The
View from Here
William C Eckelman
Molecular Imaging is being touted as an important biomarker in drug development. Of the various imaging approaches that have shown promise, molecular targeting of low-density sites such as receptors, transporters, and some enzymes is of particular interest...
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Upcoming Issues
Issue 6/June '07
Fragment-based screening
Issue 7/July '07
Chemoinformatics
Issue 8/July '07
Molecular modelling
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A
review of 2006
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Top
Reviews |
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Scaffold selection and scaffold hopping in lead generation: a medicinal chemistry perspective
Zhao H
Drug Discovery Today
Hit selection and lead generation are crucial for the success of the resource-demanding leadoptimization
phase in drug discovery, and represent a major research area of medicinal chemistry today.
Ligand-binding efficiency, ligand complexity, ligand–target profile complementarity and chemical
tractability are important parameters in hit selection....
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Blood-brain barrier delivery
Pardridge WM
Drug Discovery Today
Neuropharmaceutics is the largest potential growth sector of the pharmaceutical industry. However, this
growth is blocked by the problem of the blood–brain barrier (BBB). Essentially 100% of large-molecule
drugs and >98% of small-molecule drugs do not cross the BBB...
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Drug discovery: selecting the optimal approach
Sams-Dodd F
Drug Discovery Today
The target-based drug discovery approach has for the past 10–15 years been the dominating drug
discovery paradigm. However, within the past few years, the commercial value of novel targets in
licensing deals has fallen dramatically, reflecting that the probability of reaching a clinical drug
candidate for a novel target is very low...
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Abstracts
of Key Research Articles
Combinatorial chemistry improves molecular options over pre-existing leads
Edwards P
Drug Discov Today. 2007;12:185-6.
Imaging Alzheimer's disease pathology: one target, many ligands
Lockhart A
Drug Discov Today. 2006;11(23-24):1093-9.
Strategies to optimize the validity of disease models in the drug discovery process
Sams-Dodd F
Drug Discov Today. 2006;11(7-8):355-63
Postmeeting summary on the round table discussion at the Seventh International Symposium on Technetium in Chemistry and Nuclear Medicine held in Bressanone
Eckelman WC, Erba PA, Schwaiger M, Wagner HN Jr, Alberto R, Mazzi U
Nucl Med Biol. 2007;34(1):1-4.
Are there lessons to be learned from drug development that will accelerate the use of molecular imaging probes in the clinic?
Eckelman WC, Rohatagi S, Krohn KA, Vera DR
Nucl Med Biol. 2005;32(7):657-62.
Seeing into cells
Daniel C. Sullivan and Gary Kelloff
EMBO Rep. 2005; 6(4): 292–296.
The progress and promise of molecular imaging probes in oncologic drug development
Kelloff GJ, Krohn KA, Larson SM, et al.
Clin Cancer Res. 2005; 11(22): 7967-7985.
Using positron emission tomography to facilitate CNS drug development
Lee CM, Farde L.
Trends Pharmacol Sci. 2006; 27 (6): 310-316.
Imaging and Other Biomarkers in Early Clinical Studies: One Step at a Time or Re-Engineering Drug Development?
Collins JM
J Clin Oncol. 2005; 23(24): 5417-5419.
New science-based endpoints to accelerate oncology drug development
Kelloff GJ, Sigman CC.
Eur J Cancer. 2005; 41(4): 491-501.
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