|
|
| The View From Here These studies raise a number of important questions, two of which dominate the selection of articles presented here. Firstly, how can we expand the set of druggable protein domains? A new “-omics” seems to be emerging with “pocketomics”, the science of binding sites suitable for small molecule ligands. Successful application of “pocketomics” leads to the second issue: how do we adapt pre-clinical evaluation strategies to provide valid predictions for the clinical usefulness of novel targets? Target validation continues to be a limiting factor for the drug industry, and some of the articles listed below summarize recent developments in this area. There is little information in the literature about a third issue: is there a strong biological reason why certain protein families like the GPCRs have been so successful as drug targets, or have they been favoured by bias in the published literature, assays, and screening protocols? Most likely this question will only be answered in hindsight many years from now. Fortunately, at least one of the issues about druggability might be settled now. Most authors now spell it with a double g ;-) Enjoy the read! Andreas Russ University Lecturer |
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, but has provided a very useful and detailed overview of the molecular mechanisms of well-established therapies. Irrespective of differences in methodology and definitions, the most recent publications converge on 200-400 proteins from only a handful of domain families as the targets of all marketed drugs.