# Development of human 12/15-lipoxygenase therapeutics for stroke

> **NIH NIH UH3** · MASSACHUSETTS GENERAL HOSPITAL · 2020 · $661,539

## Abstract

Summary
The goal is to develop novel therapeutics effective in stroke. This will be achieved by advancing
candidate molecules toward clinical application utilizing our assay cascade to identify novel,
selective inhibitors of the 12/15 lipoxygenase that protect against ischemic stroke. Our drug
discovery approach will be to synthesize novel ligands based on the ML351 scaffold that are
potent inhibitors of the human 12/15 lipoxygenase and that protect neurons against oxidative
stress-related cell death. Candidate molecules will undergo profiling to assess criteria
specifically related to the physicochemical properties of compounds in a therapeutic setting,
including enzyme selectivity and tests to determine potential interactions with key metabolic
enzyme systems. Best candidates will be evaluated in a battery of tests for protection against
experimental stroke in mice and rabbits.

## Key facts

- **NIH application ID:** 9922389
- **Project number:** 5UH3NS106854-03
- **Recipient organization:** MASSACHUSETTS GENERAL HOSPITAL
- **Principal Investigator:** KLAUS VAN LEYEN
- **Activity code:** UH3 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $661,539
- **Award type:** 5
- **Project period:** 2018-05-01 → 2022-02-28

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9922389

## Citation

> US National Institutes of Health, RePORTER application 9922389, Development of human 12/15-lipoxygenase therapeutics for stroke (5UH3NS106854-03). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/9922389. Licensed CC0.

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