# Lead optimization and target identification of drugs targeting hypnozoites

> **NIH NIH R01** · UNIVERSITY OF GEORGIA · 2024 · $649,072

## Abstract

PROJECT SUMMARY/ABSTRACT
The goal of this proposal is to optimize a new lead series for treatment of relapsing malaria
caused by Plasmodium vivax. When an infectived mosquito bits she inoculates sporozoites that
invade hepatocytes. Within the hepatocyte the forms can either develop and reproduce or
become dormant. These dormant hypnozoites are the forms that persist for weeks to years and
can reactivate to cause disease. There are no good drugs for treating hypnozoites that are safe,
especially for glucose-6phosphate dehtdriogenase deficient people. In this project wi wil use a
novel liver stage culture system to drive the medicinal chemistry optimization of the new lead
series of drugs with anti-hypnozoite activity. Secondly we aim to use the lead and back up
series to develop chemical probes to identify the targets for hypnozoite killing. Cyrrently there
are no validated targets for drug discovery against hypnozoites. Finally we aim to use a
combination of chemical biology, advanced culture techniques, and new metabolic labelling
approaches to validate the new leads and gthe liver stage culture model.

## Key facts

- **NIH application ID:** 10903784
- **Project number:** 5R01AI153290-05
- **Recipient organization:** UNIVERSITY OF GEORGIA
- **Principal Investigator:** DENNIS E KYLE
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $649,072
- **Award type:** 5
- **Project period:** 2020-08-07 → 2026-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10903784

## Citation

> US National Institutes of Health, RePORTER application 10903784, Lead optimization and target identification of drugs targeting hypnozoites (5R01AI153290-05). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10903784. Licensed CC0.

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