Search Results - "Marks, Bryan"
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Threshold Levels of ABL Tyrosine Kinase Inhibitors Retained in Chronic Myeloid Leukemia Cells Determine Their Commitment to Apoptosis
Published in Cancer research (Chicago, Ill.) (01-06-2013)“…The imatinib paradigm in chronic myelogenous leukemia (CML) established continuous BCR-ABL inhibition as a design principle for ABL tyrosine kinase inhibitors…”
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2
Development and applications of a broad-coverage, TR-FRET-based kinase binding assay platform
Published in Journal of biomolecular screening (01-09-2009)“…The expansion of kinase assay technologies over the past decade has mirrored the growing interest in kinases as drug targets. As a result, there is no shortage…”
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3
Sensing Hydrogen Gas from Atmospheric Pressure to a Hundred Parts per Million with Nanogaps Fabricated Using a Single-Step Bending Deformation
Published in ACS sensors (22-01-2016)“…The widespread use of H2 gas as an energy carrier will necessitate the development of inexpensive, easily manufactured sensors which reliably monitor gas…”
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The Androgen Receptor T877A Mutant Recruits LXXLL and FXXLF Peptides Differently than Wild-Type Androgen Receptor in a Time-Resolved Fluorescence Resonance Energy Transfer Assay
Published in Biochemistry (Easton) (23-01-2007)“…The interactions of the ligand binding domain (LBD) of androgen receptor (AR) and the AR T877A mutant, found in prostate cancer, with peptides from coactivator…”
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5
A substrate-independent TR-FRET histone deacetylase inhibitor assay
Published in Journal of biomolecular screening (01-12-2011)“…Developing molecularly targeted therapeutics with minimal off-target effects is facilitated by an understanding of compound selectivity. However, for HDAC…”
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Highly miniaturized formats for in vitro drug metabolism assays using vivid fluorescent substrates and recombinant human cytochrome P450 enzymes
Published in Journal of biomolecular screening (01-02-2005)“…Highly miniaturized P450 screening assays designed to enable facile analysis of P450 drug interactions in a 1536-well plate format with the principal human…”
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Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening
Published in Assay and drug development technologies (01-04-2009)“…The human pregnane X nuclear receptor (PXR) is a xenobiotic-regulated receptor that is activated by a range of diverse chemicals, including antibiotics,…”
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Development of a coactivator displacement assay for the orphan receptor estrogen-related receptor-γ using time-resolved fluorescence resonance energy transfer
Published in Analytical biochemistry (01-10-2006)“…The estrogen-related receptor-γ (ERRγ) is a constitutively active orphan receptor that belongs to the nuclear receptor superfamily and is most closely related…”
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Development of the predictor HERG fluorescence polarization assay using a membrane protein enrichment approach
Published in Assay and drug development technologies (01-04-2008)“…The life-threatening consequences of acquired, or drug-induced, long QT syndrome due to block of the human ether-a-go-go-related gene (hERG) channel are well…”
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10
Multiparameter analysis of a screen for progesterone receptor ligands: comparing fluorescence lifetime and fluorescence polarization measurements
Published in Assay and drug development technologies (01-12-2005)“…Direct measurement of the fluorescence lifetime (FLT) of a fluorescent label is an emerging method for high-throughput screening. Changes in the fluorescence…”
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High-throughput screening assays for the assessment of CYP2C91, CYP2C92, and CYP2C93 metabolism using fluorogenic Vivid substrates
Published in Journal of biomolecular screening (01-08-2004)“…CYP2C9 is a genetically polymorphic human cytochrome P450 isozyme involved in the oxidative metabolism of many drugs, including nonsteroidal anti-inflammatory…”
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A high throughput screening assay to screen for CYP2E1 metabolism and inhibition using a fluorogenic vivid p450 substrate
Published in Assay and drug development technologies (01-11-2002)“…Large-scale screening of multiple compound libraries and combinatorial libraries for pharmacological activity is one of the novel approaches of the modern drug…”
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13
High-Throughput screeening assays for CYP2B6 metabolism and inhibition usuing fluorogenic vivid substrates
Published in AAPS PharmSci (01-06-2003)“…CYP2B6 is a highly polymorphic P450 isozyme involved in the metabolism of endo-and xenobiotics with known implications for the activation of many…”
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Validation of LC–MS/MS methods for quantitative analysis of kynurenine pathway metabolites in human plasma and cerebrospinal fluid
Published in Bioanalysis (01-06-2023)“…Dysregulation of the kynurenine metabolic pathway has been reported in several neurological conditions. Sensitive and selective LC–MS/MS methods have been…”
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Abstract 5496: Determination of drug-kinase residence time in a homogenous, low-volume format
Published in Cancer research (Chicago, Ill.) (15-04-2010)“…In addition to drug-target affinity, drug-target residence time is becoming recognized as a critical parameter influencing drug efficacy. Desired compound…”
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16
Threshold levels of ABL tyrosine kinase inhibitors retained in chronic myeloid leukemia cells define commitment to apoptosis
Published in Cancer research (Chicago, Ill.) (10-04-2013)“…The imatinib paradigm in chronic myeloid leukemia (CML) established continuous BCR-ABL inhibition as a design principle for ABL tyrosine kinase inhibitors…”
Get full text
Journal Article -
17
Cryptic Intracellular Retention of ABL Tyrosine Kinase Inhibitors within CML Cells Mediates Apoptosis Commitment Following Acute Drug Exposure
Published in Blood (18-11-2011)“…Abstract 3504 The imatinib paradigm established continuous BCR-ABL inhibition as a design principle for ABL tyrosine kinase inhibitors (TKIs). However,…”
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A simultaneous assessment of CYP3A4 metabolism and induction in the DPX-2 cell line
Published in The AAPS journal (04-03-2005)“…The DPX-2 cell line, a derivative of HepG2 cells, harbors human PXR and a luciferase-linked CYP3A4 promoter. These cells were used in a panel of cell-based…”
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High-throughput screening assays for CYP2B6 metabolism and inhibition using fluorogenic vivid substrates
Published in AAPS PharmSci (2003)“…CYP2B6 is a highly polymorphic P450 isozyme involved in the metabolism of endo- and xenobiotics with known implications for the activation of many…”
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