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2017 - Discovery of Compounds that Positively Modulate the High Affinity Choline Transporter

Icon N1  SURFE²R N1 publication in Frontiers in Molecular Neuroscience (2017)

Authors: 
Choudhary P., Armstrong E.J., Jorgensen C.C., Piotrowski M., Barthmes M., Torella R., Johnston S.E., Maruyama Y., Janiszewski J.S., Storer R.I., Skerratt S.E., Benn C.L.

Journal: 
Frontiers in Molecular Neuroscience (2017) 10:40


Abstract: 

Cholinergic hypofunction is associated with decreased attention and cognitive deficits in the central nervous system in addition to compromised motor function. Consequently, stimulation of cholinergic neurotransmission is a rational therapeutic approach for the potential treatment of a variety of neurological conditions. High affinity choline uptake (HACU) into acetylcholine (ACh)-synthesizing neurons is critically mediated by the sodium- and pH-dependent high-affinity choline transporter (CHT, encoded by the SLC5A7 gene). This transporter is comparatively well-characterized but otherwise unexplored as a potential drug target. We therefore sought to identify small molecules that would enable testing of the hypothesis that positive modulation of CHT mediated transport would enhance activity-dependent cholinergic signaling. We utilized existing and novel screening techniques for their ability to reveal both positive and negative modulation of CHT using literature tools. A screening campaign was initiated with a bespoke compound library comprising both the Pfizer Chemogenomic Library (CGL) of 2,753 molecules designed specifically to help enable the elucidation of new mechanisms in phenotypic screens and 887 compounds from a virtual screening campaign to select molecules with field-based similarities to reported negative and positive allosteric modulators. We identified a number of previously unknown active and structurally distinct molecules that could be used as tools to further explore CHT biology or as a starting point for further medicinal chemistry.


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