# Sumoylation: A Novel Mechanism for Regulating Drug/Xenobiotic Transporters OATs

> **NIH NIH R01** · RUTGERS, THE STATE UNIV OF N.J. · 2020 · $310,000

## Abstract

Project Summary
Organic anion transporters (OATs) mediate the absorption, distribution, and excretion of a diverse array
of environmental toxins, and clinically important drugs, including anti-cancer drugs, anti-viral agents,
diuretics, antibiotics, anti-hypertensives, and anti-inflammatories. OATs are abundantly expressed in
kidney, liver, brain, and placenta. OAT dysfunction in these organs significantly contributes to the renal,
hepatic, neurological, and fetal toxicity and disease. Our long-term goal is to define the molecular
mechanisms underlying drug disposition through OAT pathway. During the previous grant period,
significant progress and productivity have been achieved, and the new findings from this period led to
the establishment of a fine-tuned research plan and strategy in this competing renewal. We propose to
test the novel hypothesis that post-translational modification of OAT by SUMO conjugation is an
important means of controlling the stability, subcellular localization, and activity of the transporter. Three
Specific Aims are outlined. In Specific Aim I, we will identify the nature of OAT sumoylation. In Specific
Aim II, we will assess the role of sumoylation in OAT-mediated drug transport in cultured cells. In
Specific Aim III, we will evaluate the physiological and pathophysiological relevance of sumoylation in
OAT-mediated drug transport. Combined approaches of biochemistry and molecular biology will be
employed for the proposed studies in cultured cells, in tissue slices, and in animals. Understanding the
role of sumoylation in the regulation of OATs, a novel focus in drug transport field, will have significant
impact on the future design of strategies aimed at maximizing therapeutic efficacy and minimizing
toxicity, and will permit insight into the molecular, cellular, and clinical bases of renal, hepatic,
neurological and fetal toxicity and disease.

## Key facts

- **NIH application ID:** 9990784
- **Project number:** 5R01GM097000-08
- **Recipient organization:** RUTGERS, THE STATE UNIV OF N.J.
- **Principal Investigator:** GUOFENG YOU
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $310,000
- **Award type:** 5
- **Project period:** 2012-06-07 → 2023-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9990784

## Citation

> US National Institutes of Health, RePORTER application 9990784, Sumoylation: A Novel Mechanism for Regulating Drug/Xenobiotic Transporters OATs (5R01GM097000-08). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9990784. Licensed CC0.

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