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The Transcreener® ADP2 Universal Kinase Assay from BellBrook Labs is readily performed on BMG LABTECH microplate readers using different assay formats

The Transcreener® ADP2 FI assay kit from BellBrook Labs is a simple one-step competitive red fluorescence immunoassay based on the detection of ADP. In this application note we show that this assay is compatible with four different microplate readers from BMG LABTECH. With the PHERAstar FS and Plus, as well as the POLARstar and FLUOstar Omegas comparable standard curves and EC50 values were obtained.

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Predicting hepatotoxicity: Reactive metabolite trapping using glutathione and freshly isolated hepatocytes
Birks, V., Webber, G., Geoffroy, S., Cole, R., and Wood, S.

This poster presents our results to date using clozapine (a compound known to be associated with GSH-adduct formation) as substrate and using stable isotope GSH (GSH13C2,15N) to enhance specificity. In addition, all analyses have been conducted using an Waters Acquity UPLC-MS/MS. Results we have obtained in hepatocytes are compared against findings using human liver microsomes (HLM).

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In-silico Prediction of Human Intestinal Absorption and human oral bioavailability
Aixia Yan*

Human intestinal absorption (HIA) and human oral bioavailability are two important ADME properties in drug design. We built some in-silico models for classification of human intestinal absorption (HIA) and human oral bioavailability by Kohonen’s self-organizing Neural Network (KohNN), and several quantitative models for prediction of HIA and bioavailability of several subset compounds datasets by Support Vector Machine (SVM).

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Label-Free High Throughput Homogeneous ADME Assays
David Ricketts, Patricia De Pril, Anne Van Hoonacker, Patrick Englebienne

SoPRano is a novel label-free screening platform using specifically derivatised gold nanoparticles in solution form. It enables SPR-based screening in high throughput using simple homogenous assay protocols on a standard absorbance plate-reader. SoPRano is flexible and can be applied to many affinity screening applications.

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Homology modeling and docking studies of Comamonas testosteroni B-356 biphenyl-2, 3-dioxygenase involved in degradation of polychlorinated biphenyls
M. Saqib Baig and N. Manickam

The three-dimensional model of a-subunit of Biphenyl dioxygenase (BphA) from Comamonas testosteroni B-356 has been constructed. The kinetic parameters of biphenyl compounds were well matched with the docking results. The binding properties of these biphenyl compounds along with identification of critical active site residues could be used for further site-directed mutagenesis experiments in order to identify their role in activity and substrate specificity.

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Anti-inflammatory activity of Dalbergia sissoo Roxb. heart-wood
Ohm Devani, S. K. Lahiri, D. D. Santani, M. B. Shah

The heart-wood of Dalbergia sissoo Roxb. is reported to be used in traditional medicinal practices, of which anti-inflammatory is one. The present work evaluates the effect of the heart-wood extract on the carrageenan induced rat paw edema. The drug was found to be active at lowest of 3 doses tried. the drug can be said to posses anti-inflamatory activity but needs further evaluation of discover the pathway of the same.

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Necessity of quantum mechanics for predicting binding free energy
Ting Zhou, Danzhi Huang, Amedeo Caflisch

We demonstrate the necessity of quantum mechanics (QM) for predicting binding free energy by comparing the results of the linear interaction energy model with continuum model (LIECE) and the equivalent model with QM (QMLIECE).

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Resorufin - a lead for a new protein kinase CK2 inhibitor
Iben Skjøth Sandholt1, Birgitte Brinkmann Olsen1, Barbara Guerra1, Olaf-Georg Issinger1, Brigitte Boldyreff2

Screening of a natural compound library led to the identification of resorufin, as a highly selective and potent inhibitor for protein kinase CK2. Out of 52 kinases tested only CK2 was inhibited. The IC50 values determined for the CK2 holoenzymes were 1.5 µM and for the free catalytic subunits ca. 4 µM. In different cancer cell lines treatment with resorufin led to cell death and endogenous CK2 was inhibited.

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Experimental Determination of ADMET Parameters in High Throughput, Using Colloidal Gold Composites and a Conductive Polymer as Reporting Reagents
Roberto Martinez-Neira, Patricia De Pril, Anne Van Hoonacker, Patrick Englebienne

We developed and validated a high throughput in vitro setting to experimentally determine hSA and Orosomucoid affinities, fraction absorbed, Log BBB and Redox potential of NCEs using gold nanoparticles functionalized with proteins, lipids or conductive polymers. Such automated ADME assays provide means for more objective decisions in early drug discovery.

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Showing Results 61 - 70 of 122
Scientific News
3-D Engineered Bone Marrow Makes Functioning Platelets
Scalable model supports patient-specific treatments, advanced study of blood disorders.
Single-Cell, 42-plexed Protein Analysis Achieved with a New Microchip Technology
A novel microdevice capable of detecting 42 unique immune effector proteins has been developed.
Mini Synthetic Organism Instead Of Test Animals
Using a compact multi-organ chip, and those of three separate microcircuits, researchers can study the regeneration of certain kidney cells.
Novel Organoid Matrix Enables Long-Term Culture of Human Hepatocytes
Organoid growth matrix to enable long-term culture of genome-stable bipotent stem cells from adult human liver.
First Contracting Human Muscle Grown in Laboratory
Researchers at Duke University report the first lab-grown, contracting human muscle, which could revolutionize drug discovery and personalized medicine.
Antriabio Announces Completion Of PK/PD Studies Of AB101
AB101 positioned to be the first once-weekly basal insulin for diabetes patients.
Anti-Diabetic Drug Springs New Hope for Tuberculosis Patients
Drug for treating diabetes can double up as adjunct treatment for tuberculosis.
A Poisonous Cure
Toxic fungi may hold the secrets to tackling deadly diseases.
Antibiotic Resistance Threatens Future of Modern Medicine
Overuse and misuse of antibiotics, one of the key contributors to antimicrobial resistance (AMR).
Bacterial Toxin Targets Discovered
Understanding how bacterial toxins target human cells is set to have major implications for the development of novel drugs.
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