Search Results - "Penhallow, Becky"
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Renal Cell Carcinoma (RCC) Tumors Display Large Expansion of Double Positive (DP) CD4+CD8+ T Cells With Expression of Exhaustion Markers
Published in Frontiers in immunology (26-11-2018)“…Checkpoint inhibitors target the inhibitory receptors expressed by tumor-infiltrating T cells in order to reinvigorate an anti-tumor immune response…”
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Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors
Published in Molecular cancer therapeutics (01-11-2008)“…In developing inhibitors of the LIM kinases, the initial lead molecules combined potent target inhibition with potent cytotoxic activity. However, as…”
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Transcriptional profiling of the dose response: a more powerful approach for characterizing drug activities
Published in PLoS computational biology (01-09-2009)“…The dose response curve is the gold standard for measuring the effect of a drug treatment, but is rarely used in genomic scale transcriptional profiling due to…”
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Discovery of (R)-7-Cyano-2,3,4,5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a Farnesyltransferase Inhibitor with Potent Preclinical Antitumor Activity
Published in Journal of medicinal chemistry (05-10-2000)“…Continuing structure−activity studies were performed on the 2,3,4,5-tetrahydro-1-(imidazol-4-ylalkyl)-1,4-benzodiazepine farnesyltransferase (FT) inhibitors…”
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Discovery and Structure−Activity Relationships of Imidazole-Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase
Published in Journal of medicinal chemistry (16-12-1999)“…2,3,4,5-Tetrahydro-1-(imidazol-4-ylalkyl)-1,4-benzodiazepines were found to be potent inhibitors of farnesyltransferase (FT). A hydrophobic substituent at the…”
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Abstract 4687: Double positive (DP) CD4+CD8+ T cells with an exhausted phenotype in renal cell carcinoma (RCC) patients
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Checkpoint inhibitors target the inhibitory receptors expressed by tumor infiltrating T cells in order to reinvigorate an anti-tumor immune response…”
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Abstract 5016: Antitumor activity of anti-PD-1 in combination with tyrosine kinase inhibitors in a preclinical renal cell carcinoma model
Published in Cancer research (Chicago, Ill.) (01-10-2014)“…Abstract Introduction: Nivolumab (BMS-936558; MDX-1106; ONO-4538) is a fully human IgG4 programmed death-1 (PD-1) immune checkpoint inhibitor antibody that…”
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Abstract LB-127: From bench to bedside: Exploring OX40 receptor modulation in a phase 1/2a study of the OX40 costimulatory agonist BMS-986178 ± nivolumab (NIVO) or ipilimumab (IPI) in patients with advanced solid tumors
Published in Cancer research (Chicago, Ill.) (01-07-2018)“…Abstract Background: Activation of OX40, a costimulatory protein in the tumor necrosis factor receptor super family, enhances T effector cell activation and…”
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Discovery and Structure−Activity Relationships of Imidazole-Containing Tetrahydrobenzodiazepine Inhibitors of Farnesyltransferase
Published in Journal of medicinal chemistry (16-12-1999)Get full text
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Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms
Published in ACS medicinal chemistry letters (13-08-2015)“…JAK2 kinase inhibitors are a promising new class of agents for the treatment of myeloproliferative neoplasms and have potential for the treatment of other…”
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Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists
Published in Bioorganic & medicinal chemistry letters (15-06-2012)“…5-Butyl-1,4-diphenyl pyrazole and 2-amino-5-chloro pyrimidine acylsulfonamides were developed as potent dual antagonists of Bcl-2 and Bcl-xL. Compounds were…”
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Modulation of cofilin phosphorylation by inhibition of the Lim family kinases
Published in Bioorganic & medicinal chemistry letters (15-09-2012)“…The design, synthesis, and SAR for a series of aminothiazole pyrimidines as potent LIMK inhibitors are described. Compound 31 effectively inhibited cofilin…”
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Characterization of BMS-911543, a Functionally Selective Small Molecule Inhibitor of JAK2
Published in Blood (19-11-2010)“…Abstract 4112 We report the characterization of BMS-911543, a potent and functionally selective small molecule inhibitor of the Janus kinase family (JAK)…”
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Selective Itk Inhibitors Block T-Cell Activation and Murine Lung Inflammation
Published in Biochemistry (Easton) (31-08-2004)“…Nonreceptor protein tyrosine kinases including Lck, ZAP-70, and Itk play essential roles in T-cell receptor (TCR) signaling. Gene knockout studies have…”
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Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors
Published in Bioorganic & medicinal chemistry letters (15-07-2006)“…A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure–activity relationships (SARs),…”
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Abstract DDT01-03: Discovery of BMS-911543, a highly selective JAK2 inhibitor, as a clinical candidate for the treatment of myeloproliferative disease and other malignancies
Published in Cancer research (Chicago, Ill.) (15-04-2011)“…Abstract Myeloproliferative diseases (MPDs) are a subset of myeloid malignancies that are characterized by the expansion of a multipotent hematopoietic stem…”
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Transcriptional Profiling of the Dose Response: A More Powerful Approach for Characterizing Drug Activities: e1000512
Published in PLoS computational biology (01-09-2009)“…The dose response curve is the gold standard for measuring the effect of a drug treatment, but is rarely used in genomic scale transcriptional profiling due to…”
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Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2006)“…A series of structurally novel aminothiazole based small molecule inhibitors of Itk were prepared to elucidate their structure–activity relationships (SARs),…”
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Discovery of ( R )-7-Cyano-2,3,4,5-tetrahydro-1-(1 H -imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1 H -1,4-benzodiazepine (BMS-214662), a Farnesyltransferase Inhibitor with Potent Preclinical Antitumor Activity
Published in Journal of medicinal chemistry (01-10-2000)Get full text
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