December 2006
Volume 1, Issue 12
A review of 2006
     
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Ulrike Knies-Bamforth
The View from Here
Ulrike Knies-Bamforth, Editor Drug Discovery Today

With this issue, the first year of E-Choice is coming to an end. It has been a successful launch and I would like to thank all the Guest Editors for their valuable contributions. The focus of this month’s E-Choice is our journal, Drug Discovery Today...
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A review of 2006


  Top Reviews
I want a new drug: G-protein-coupled receptors in drug development

Schlyer, S. and Horuk, R.
Drug Discovery Today

Huey Lewis and the News summed it up nicely in their 1980s hit record: ‘I want a new drug, one that won’t make me sick, one that won’t make me crash my car, or make me feel three feet thick’. The song could be an anthem for drug discovery in the pharmaceutical industry...

New drug candidates and therapeutic targets for tuberculosis therapy

Zhang, Y., Post-Martens, K., Denkin, S.
Drug Discovery Today

Despite advances in chemotherapy and the BCG (Bacillus Calmette–Guérin) vaccine, tuberculosis remains a significant infectious disease. Although it can be cured, the therapy takes at least 6–9 months, and the laborious and lengthy treatment brings with it dangers of noncompliance, significant toxicity and drug resistance...

Designing better drugs: predicting cytochrome P450 metabolism

De Groot, M.J.
Drug Discovery Today

Many 3D ligand-based and structure-based computational approaches have been used to predict, and thus help explain, the metabolism catalyzed by the enzymes of the cytochrome P450 superfamily (P450s). P450s are responsible for >90% of the metabolism of all drugs, so the computational prediction of metabolism can help to design out drug–drug interactions...

Harnessing in vivo siRNA delivery for drug discovery and therapeutic development

Xie F.Y., Woodle, M.C., Lu, P.Y.
Drug Discovery Today

The use of RNA interference (RNAi) is spreading rapidly to nearly every aspect of biomedical research. The gene silencing capability of RNAi is being used to study individual gene’s biological function and role in biochemical pathways. However, the efficacy of RNAi depends upon efficient delivery of the intermediates of RNAi, short interfering RNA (siRNA) and short hairpin RNA (shRNA) oligonucleotides...


  Abstracts of Key Research Articles

Novel GPCR screening approach: indirect identification of S1P receptor agonists in antagonist screening using a calcium assay
Siehler, S. and Guerini, D.
J Recept Signal Transduct Res. 26(5-6):549-75

GLIDA: GPCR-ligand database for chemical genomic drug discovery
Okuno, Y., Yang, J., Taneishi, K., Yabuuchi, H., Tsujimoto, G.
Nucleic Acids Res. 34(Database issue):D673-7

GPCR agonists and antagonists in the clinic
Tyndall, J.D. and Sandilya, R.
J Med Chem. 1(4):405-21

A case for passive immunoprophylaxis against tuberculosis
Reljic, R. and Ivanyi, J.
Lancet Infect Dis. 6(12):813-8

Proteome-wide profiling of isoniazid targets in Mycobacterium tuberculosis
Argyrou, A., Jin, L., Siconilfi-Baez, L., Angeletti, R.H., Blanchard, J.S.
Biochemistry. 45(47):13947-53

Dissecting virulence pathways of Mycobacterium tuberculosis through protein-protein association
Singh, A., Mai, D., Kumar, A., Steyn, A.J.
Proc Natl Acad Sci USA 103(30):11346-51

Cytochrome P450 nomenclature, 2004
Nelson, D.R.
Methods Mol Biol. 320:1-10

Crystal structure of human cytochrome P450 2D6
Rowland, P., Blaney, F.E., Smyth, M.G., Jones, J.J., Leydon, V.R., Oxbrow, A.K., Lewis, C.J., Tennant, M.G., Modi, S., Eggleston, D.S., Chenery, R.J., Bridges, A.M.
J Biol Chem. 17;281(11):7614-22

Ligand-targeted delivery of therapeutic siRNA
Ikeda, Y., Taira, K.
Pharm Res. 23(8):1631-40

Cell type-specific delivery of siRNAs with aptamer-siRNA chimeras
McNamara, J.O. 2nd, Andrechek, E.R., Wang, Y., Viles, K.D., Rempel, R.E., Gilboa, E., Sullenger, B.A., Giangrande, P.H.
Nat Biotechnol. 24(8):1005-15

Aptamer mediated siRNA delivery
Chu, T.C., Twum K.Y., Ellington, A.D., Levy, M.
Nucleic Acids Res. 1;34(10):e73


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