCB054329 in models of lymphoma
Published in Cancer research (Chicago, Ill.) (15-07-2016)“…Inhibitors of the BET family of Bromodomain proteins have been shown to be growth inhibitory across a spectrum of tumor types due to their ability to regulate…”
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Induction of endogenous genes by peroxisome proliferator activated receptor alpha ligands in a human kidney cell line and in vivo
Published in The Journal of steroid biochemistry and molecular biology (01-05-2003)“…The peroxisome proliferator activated receptor alpha (PPARα) plays a key role in regulating fatty acid metabolism by regulating expression of genes involved in…”
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