Drug Discovery Editor's Choice Email - October 2006 Volume 1

October 2006
Volume 1, Issue 10
Medicinal Chemistry

The View from Here
Peter Gallagher, PhD

Medicinal chemistry has delivered significant improvements in healthcare over the last 60 years. During this time the pharmaceutical industry has become the dominant provider of new medicines, through the application of medicinal chemistry and allied technologies...
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	Top Reviews
	The growing impact of click chemistry on drug discovery Hartmut Kolb and K. Barry Sharpless Drug Discovery Today Click chemistry is a modular approach that uses only the most practical and reliable chemical transformations. Its applications are increasingly found in all aspects of drug discovery, ranging from lead finding through combinatorial chemistry and target-templated in situ chemistry, to proteomics and DNA research, using bioconjugation reactions...
	Automated medicinal chemistry Marcus Koppitz and Knut Eis Drug Discovery Today With the advent of high throughput technologies in biological screening in the 1980s, providing sufficient numbers of small molecules for screening became a bottleneck in the drug discovery process. Combinatorial chemistry was the first attempt by chemists to address this issue. However, since its first applications, combinatorial chemistry has evolved rapidly into diverse fields....
	Chemical microarray: a new tool for drug screening and discovery Haiching Ma and Kurumi Horiuchi Drug Discovery Today HTS with microtiter plates has been the major tool used in the pharmaceutical industry to explore chemical diversity space and to identify active compounds and pharmacophores for specific biological targets. However, HTS faces a daunting challenge regarding the fast-growing numbers of drug targets arising from genomic and proteomic research, and large chemical libraries generated from highthroughput synthesis... Click here to subscribe to *Drug Discovery Today*.

	Abstracts of Key Research Articles Using positron emission tomography to facilitate CNS drug development Lee, CM and Farde, L. Trends in Pharmacological Sciences (2006) 27(6):310-6 Positron Emission Tomography As an Imaging Biomarker Weber WA J Clinical Oncology (2006) 24(20):3282-92 Novel Procedure for Modelling Ligand/Receptor Induced Fit Effects Sherman W et al. J. Medicinal Chemistry (2006) 49(2):534-53 Molecular Field Extrema as Descriptors of Biological Activity: Definition and Validation Cheeseright T et al. J Chem. Inf. Model 46:665 Locating active-site hydrogen atoms in d-xylose isomerase: Time of flight neutron diffraction Katz A et al. PNAS (2006) 103(22):8342-7 Screening approach for chiral separation of pharmaceuticals Part III. Supercritical fluid chromatography for analysis and purification in drug discovery Maftouh M et al. Journal of Chromatography A (2005) 1088(1-2):67-81 SAR by ILOE’s: An NMR-Based Approach to Reverse Chemical Genetics Becattini B and Pellecchia M Chem Eur. J. (2006) 12(10):2658-62 Structure-activity relationships by interligand NOE-based design and synthesis of anti-apototic compounds targeting Bid Becattini B et al. PNAS (2006) 103(33):12602-6

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