# Targeting through Selective Cell Labeling

> **NIH NIH R01** · UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN · 2020 · $465,127

## Abstract

Biological targeting has been a key concept in cancer treatment. Despite the clinical success of some biological
targeting systems, significant challenges still remain. For example, there are few tumor-specific biomarkers that
are expressed at sufficient high level for targeted drug delivery. Many cancers do not have tumor-specific
biomarkers that are amenable for targeting. One sure example is triple-negative breast cancers (TNBCs), tumors
that do not overexpress estrogen receptor, progesterone receptor and human epidermal growth factor receptor
2. Therefore, there is great need of developing new technology that can be broadly used in the targeting of
cancers, in particular those without natural biomarkers. In this study, we aim to develop azido moiety (N3)-
mannose analogues that are metabolically active only in cancer cells but are not in non-cancerous cells/tissues,
and the metabolism of such azido-mannose analogues lead to “over-expression” of N3 group on cancer cell
surfaces as endogenously inserted tumor biomarkers for in vitro and in vivo Click Chemistry mediated targeting.
Our work will provide an entirely small-molecule-based targeting technology for many cancers that do not have
established biomarkers. We aim to incorporate the use of this new cancer targeting technology in nanomedicine
and develop an effective nanotherapeutics for targeted cancer chemotherapy and immunotherapy against
TNBCs. The key hypotheses to be tested in this project are (1) whether effective in vitro and in vivo cancer
targeting can be achieved based on endogenous insertion of azide, a synthetic chemical functional group, as
the unnatural biomarker, followed by in vitro and in vivo covalent Click Chemistry and (2) whether this new
targeting technology coupled with nanomedicine can be used to treat cancers that are typically non-targetable.

## Key facts

- **NIH application ID:** 9916757
- **Project number:** 5R01EB025651-03
- **Recipient organization:** UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN
- **Principal Investigator:** Jianjun Cheng
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $465,127
- **Award type:** 5
- **Project period:** 2018-08-15 → 2022-04-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9916757

## Citation

> US National Institutes of Health, RePORTER application 9916757, Targeting through Selective Cell Labeling (5R01EB025651-03). Retrieved via AI Analytics 2026-05-25 from https://api.ai-analytics.org/grant/nih/9916757. Licensed CC0.

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