Conference dates: FEBRUARY 26, 2023 – MARCH 1, 2023

Booth: 2127

Location: San Diego Convention Center

Speaking session

Title: High-throughput SPR assay for FcγR binding to drug candidates on the new Carterra LSAXT

Speaker: Zachary V. Fagiani

Speaker Title: Research Associate, Dragonfly Therapeutics

Date: Monday, February 27, 2023

Time: 2:00 PST

Location: Solutions Spotlight Theater (#230 in Exhibition)

Abstract: Fc gamma receptor (FcγR) binding is a critical component of ADCC, ADCP, and CDC and an important feature to measure in Fc-containing drugs. The purpose of our study was to determine if testing IgG drugs against a full panel of biotinylated FcγRs can be completed on Carterra’s LSAXTinstrument with higher throughput than a traditional 8-channel biosensor while maintaining equivalent data quality. Our results show that the LSAXT demonstrates highly comparable data relative to the traditional 8-channel biosensor while using 7.5 times less analyte, 6 fewer hours of analyst time, ~$3,000 less in consumables, and producing 8 times as many replicates.

Poster sessions

Poster 1: Large-scale characterization of drug candidates against transmembrane receptors using HT-SPR

Presenter: Rebecca Rich, PhD, Principal Scientist, Carterra

Abstract: Transmembrane targets make up a substantial part of the overall “undruggable” therapeutic space that has recently garnered widespread interest. High-throughput surface plasmon resonance (HT-SPR) is a powerful technique that is transforming characterization workflows and enabling a greater breadth and depth of information for up to thousands of drug candidates. This workflow highlights opportunities to perform detailed binding characterization for up to thousands of drug candidates in parallel, accelerating the discovery of drug candidates targeting transmembrane receptors.

Poster 2: Selectivity and cooperativity of PROTAC®s using HT-SPR

Presenter: Rebecca Rich, PhD, Principal Scientist, Carterra

Abstract: The unique heterobifunctional nature of PROTAC®s necessitates expanding the toolbox of characterization techniques to enable efficient drug discovery. Multiple warhead and linker combinations must be tested against the target protein(s) and ligases. Highlighted here is a strategy to characterize both binary and ternary kinetics for PROTAC®s against a panel of E3 ligases, targets, and off-targets in parallel. Utilizing HT-SPR, a comprehensive assessment of both detailed binding selectivity and cooperativity can be obtained quickly using very small quantities of reagents.

Poster 3: Increasing DEL Compound Screening Resolution Using HT-SPR

Presenter: Noah Ditto, Technical Product Manager, Carterra

Abstract: While a huge benefit to DNA encoded library (DEL) technology is its reduction in the sheer number and tracking of discrete compounds through the screening process, it does come with a limitation in binding properties that can be gleaned from potential hits. To address this resolution gap in DEL screening, demonstrated here is a technique to further characterize hits with improved resolution using high-throughput surface plasmon resonance (HT-SPR). With a screening capacity of thousands per week, HT-SPR affords a high-resolution technique that matches the throughput needs during discovery between the full library and a handful of well-validated leads.

Poster 4: Extending the Applications Space of HT-SPR

Presenter: Noah Ditto, Technical Product Manager, Carterra

Abstract: HT-SPR has transformed how real-time, label free binding is deployed in modern, sophisticated drug discovery processes. These transformations have come from both substantial gains in throughput and reduced sample amounts. Described here is an expansion to the breadth of assays and applications HT-SPR can address by improvements in sensitivity and overall data quality. With these improvements, the versatility of HT-SPR can now be more easily leveraged in more challenging assay types such as PROTACs and kinase inhibitors.