FORTÉBIO

Pioneer Systems

OneStep SPR

Complete solution for biomolecular interaction analysis with next generation SPR injections

Identify hits faster, obtain information-rich data and eliminate sample dilutions

Pioneer SPR systems provide high quality kinetic data (ka, kd) and affinity measurements (KD) to characterise a wide range of biomolecular interactions from small molecule fragments to biologics.  OneStep SPR injections enable faster assay workflows where a single analyte concentration is sufficient for accurate kinetics and affinity determination.

Simplified kinetic characterisations

With OneStep injections, users can obtain accurate kinetic and affinity values from one analyte concentration eliminating the need to run multiple analyte titrations saving time and error associated with making dilutions.  NeXtStep injections provide a simple workflow to characterise competitive binders against a ligand to capture the mechanism of action.

Robust fluidics design

Pioneer fluidic system is made up of inert materials such as PEEK, ceramic and Tefzal providing durability and low maintenance.

Low baseline noise, minimal drift, high sensitivity and up to 40 Hz data collection rate

Extremely low baseline noise and drift enable measurement of reliable kinetics and affinity values for high affinity and challenging binders.  With up to 40 Hz of data acquisition capabilities, Pioneer FE systems are capable of capturing very fast kinetic association and dissociation phases of a wide range of biomolecules and small molecule fragments.

Features

3 channel, fully automated SPR system

With three sensing channels, two target proteins or ligands can be analysed simultaneously for binding with one surface utilised as a reference channel.

Screen 768 fragments in 24 hours

Pioneer FE platform’s high-throughput screening feature enables kinetic screening of 768 small molecule fragments in a single experiment in 24 hours.

Up to 72 hours of unattended run time

Offers a variety of sample vessel formats with up to two 384 well plate capacity with an unattended runtime of about 72 hrs for performing large binding screens.

Rapid data analysis with QDat software and hit selection feature

Pioneer SPR systems are equipped with an integrated, industry-proven data analysis software based on Scrubber and Clamp platforms.  Raw data across multiple runs, days, and sensors can be combined and analysed using binding algorithms such as single site, multi-site binding, mass transport, and irreversible inhibitor analysis as required for analysis.  Hit-selection software feature enables rapid identification of fragment hits that are acquired by Pioneer FE SPR systems.

Gain more data with less

As the analyte gradient is generated in OneStep injections, the diffusion coefficient is calculated that provides an assessment of aggregation enabling users to gain information not only on kinetics and affinity but also on aggregation in just one injection.

Applications

Drug discovery

Pioneer systems accelerate the drug discovery process by providing fast, high quality kinetics to identify targets and characterise drug interactions.  Perform high throughput fragment screening and characterise high affinity biologic interactions with confidence.

  • Affinity & Kinetics
  • Biologics & Small Molecule Research
  • Fragment Based Drug Discovery
  • Lead Characterisation

Characterisation of high affinity biologic interactions

Target binding characterisation is an essential analytical step for the selection of high affinity (KD <1 nM) and highly specific biologics regardless of the types of molecules.  A kinetic analysis further describes the components of association and dissociation that comprise the overall affinity interaction.  For example, two lead compounds may possess a similar affinity (KD) to its target, but their differences in kinetic rate constants of association and dissociation can be used to estimate which will be more useful in vivo.  Accurate analysis of these kinetic rate constants is therefore important information for lead selection and predicting the efficacy of protein therapeutics.  The Pioneer SPR system with next generation SPR injections improves the efficiency of the characterisation process over traditional SPR by determining the kinetics and affinity in a single step.  The next-generation OneStep® gradient injection featured on the Pioneer platform dramatically increases the speed of affinity characterisation while maintaining accuracy and high confidence in results.

Characterise irreversible inhibitors and measure commitment to covalency

The majority of small molecule inhibitor assays tested with label-free, real-time biosensor technologies are reversible interactions, characterised by commonly used kinetic rate models.  However, a significant fraction of therapeutic enzyme inhibitors on the market functions through covalent modification of the target.  ForteBio’s Pioneer FE is a SPR platform that can be used with regenerable Streptavidin biosensors to reversibly capture protein targets and quantify the efficiency of covalent inhibitors binding to the target.  The Pioneer FE system’s irreversible inhibitor applications method can be used to determine inhibitor compound’s commitment to covalency (Cc) as a metric for irreversible inhibitors.

High throughput fragment screening

Fragment-based drug design has become an increasingly popular platform for the identification of lead candidates in drug discovery programs.  The detection and characterisation of fragment binding events is facilitated by sensitive biophysical technologies capable of detecting low affinity interactions of low molecular weight compounds.  SPR has become one of the core technologies used in the identification of these low-affinity fragment compounds.  SPR-based biosensors such as the Pioneer FE have the necessary sensitivity and throughput to provide complete fragment screens on libraries of several thousand compounds in just a few weeks per target.

Systems

Pioneer

Complete solution for biomolecular interaction analysis with Next Generation SPR Injections

Pioneer FE

Make decisions earlier in fragment screens with the Pioneer FE

Specifications

Pioneer Pioneer FE
Number of channels; flowpaths 3 channels; 1, 1–2, 1–2–3, 3, 3–2, 3–2–1
Short term noise < 0.1 RU < 0.035 RU
Limit of detection:
Molecular weight
On-rate ka
Off-rate kd

> 70 Da
102 – 108
10-6 – 0.1

> 70 Da
102 – 109
10-6 – 2.5
Variable data rate 1 – 20 Hz 1 – 40 Hz
Sample temperature control 4 – 40 °C (max 15 °C below ambient)
Sample capacity and configuration 2 sample racks; 96 vial, deep well and PCR formats, 384 well microplates, custom high volume
Simultaneous injections; automation capabilities Yes – dual sample loops; up to 72 hr unattended operation
High throughput screening mode No Yes
Qdat hit selection feature No Yes

About Solve Scientific

Solve Scientific caters to the Australian and New Zealand scientific market with high-quality product and innovative technologies. In close partnership with our suppliers our role is delivering premium local support in enabling our customer’s results.

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