# Novel Targeted Anticancer Agents from Marine Cyanobacteria

> **NIH NIH R01** · UNIVERSITY OF FLORIDA · 2021 · $439,130

## Abstract

PROJECT SUMMARY
Cyanobacteria are among the most ancient organisms on Earth and have evolved chemical weapons for
defensive purposes, which we are exploiting for anticancer drug discovery. Our past research has exemplified
that marine cyanobacteria produce compounds with exceptionally potent activity and/or possess unusual or first-
in-class inhibitors with novel mechanisms of action. We apply a broad yet focused screening platform to
maximize discovery rate of new anticancer agents. We also integrate a synthetic chemistry component into our
program in order to perform rigorous biological studies to rapidly add value to our discoveries and to help solve
the supply problem. Specifically, we will carry out field collections of marine cyanobacteria and prepare fraction
libraries for screening in a set of innovative pathway-focused cell-based assays, utilizing various isogenic
colorectal cancer cell lines and reporter gene assays, as well as newly developed unbiased phenotypic assays.
We will perform dereplication, identify cyanobacteria through molecular analysis and establish phylogenetic
relationships among benthic cyanobacteria. Samples will be prioritized based on bioactivity profiles and genetic
uniqueness for further processing. Prioritized samples will be subjected to bioassay-guided isolation of the active
compounds. Structures will be determined using NMR and mass spectrometry. Basic validation of bioactivity
and secondary assays will be performed before prioritizing targets for further investigation. Selected compounds
with intriguing structure and promising validated bioactivity will be targeted for total synthesis so that a rigorous
biological characterization can be performed to pinpoint the molecular changes induced in the cancer cell and to
determine potential direct targets. For novel noncytotoxic compounds that show potential antimetastatic activity,
we will apply an orthogonal target-based screening platform.

## Key facts

- **NIH application ID:** 10246927
- **Project number:** 5R01CA172310-08
- **Recipient organization:** UNIVERSITY OF FLORIDA
- **Principal Investigator:** HENDRIK LUESCH
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $439,130
- **Award type:** 5
- **Project period:** 2013-03-06 → 2024-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10246927

## Citation

> US National Institutes of Health, RePORTER application 10246927, Novel Targeted Anticancer Agents from Marine Cyanobacteria (5R01CA172310-08). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10246927. Licensed CC0.

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