# Role of small molecule interactions and multiprotein assemblies in CYP1B1 disease-associated function and dysfunction

> **NIH NIH R01** · UNIVERSITY OF KENTUCKY · 2021 · $124,564

## Abstract

Abstract
The goal of this project is to determine how mutations, elevated protein levels, and environmental
conditions impact the function and dysfunction of Cytochrome P450 1B1 (CYP1B1). The addition of
instrumentation is proposed to facilitate characterization of small molecule modulators of CYP1B1, and
the metabolic products of this CYP. Selective inhibition of CYPs is an important goal in medicinal
chemistry, but these enzymes can chemically modify their inhibitors, resulting in deactivation. The
requested High Pressure Liquid Chromatography (HPLC) instrument, along with three orthogonal
detection systems, will allow for accurate and rapid determination of chemical structures and enzymatic
modifications. This will be accomplished with small amounts of sample, as the analytes will come from
cells grown in tissue culture. As CYPs generally increase the polarity of hydrophobic substrates, the
instrumentation includes specific modifications that are required for analysis of aqueous media
solutions. Such solutions are incompatible with most LC mass spectrometers. This equipment will be
also used to evaluate if mutations, protein:protein association, and environmental conditions alter CYP
metabolic products, with implications for tissue-selective metabolism under hypoxia or due to the
presence of signaling molecules.

## Key facts

- **NIH application ID:** 10389514
- **Project number:** 3R01GM138882-02S1
- **Recipient organization:** UNIVERSITY OF KENTUCKY
- **Principal Investigator:** Edith C Glazer
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $124,564
- **Award type:** 3
- **Project period:** 2020-09-01 → 2024-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10389514

## Citation

> US National Institutes of Health, RePORTER application 10389514, Role of small molecule interactions and multiprotein assemblies in CYP1B1 disease-associated function and dysfunction (3R01GM138882-02S1). Retrieved via AI Analytics 2026-05-28 from https://api.ai-analytics.org/grant/nih/10389514. Licensed CC0.

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