Partnering - Track Record

Sareum's experienced team has developed and completed a broad range of high quality structure-based drug discovery programmes, and provided tailored research services to a wide variety of customers over many years. Our founders and scientists have a successful track record of:

Expressing completely novel proteins
Solving difficult protein structures
Finding hits for previously intractable targets
Developing novel lead compounds
Creating high quality pre-clinical drug candidates

Our track record is strongest where our biology, computational and synthetic chemistry skills have been fully integrated in structure-based discovery programmes. We have also delivered successful results in each stage of the discovery value chain from gene to structure, structure to lead and lead to candidate. For the selected set of protein targets in our Crystal Bank we have already developed robust routes that allow us to rapidly produce ligand-protein co-complex crystal structure data.

Discovery Programmes

Examples of our team members' track record in full discovery programmes include use of:

Protein structures to modify a client's lead chemical series to overcome patent issues by scaffold replacement in one month.
Homology models and crystal structures to progress a client's project from hit to pre-clinical candidate selection in two years.
Template-based approach to generate hits and progress project though to pre-clinical candidate selection.

Gene to Structure

Examples of our team members' track record in gene to structure programmes include:

Successfully expressed a selection of novel genomic target proteins in a rapid time frame using proprietary high throughput expression systems. The client had previously not been able to make these proteins in their laboratories using standard baculoviral or E.coli expression methods.
Enabled our client to unravel difficult SAR by providing high resolution crystal structures in just 4 weeks (at a resolution of less than 1.5 angstroms). This project provided both robust ligand soaking and ligand co-crystallisation procedures to allow rapid data generation.
Rapidly expression-profiled client's novel genomic targets to prioritise their internal medicinal chemistry resource.
Solving multiprotein complex structures which provided our client with data on which to make a go/no-go decision on a drug discovery project.

Structure to Lead

Examples of our team members' track record in structure to lead programmes include:

Use of Sareum's template-based x-ray crystallography technology to generate multiple novel chemical lead series on a protein target which had failed in our client's high throughput screening.
Synthesis of a focused library which immediately provided our client with hits as potent as 200 picomolar. The selectivity of these hits meant that they were the only chemical matter taken forward into medicinal chemistry programs.
Use of Structure activity relationship information to design successful novel small molecule agonists to a peptide binding GPCR target.

Lead to Candidate

Examples of our team members' track record in lead to candidate programmes include:

Provided rapid weekly turnaround of protein structures containing ligands from international client that greatly focused lead optimisation.
Used our computational chemistry expertise to progress a number of client's programmes through lead optimisation.
Provided structural information on enzyme isoform selectivity that enabled our client to progress their project to pre-clinical candidate selection.
Generated protein structures for our client that allowed rescue and progression of lead inhibitor series.