Application Note | April 23, 2024

Cell Surface Proteomics for Radioligand Therapies: Profiling Cancer Cell Receptors

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Radioligands are a powerful modality in cancer treatment, offering utility as both a diagnostic tool and as a precision therapy. Comprised of a radioactive isotope linked to a cell-targeting ligand, radioligands are designed to selectively bind to cell receptors that are overexpressed on tumor cells. The radiation emitted by the radioligand can be used to destroy or inhibit the target cancer cells while minimizing damage to surrounding healthy tissue. Radioligand binding proteomics is an essential component in the development of these therapies, as efficacy and safety depends on the binding optimization of radioligand to its cell receptor target.

To limit toxic liability and enable a wider therapeutic window, it is imperative to comprehensively characterize cell surface receptors that are overexpressed, mutated, or uniquely expressed in cancer cells.

Explore how Sapient’s /Deep/ Cell Surface Proteomics approach method is optimized to measure cell surface receptors at unprecedented depth and scale. This mass spectrometry-based method captures and measures the abundances of up to 1,000 well defined cell surface proteins in as little as 20ug protein lysates, to identify those receptors that are differentially expressed on cancer cells.

Download the Application Note to learn the technical details of our method for radioligand binding proteomics, which features fully automated end-to-end sample preparation for rapid turnaround and is readily scalable from tens to thousands of biosamples.

In fact, our /Deep/ Cell Surface Proteomics workflow can be used to rapidly perform global proteomic experiments or can selectively enrich cell surface proteins to screen different cell lines, tissues, and tumors. This can be performed within and across varied cell lines and tumor samples to discover novel cancer cell receptors for radioligand targeting.

Importantly, our workflow not only provides information on the abundances of tumor receptors but can also provide an estimation of their copy numbers. Quantification of protein copy numbers within and across indications helps to prioritize receptors as key targets for radioligand therapies.

By leveraging ultra-sensitive mass spectrometry and innovative workflows, we empower sponsors with actionable data to make informed decisions on cancer cell receptor selection, ultimately driving the optimization of radioligands for enhanced efficacy and safety as precision medicines for cancer.

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