Development Partnerships
The Dimerix GPCR-HIT platform’s unique features of functionality and performance in the identification and investegation of GPCR heteromers has application to the pharmaceutical industry at various stages of the drug development process, including library screening and compound profiling.
Depending on the project scope required, Dimerix is able to work with partners to leverage the utility of the GPCR-HIT platform, and also Dimerix’ depth of knowledge in the field.
In summary, our GPCR-HIT capability and our insights to GPCR heteromerisation have relevance and potential for application in the following areas:
- Novel GPCR Heteromer Targets: Identification of heteromer receptor combinations formed by any GPCR monomer of interest, followed by investigation of ß-arrestin signal profile;
- Drug Discovery: Screening and/or profiling of hits and lead candidates for their heteromer specific signal effects, leading to the development of safer drugs with increased specificity of action (i.e. best in class drugs);
- Drug Profiling: Profiling of development/clinical stage candidates and marketed drugs and analogues for their heteromer specific signal effects; and
- Candidate Re-evaluation & Re-positioning: Profiling of discontinued development candidates and marketed drugs for their heteromer-specific effects, including the generation of fixed dose combination products with novel modes of action.
Screening
Dimerix’ GPCR-HIT assay platform is able to be integrated with existing industry GPCR screening programs, either as a primary or secondary screen. Depending on the size of the compound library to be screened and custom configuration required (if any), Dimerix is able to work closely with commercial partners optimise the assay in the desired configuration.
Illustrative example of performance of GPCR-HIT in HTS application
Profiling
In addition to use in library screening, Dimerix’ GPCR-HIT platform also has application in profiling of development stage and marketed compounds for optimisation of their signalling profile to include heteromer effects. The understanding and optimisation of heteromer effects may be essential to explain and ultimately manage certain off-target or confounding data observed in vivo.
Dimerix has demonstrated biased β-arrestin signalling through a proprietary heteromer target with implications for currently marketed drugs targeting monomer receptors that form the heteromer complex.
