# High-Throughput Screening Platform for Cancer Drug Discovery

> **NIH NIH R33** · PALO ALTO RESEARCH CENTER · 2020 · $720,575

## Abstract

Project Summary
Targeted therapies have shown great promise in the treatment of cancer. High-throughput screening (HTS)
campaigns have often relied on assays using labeled ligands or enzyme substrates. Artifacts associated with
labeling have led to the erroneous identification of compounds that act in on the labeled substrate rather than
the intended target. A label-free, solution-based HTS method will facilitate identification of compounds acting
specifically on the intended targets. The goals of this proposed project are to advance development and
validate this calorimetry platform as an accessible approach for high throughput ITC analysis, demonstrating its
advantages to study a variety of cancer therapeutic targets.
To achieve this goal, we will improve mixing of reagents in droplets, multiplex temperature readout from
individual droplets, automate fluidic handling and data analysis, and validate the applicability of the improved
technology to study: 1) SH2 domain/phosphopeptide interactions, 2) spleen tyrosine kinase (Syk) enzyme
activity, and 3) Bromodomain/acetylated histone peptide interactions, further applied in small molecule
screening.
The realization of the spectro-optical calorimetry technology platform will enable full thermodynamic
characterization of binding and enzymatic reactions at the throughput of 1536-well plate assays but with
significantly reduced assay development time and larger numbers of repeats and analyte concentrations. The
combination of increased throughput and reduced sample consumption will change the way researchers view
calorimetry: rather than being seen as a technique for a limited number of high-value measurements, it will be
viewed as a primary screening method for cancer therapeutic targets.

## Key facts

- **NIH application ID:** 9935941
- **Project number:** 1R33CA240191-01A1
- **Recipient organization:** PALO ALTO RESEARCH CENTER
- **Principal Investigator:** Michael Recht
- **Activity code:** R33 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $720,575
- **Award type:** 1
- **Project period:** 2020-06-01 → 2023-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9935941

## Citation

> US National Institutes of Health, RePORTER application 9935941, High-Throughput Screening Platform for Cancer Drug Discovery (1R33CA240191-01A1). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/9935941. Licensed CC0.

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