Click Chemistry Probes for Specific Targeting of Sialic Acid Tumor Antigens


Technology: Researchers at MUSC have identified methods for selectively modifying linked sialic acid or polysialic acid with bioorthagonal reaction schemes having applications broad applications in drug delivery. This is achieved by exposing a 2,3 linked sialic acid and/or a 2,8 linked polysialic acid to condensing reagents under suitable reaction conditions. The selectively modified sialic acid can be paired with a payload molecule (molecule used to deliver an active agent) to induce a biological or physiological effect to the subject. The payload molecule can range from a pharmaceutical drug to polynucleotide modifying agents such as CRISPR. Furthermore, the linked sialic acid and/or polysialic acid can be incorporated with other biological molecules such as antibodies, peptides, proteins, carbohydrates etcetera to help the chemical attach to a desired area. By using this sialic/polysialic acid as a label paired with optically active imaging modalities, cancer cells expressing the markers can be easily targeted.

Figure 1.  Shows an exemplary reaction wherein a 2,3 linked sialic acid is modified to possess a click chemistry alkyne or azide feature. It can now be utilized for targeted delivery of a payload.  The same functional change is not seen with the 2,6 linked sialic acid.


Overview: Despite the availability of bioorthagonal reaction schemes and reagents, there still exists a need for new reactions, reagents, and/or methods that can improve, for example, the efficiency, the specificity, and/or the application of bioorthagonal reactions.  This specific method has great utility in targeting cancer cells. Small molecule targeted cancer therapy can use medication to block cancerous growth by destroying molecules that result in the growth of tumors, preventing the need for harmful radiations that see wide use in conventional cancer treatment.  The targeted approach and minimal after side-effects. This along with the increase in the rate of cancer incidences are contributing to the growth of the market [1]. The global small molecule drug discovery market was valued at $29,363.85 million USD in 2018, and is estimated to be valued at $46,882.22 million USD in 2024, witnessing a CAGR of 8.11% [2]. There is a large market for these targeted drug therapies, and this new technology has the potential to tap into this market.


Applications: cancer cell targeting, glycan engineering, microscopic imaging, analytic composition, CRISPR, drug delivery, pharmaceutical formulations, mass spectrometry



1.       Broad Applications – Drugs, CRISPR, immunomodulator, antibody, antipyretic, chemotherapeutic, anti-neoplastic agent, anti-fungal, anti-bacterial, anti-viral, a pain modulating agent, anti-microbial agent, anti-infective agent

2.       Cancer Labeling – Can be used as a label to target cells expressing cancerous genes


Key Words: Bioorthagonal chemistry, specificity, reagents, pharmacology, cancer treatment, drug delivery, labeling


Inventors: Richard Drake, Xiaowei Lu       


Patent Status:       U.S. Provisional Patent Serial No. 63/010,499 filed April 15, 2020       


MUSC-FRD Technology ID: P20075






Patent Information:
For Information, Contact:
Docket BioPharma
Zucker Institute of Innovation Commercialization powered by MUSC
Richard Drake
Xiaowei (Vivian) Lu
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