# Split-luciferase Epigenetic Assays for Drug Discovery

> **NIH NIH R43** · LUCEOME BIOTECHNOLOGIES, LLC · 2022 · $240,429

## Abstract

Project Summary
Epigenetic control is essential for maintaining transcriptional integrity. Regulation of the dynamic
epigenome is mediated through a range of post translational modifications on DNA and histone
tails. Histone modifications are mediated by enzymes which can be broadly classified into “writers”
that catalyze the addition of chemical modifications, “erasers” that remove the modifications, and
“readers” that can recognize chemical modifications through specific protein domains. The writing
and erasing of histone marks by enzymes is a dynamic process, and when dysregulated is
associated with cancer, inflammatory and neurological diseases.
In this application we focus on the two classes of histone modifying enzymes, lysine methyl
transferases (KMTs) and lysine demethylases (KDMs), and aim to develop and validate cell-
based assays targeting both KMTs and KDMs. These assays, based on a three-hybrid split
luciferase system, are reversible allowing dose dependent quantification of inhibitor binding.
These efforts are both significant and innovative as they can report on the direct binding of a drug
to the target protein at its intended site of action, thereby facilitating the generation of lead
therapeutic candidates and identification of chemical probes for studying histone biology and
pathways.

## Key facts

- **NIH application ID:** 10482555
- **Project number:** 1R43GM146510-01
- **Recipient organization:** LUCEOME BIOTECHNOLOGIES, LLC
- **Principal Investigator:** REENA ZUTSHI
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $240,429
- **Award type:** 1
- **Project period:** 2022-04-01 → 2024-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10482555

## Citation

> US National Institutes of Health, RePORTER application 10482555, Split-luciferase Epigenetic Assays for Drug Discovery (1R43GM146510-01). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10482555. Licensed CC0.

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