August 2007
Volume 2, Issue 8
Druggability
     
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Sr Principal Scientist
Pfizer Inc.
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Screening and Compound Profiling Biologist
GlaxoSmithKline
Harlow - Essex, South East, UK

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Eli Lilly
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Andreas Russ
The View from Here
Andreas Russ

Druggability is a very pragmatic concept that summarizes which biochemical pathways we can modulate with a given technical toolkit. The analysis of the targets of our current set of approved drugs turned out to be much more challenging than expected...
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A review of 2006


  Top Reviews
Predicting protein druggability

Hajduk PJ, Huth JR and Tse C
Drug Discovery Today

The ability to predict whether a particular protein can bind with high affinity and specificity to small, drug-like compounds based solely on its 3D structure has been a longstanding goal of structural biologists and computational scientists...

Identifying and validating novel targets with in vivo disease models: Guidelines for study design

Anders H-J and Vielhauer V
Drug Discovery Today

In vivo studies are an important tool for the identification and validation of novel drug targets in medicine; however, the interpretation of submitted and published data is often ompromised by inadequate study design...

Finding new drug targets in the 21st century

Lindsay MA
Drug Discovery Today

The past 30 years have witnessed a steady decline in the number of new drug targets. This review concentrates on the initial process of target identification and argues that current problems have resulted from a decrease in clinical research, an overemphasis on the discovery of new targets...


  Abstracts of Key Research Articles

Predicting protein interaction sites: binding hot-spots in protein-protein and protein-ligand interfaces
Burgoyne N, Jackson R
Bioinformatics 2006; 22(11): 1335-42

sc-PDB: an annotated database of druggable binding sites from the Protein Data Bank
Kellenberger E, Muller P, Schalon C, Bret G, Foata N, Rognan D
J Chem Inf Model 2006; 46(2): 717-27

Drug-target identification in Drosophila cells: combining high-throughout RNAi and small-molecule screens
Perrimon N, Friedman A, Mathey-Prevot B, Eggert US.
Drug Discov Today
. 2007;12(1-2):28-33

From the similarity analysis of protein cavities to the functional classification of protein families using cavbase
Kuhn D, Weskamp N, Schmitt S, Hullermeier E, Klebe G
J Mol Biol. 2006; 359(4): 1023-44

Healthy animals and animal models of human disease(s) in safety assessment of human pharmaceuticals, including therapeutic antibodies
Dixit R and Boelsterli UA
Drug Discov Today. 2007;12(7-8):336-42

Transgenic animals and their impact on the drug discovery industry
Dunn DA, Pinkert CA, Kooyman DL
Drug Discov Today. 2005;10(11):757-67

Structure-based maximal affinity model predicts small-molecule druggability
Cheng AC, Coleman RG Smyth KT, Cao Q, Soulard P, Caffrey DR, Salzberg AC, Huang ES
Nat Biotechnol 2007; 25(1): 71-5

Functional human tissue assays
Hillier C and Bunton D
Drug Discov Today 2007;12(9-10):382-8

Orphan enzymes could be an unexplored reservoir of new drug targets
Lespinet O and Labedan B
Drug Discov Today 2006; 11(7-8):300-5

Pocketome via comprehensive identification and classification of ligand binding envelopes
An J, Totrov M, Abagyan R
Mol Cell Proteomics. 2005;4(6):752-61


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