Search Results - "Vogel, Kurt W"
-
1
Parkinson disease-associated mutation R1441H in LRRK2 prolongs the "active state" of its GTPase domain
Published in Proceedings of the National Academy of Sciences - PNAS (18-03-2014)“…Mutation in leucine-rich-repeat kinase 2 (LRRK2) is a common cause of Parkinson disease (PD). A disease-causing point mutation R1441H/G/C in the GTPase domain…”
Get full text
Journal Article -
2
Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation
Published in PloS one (28-08-2012)“…Mutations in the leucine-rich repeat kinase-2 (LRRK2) have been linked to Parkinson's disease. Recent studies show that inhibition of LRRK2 kinase activity…”
Get full text
Journal Article -
3
Pharmacological inhibition of LRRK2 cellular phosphorylation sites provides insight into LRRK2 biology
Published in Biochemical Society transactions (01-10-2012)“…Mutations in LRRK2 (leucine-rich repeat kinase 2) have been linked to inherited forms of PD (Parkinson's disease). Substantial pre-clinical research and drug…”
Get more information
Journal Article -
4
Multiplexing terbium- and europium-based TR-FRET readouts to increase kinase assay capacity
Published in Journal of biomolecular screening (01-09-2010)“…Identification and characterization of kinase inhibitor potency and selectivity is often an iterative process in which a library of compounds is first screened…”
Get more information
Journal Article -
5
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…”
Get full text
Journal Article -
6
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…”
Get more information
Journal Article -
7
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…”
Get more information
Journal Article -
8
Simultaneous Monitoring of Discrete Binding Events Using Dual-Acceptor Terbium-Based LRET
Published in Journal of the American Chemical Society (07-11-2007)“…Lanthanide resonance energy transfer (LRET) between chelated terbium and two spectrally distinct acceptor fluorophores (fluorescein and Alexa Fluor 633) is…”
Get full text
Journal Article -
9
Time-resolved fluorescence resonance energy transfer kinase assays using physiological protein substrates: Applications of terbium–fluorescein and terbium–green fluorescent protein fluorescence resonance energy transfer pairs
Published in Analytical biochemistry (01-09-2006)“…Fluorescence-based kinase assays using peptide substrates are an established format for high-throughput screening and profiling of kinases. Among…”
Get full text
Journal Article -
10
High-throughput cellular assays for regulated posttranslational modifications
Published in Analytical biochemistry (15-01-2008)“…We have developed a set of high-throughput screening (HTS)-compatible assays capable of measuring regulated, target-specific posttranslational modifications in…”
Get full text
Journal Article -
11
A substrate for deubiquitinating enzymes based on time-resolved fluorescence resonance energy transfer between terbium and yellow fluorescent protein
Published in Analytical biochemistry (2007)“…Deubiquitinating enzymes (DUBs) proteolytically cleave ubiquitin from ubiquitinated proteins, and inhibition of DUBs that rescue oncogenic proteins from…”
Get full text
Journal Article -
12
Development of LanthaScreen cellular assays for key components within the PI3K/AKT/mTOR pathway
Published in Journal of biomolecular screening (01-02-2009)“…The PI3K/AKT/mTOR pathway is central to cell growth and survival, cell cycle regulation, and programmed cell death. Aberrant activation of this signaling…”
Get more information
Journal Article -
13
A fluorescence lifetime based binding assay to characterize kinase inhibitors
Published in Journal of biomolecular screening (01-09-2007)“…The authors present a fluorescence lifetime-based kinase binding assay that identifies and characterizes compounds that bind to the adenosine triphosphate…”
Get more information
Journal Article -
14
A fluorescence anisotropy assay for the muscarinic M1 G-protein-coupled receptor
Published in Assay and drug development technologies (01-06-2010)“…In the search for new chemical entities that interact with G-proteincoupled receptors (GPCRs), assays that quantify efficacy and affinity are employed…”
Get more information
Journal Article -
15
A toolbox approach to high-throughput TR-FRET-based SUMOylation and DeSUMOylation assays
Published in Assay and drug development technologies (01-08-2009)“…The posttranslational modification of target substrates by the ubiquitin-like proteins, specifically the small ubiquitin-like modifier (SUMO), has emerged as…”
Get more information
Journal Article -
16
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…”
Get more information
Journal Article -
17
Improving lanthanide-based resonance energy transfer detection by increasing donor-acceptor distances
Published in Journal of biomolecular screening (01-06-2006)“…Lanthanide-based resonance energy transfer (LRET) is an established method for measuring or detecting proximity between a luminescent lanthanide (energy donor)…”
Get more information
Journal Article -
18
Overcoming compound interference in fluorescence polarization-based kinase assays using far-red tracers
Published in Assay and drug development technologies (01-04-2004)“…Kinase-mediated phosphorylation of proteins is critical to the regulation of many biological processes, including cell growth, apoptosis, and differentiation…”
Get more information
Journal Article -
19
Pharmacological characterization of purified recombinant mTOR FRB-kinase domain using fluorescence-based assays
Published in Journal of biomolecular screening (01-03-2008)“…The mammalian target of rapamycin (mTOR) is a serine/threonine kinase involved in nutrient sensing and cell growth and is a validated target for oncology and…”
Get more information
Journal Article -
20
Multiplexing fluorescence polarization assays to increase information content per screen: applications for screening steroid hormone receptors
Published in Journal of biomolecular screening (01-06-2004)“…As the push to reduce cost per well in high-throughput screening reaches the practical limitations of liquid handling, future cost savings will likely arise…”
Get more information
Journal Article