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THE OSTEOPROTECTIVE ACTION OF 6-OXA-8a-ANALOGUES OF STEROID ESTROGENS
A.G. Shavva, V.N. Belov, A.Yu. Solovyev, S.N. Morozkina

We synthesized fourteen 6-oxa-8a-estrogens analogues and investigated osteoprotective and uterotropic actions. We demonstrated correlation: every modification in structure of 6-oxa-8-analogues leading to strong (>30%) reduction of uterotropic action induces slump of osteoprotective activity. This allows to make conclusion: main biotarget, responsible for appearance of osteoprotective action is a-estrogen receptor. We found steroid estrogen analogues with cholesterol-lowering properties without u

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Lead Optimization Computational Protocol at PDB Scale to Rationally Optimize Attachments to a Given Kinase Inhibitor Scaffold
Moriaud F., Henry T., Adcock S.A., Vorotynsev A.M., Martin L., Doppelt O.

We’ve used MED-SuMo to query and mine the Protein’s Surface Chemical Functions surrounding fragments of PDB ligands, seeking similarities with the kinase of interest (Vegfr DFGout, pdb code 2oh4, ligand code GIG) and collecting a library of 1129 unique fragments positioned in the vegfr’s active site and annotated with the counts of contacts and h-bonds. With them we optimize a substructure of the GIG ligand to find others DFGout ligands.

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Tackling the Problem of Hit Rate Enrichment by Virtual Screening: Quality-Driven Bioactive Conformations and Pharmacophore-Biased Creative Search
Nasonov, Anatoliy F., Pletnev Igor V.

Novel ChemoSoft(TM) software tools addressing the problem of generation of bioactive conformations and virtual screening hit rate enrichment have been created.

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Caveolin-1 Expression as a Possible Biomarker in Pancreatic Cancer Diagnosis
C. Tanase, E. Raducan, L. Albulescu, E. Codorean, M.I. Nicolescu, D.I. Popescu, M.L. Cruceru and A.C. Popa

Caveolin1 (Cav-1) function either as a tumor supressor or as a promoter of metastasis. Overexpresion of cav-1 was correlated with: tumoral grading, proliferration markers (Ki67, p53), serum tumor markers (CEA, CA19.9) and angiogenic markers (VEGF, bFGF).

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Changes in the Gene Expression of mRNA Transcripts for Insulin like Growth Factor, their receptor and Facilitative Glucose Transporter in IVM Oocytes
S.C. Gupta, Neelam Gupta and Alok Pandey

The cDNA libraries from single oocytes and pre-implantation buffalo embryos from 2 cell stage to blastocyst were established. Relative expression studied with RT-PCR of IGF-I showed an increase at 12h and decline at 24h of IVM oocytes. IGF-IR was expressed at cleavage stages to blastocyts. Glut-I was expressed in IVM oocytes and SCNT embryos at all stages. Gene expression of IGF-I, IGF-IR and Glut-I plays an important role in SCNT embryo production.

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Development of a Lab-on-a-Chip for the Characterization of Human Cells
Richter, L., Stepper, C., Mak, A., Brückl, H. and Ertl, P.

Cell chips are developed to continuously monitor mammalian cell population dynamics in a non-invasive manner. In the presented work we describe the design, fabrication and characterization of a lab-on-a-chip for quantitative cell analysis.

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Label-free Identification of Microorganisms using a Contact-less Dielectric Microsensor
Ertl, P., Richter, L., Reinthaler, A., Stepper, C., Mak, A., Kast, M., Heer, R. and Brückl, H.

Microfabricated biochips are developed to continuously monitor cell population dynamics in a non-invasive manner. In the presented work we describe the novel combination of contact-less dielectric microsensors and microfluidics to promote biofilm formation for quantitative cell analysis.

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Pharmacophore Mapping of Flavone Derivatives for Aromatase Inhibiton
Shuchi Nagar, Md Ataul Islam, Arup Mukherjee and Achintya Saha

The study explores the structural requirements of flavones for inhibition of aromatase activity. The QSAR analysis generates the model that shows the importance of flavone ring and with molecular lipophilicity. Presence of additional aromatic ring and m-hydroxy substitution on that ring increases inhibitory activity. Space modeling study further adjudged the presence of hydrogen bond acceptor, hydrophobic and aromatic ring and critical distance among features for the inhibitory activity.

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Real-Time Multiplex Rt-PCR on Circulating Tumor Cells
Anieta M. Sieuwerts, Stefan Sleijfer, Jaco Kraan, Joan Bolt-de Vries, Jan-Willem Gratama, John WM Martens and John A. Foekens

Using the CTC kit (CellSearch™), cells that attached to anti-EpCAM Moab were immunomagnetically separated and used for analysis of a selected pilot set of 32 genes by real time RT-PCR. This study shows the feasibility of multiple gene expression analysis on RNA isolated from only one tumor cell. Most importantly, expression analysis of several tumor-specific genes in blood samples containing only 2 tumor cells is already possible.

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Showing Results 51 - 59 of 59
Scientific News
Big Data Project to Capture the Experience of MS Patients
Researchers will track the lives of people with multiple sclerosis in unprecedented detail in a project to improve the evaluation of treatments.
Measuring Brain Volume can Help People with Multiple Sclerosis
icometrix has developed software for measuring the brain and brain lesion volume.
Anonymised Clinical Data Key to Understanding Traumatic Brain Injuries
By exploiting big data in a real healthcare setting, it is hoped that clinicians will be able to make treatment decisions earlier.
WormBase ParaSite Launched
Open-access database WormBase ParaSite launches with data on 1.5 million genes.
Big Data Set To Make A Big Difference In Childhood Cancer Treatment
UTS researchers are working with the Kids Research Institute to visualise large quantities of patient data to better diagnose and treat childhood cancer patients.
Proteomics for Systems Toxicology
MS-based proteomics is maturing into a robust technology for the measurement of proteome-wide exposure effects.
Molecular Event Mapping Opens Door to more in silico Tests
It is hoped that this new approach to mapping and predicting the impact of chemical compounds in the body could reduce the need for toxicity tests in animals.
Big Data Helps Pinpoint Possible New Stent Drug
Replacing the current drug used to coat artery-opening stents with a drug more targeted to the actual cause of stent disease could reduce blood clots and heart attacks.
Computer Model Sets New Precedent in Drug Discovery
New computational model can precisely simulate, predict therapeutic protein behaviors to help zero in on ideal drug design candidates.
TGAC Leads Research To Help Identify Animal-To-Human Transmitted Diseases
The Genome Analysis Centre (TGAC) will lead research into the development of bioinformatics to support the identification and characterisation of viruses through metagenomics.
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