Conference dates: FEBRUARY 3-7, 2024

Booth: 938

Location: Boston Convention & Exhibition Center – Boston, Massachusetts

Speaking session

Title: Easy Kinome Profiling: Synergy of Carna Bioscience’s® Biotinylated Kinases and Carterra’s® HT-SPR™

Speaker: Adam Shutes, PhD, Carna Biosciences

Date and Time: Monday, February 5, 2024 | 2:00 – 2:20 PM EST

Location: Solutions Spotlight Theater (Exhibition 1290)

Abstract: Kinases are an attractive target class across many therapeutic areas. To dig deeper into this target class, mechanisms beyond ATP-competition are actively under investigation including allosteric inhibition, degradation, or as partners in molecular glues.

For these approaches, standard activity assays and even advanced enzymology can only go so far in providing sufficient detail to inform chemistry decisions. Direct label-free approaches, such as SPR binding, provide the intrinsic kinetics of interactions which allow differentiation of compounds and compound series that, although potentially similar in activity assays, ultimately show distinct kinetics. Critically these different mechanisms can have an impact on efficacy in humans.

In this talk we will present the benefits of kinase profiling via HT-SPR technology. Straightforward assay development, enabled by high quality biotinylated kinases, supported rapid screening of a library of small molecule compounds against 87 different kinases. By measuring 384 binding events per cycle, over 80,000 interactions were characterized in a 3-day run. Initial screening data combined with more detailed follow up assays provided a wealth of deep kinetic data which correlated well to activity data thus validating the accuracy of Carterra’s LSAXT platform as well as the quality, activity, and stability of Carna’s biotinylated kinases.

Title: Meeting Scalability Demands for Label-Free Binding Assays in an Evolving Research Landscape

Speaker: Noah T. Ditto, Technical Product Manager, Carterra

Date and Time: Wednesday, February 7, 2024 | 12:00 – 12:20 PM EST

Location: Solutions Spotlight Theater (Exhibition 1290)

Abstract: Drug discovery is undergoing a transformation across many fronts from the implementation of generative AI approaches to the growing resurgence in omics-based strategies as well as the emergence of novel therapeutic modalities. What remains constant however is the fundamental need to deliver high-quality, impactful data in less time using less resources. The historical paradigm of either focusing on either speed or depth of data has resulted in a myriad of assays that excel in one of these areas but under-deliver in the other. Real-time, label-free binding studies using biosensors are no exception and have long been a technology space that while rich in data outputs could never match the throughput requirements of robust research workflows.

HT-SPR, however, is re-writing the way real-time, label-free binding assays are deployed in modern discovery environments. With the ability to screen samples across the spectrum of small molecules to mAbs and approaching 150,000 detailed binding interactions in a single experiment, the Carterra LSAXT operates at an unmatched scale for binding characterization. Importantly, these capabilities come with less resource requirements than any other platform owing to the novel microfluidics of the LSAXT. This talk will highlight the unique advantages of using HT-SPR for highly scaled, real-time, label-free binding with examples across multiple sample types and most importantly how these measurements impact the intelligent selection of drug candidates.

Poster sessions

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

Presenter: Nicholas Abuid, Field Application Scientist, Carterra

Date and Time: Monday, February 5, 2024 | 2:00 – 3:00 PM EST

Location: 1333-B

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 1: Deep characterization of binding kinetics for 210 kinase inhibitors against 80+ kinases

Presenter: Noah T. Ditto, Technical Product Manager, Carterra

Date and Time: Tuesday, February 6, 2024 | 2:00 – 3:00 PM EST

Location: 1255-D

Abstract: As a drug target class, kinases continue to provide a wealth of opportunities for addressing human disease, but often can be challenging to work with in vitro. Additionally, the ubiquitous nature of kinases across many critical pathways means therapeutic targeting this class necessitates careful consideration regarding off-target profiles. Here we highlight the power of combining an extensive panel of active kinases with HT-SPR to generate a wealth of compound binding information. Over 80,000 binding interactions were measured during a 3-day label-free screen. Detailed kinetics were then subsequently obtained for hits of interest. Beyond simple yes/no reporting, this approach allows for nuanced kinetic profiling for up to hundreds of binding events in parallel enabling thoughtful discovery of safe and efficacious drug candidates.