# New paradigms for Hsp90 inhibition

> **NIH NIH R01** · UNIVERSITY OF NOTRE DAME · 2020 · $354,105

## Abstract

The 90 kDa heat shock proteins (Hsp90) are responsible for the maturation of approximately 200 client protein
substrates, most of which are associated with signaling cascades that regulate cellular growth and
proliferation. Therefore, Hsp90 inhibition provides a novel approach toward the treatment of cancer as
numerous signaling cascades can be derailed through inhibition of the Hsp90-dependent protein folding
process. In this application, we propose to develop selective inhibitors of the Hsp90 Isoforms, Grp94, Hsp90α,
and Hsp90β, using a structure-guided approach. In addition, we will perform side by side evaluation of these
compounds against pan-inhibitors both in vitro and in vivo to validate our approach. Together, these methods
will provide a new approach for selective inhibition of Hsp90 and will provide a new paradigm for anti-cancer
drug development.

## Key facts

- **NIH application ID:** 10000886
- **Project number:** 5R01CA213566-04
- **Recipient organization:** UNIVERSITY OF NOTRE DAME
- **Principal Investigator:** Brian S J Blagg
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $354,105
- **Award type:** 5
- **Project period:** 2017-09-15 → 2021-11-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10000886

## Citation

> US National Institutes of Health, RePORTER application 10000886, New paradigms for Hsp90 inhibition (5R01CA213566-04). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10000886. Licensed CC0.

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