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Small Molecules


Copenhagen-based Biotech Pcovery To Extend Collaboration With Enamine

   by Andrii Buvailo    2987

Founded in 2009, Pcovery is a Danish biotech startup company involved in drug discovery to fight invasive fungal infections. On November 22, 2016 Pcovery announced the extension of collaboration with a leading producer of building blocks and screening libraries -- Enamine Ltd. In the ongoing drug discovery program, Pcovery will utilize Enamine’s experience in synthesis of small compound libraries and singletons, route scouting, process optimization, and scale-up of lead compounds.

A Second Chance for Integrins: Biotech Startup Morphic Therapeutic Reinvents Old Target

   by Andrii Buvailo    1691

Integrins are a group of transmembrane receptors playing a major role in cell-cell and cell-extracellular matrix (ECM) interactions. When triggered, integrin receptors transduce signals to the interior of the cell, providing quick and flexible “status update” about chemical composition and mechanical status of the ECM. It results in a cellular response, such as a change in the cell shape, regulation of the cell cycle, adjusting motility, or adding new receptors to the cell membrane.

What Chemicals Are Popular Among Medicinal Chemists?

   by Andrii Buvailo    2090

 

Increasing the success rate of high-throughput screening (HTS) and the quality of the resulting hits as well as developability of drug candidates is among the key challenges of small molecule drug discovery programs.

The above goals are associated with so called “compound quality” or “drug-likeness” of the starting small molecules. While the majority of considerations in this context is related to  lead-like properties, physicochemical properties, diversity, effective coverage of the chemical space, privileged structures for drugs or structures possessing favourable physical properties or metabolic stability, it was shown in a recent analysis by F.W. Goldberg et al. (2014) that an effective and somewhat overlooked strategy to increase the compound quality is to focus closer on the choice of the building blocks used in the course of drug discovery programs.  The nature of the selected building blocks determines not only the speed of the research but also the quality of the resulting drug candidates and their potential in further trials.

Obviously, some reagent classes are more popular than others due to historically synthetic routes adopted by organic and medicinal chemists.