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Dimerix Bioscience Pty. Ltd.

This article was originally published in Start Up

Executive Summary

Dimerix Bioscience is using its proprietary assay technology to identify GPCRs that act in pairs to form GPCR heterodimers. These receptor pairs bind ligands differently, and trigger alternate signaling pathways to stand-alone GPCR monomers, which have provided the model for most drug discovery in this area to date. This understanding, gained over the last decade or so, that some GPCRs act in groups of two or more, raises the possibility of using several types of ligands to elicit precisely the response pattern required from the individual GPCRs within the pair. Thus for example if one GPCR leads to a positive effect and the other to a negative one, scientists might combine an agonist to generate the positive effect, and an antagonist to block the negative response.

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Start-Up Previews (02/2009)

A preview of the emerging health care companies profiled in the current issue of Start-Up. This month's profile group, "Building the Next-Generation of GPCR-Targeting Drugs," features profiles of Catena Pharmaceuticals, Dimerix Bioscience, Heptares Therapeutics and Trevena. Plus these Start-Ups Across Health Care: Carmat, Glycan Biosciences, Itero and MaRVis Technologies.

Trevena Inc.

Trevena has carved out a niche in seeking so-called 'biased ligands'--GPCR-binding compounds that selectively activate just one (or a few) of the many biological pathways mediated via a particular GPCR complex. By identifying a ligand that hits the pathways responsible for a medicine's benefits, and avoiding those behind the ill effects, the company hopes to develop safer and more effective therapies, initially in CNS and cardiovascular disease.

Catena Pharmaceuticals Inc.

Catena Pharmaceuticals is seeking anti-angiogenic GPCR-antagonist compounds, and has a license to one that targets a subset of GPCRs specific for lysophosphatidic acid (LPA). LPA is one of a family of fatty molecules called lysophospholipids that is generating increasing interest among scientists for their role in cell proliferation and inflammation. The company says its small molecules have shown early promise in a number of indications, from oncology to fibrosis and neuropathic pain. Catena will concentrate initially on developing antagonists to LPA receptors for the treatment of solid tumors.

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