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Drug Discovery Insights


How Many Drug Targets Are There? A Status Update Review

   by Alfred Ajami    3170

The question is often raised, but the answer remains to be uncovered because the definition of drug "target" continues to evolve.  Historical conceptualization is focused on catalytic sites, substrate binding sites, or epigenetic modification sites. Current understanding that protein-protein interactions are druggable, along with the emerging realization that "nodes" in signaling pathways and biological networks themselves can be manipulated with small molecules in non-traditional ways, has opened up new targeting options. This review is intended to provide a status update, and you can also access a list of 36 actionable web resources for target hunting.

How CRISPR Transforms Modern Drug Discovery

   by Alfred Ajami    2432

Consensus seems universal and the news about it flows literally by the minute over gene editing as a future therapy, complete with patent sagas and ethical conundrums. But at the bench, CRISPR's impact is also proving disruptive, and revolutionary, soon to irrevocably change the mechanics of drug discovery and pre-clinical development in multiple ways. One particular set of  CRISPR applications should be on every drug hunter's radar: disease relevant cellular reporter models manipulated to reflect disease phenotypes.

How To Hunt For Drugs In Dark Chemical Matter

   by Alfred Ajami    2384

Pharma productivity has remained a daunting challenge, notably because R&D departments have been shuffled and reorganized over the last few years in attempts to revitalize the process. One trend, among multiple parallel tracks, has come into fashion. With millions of compounds in inventory, why not re-examine the ones that have consistently shown no activity in bioassays (and presumed are safe if inactive also in toxicological assays) rather than re-invent new ones? Enter the concept of exploring Dark Chemical Matter (DCM).

Converging Trends Brings Organic Electrochemistry To The Front Line Of Drug Discovery

   by Alfred Ajami    2973
Converging Trends Brings Organic Electrochemistry To The Front Line Of Drug Discovery

In a case of "back to the future", chemists at Scripps collaborating with instrument engineers at IKA have unveiled a powerful tool for electrifying chemistry to achieve complex reactions. The ElectraSyn is expected to change approaches to 3D-molecules, late-stage derivatization, and focused library construction, while promoting environmentally conscious chemistry. The teaser graphic here is from Ref. 5 in the text that follows.