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Bio Information Technologies Ltd.

This article was originally published in Start Up

Executive Summary

The hunt for drugs that act on G-protein coupled receptors (GPCR) presents a unique challenge in drug discovery, because pharmaceutical researchers don't possess the three-dimensional structure of a single therapeutically relevant GPCR, crucial information that provides a starting point for understanding the function of a receptor, and then designing drugs that bind to it. The founders of Bio-IT have created a program that works at the atomic level to predict the three-dimensional structures of GPCRs. The model uses as inputs amino acid sequence information, geometric algorithms, and physicochemical factors.

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G-Protein Coupled Receptors

It has always been popular to start companies around families and subfamilies of targets, banking on the similarity among the receptors to speed drug discovery. But the idea largely hasn't panned out, in part because of the new target risk--sometimes they're not pharmaceutically relevant and sometimes they resist the available chemistries. That's why G-protein coupled receptors (GPCRs) have been so important: they're clearly relevant (many, perhaps most, blockbusters come from this class of receptor) and their unique structure makes them both relatively easy to hit with ligands and likely to do something when hit. But the same structural advantages turn into scientific disadvantages for researchers: they resist screening and other techniques of modern drug discovery. We explore some of the newest approaches to mining this rich vein of opportunity.

Norak Biosciences Inc.

Norak's founders think that beta-arrestin's movement from within the body of the cell to the membrane-bound receptor is a specific marker of GPCR receptor activation-and their method for watching it all happen in glowing green is the basis of the company's Transfluor technology.

Axovan Ltd.

Using proprietary high-throughput screening techniques, Axovan is now identifying compounds that bind to GPCRs with high affinity. It reduces screening time by taking into account the homology between receptors, which enables it to screen up to eight receptors in parallel: the company claims to be the only one able to screen up to 30 GPCR receptors per year.

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