# A MULTISCALE APPROACH TO TARGET THE ACHILLES HEEL OF P53 CANCER MUTANTS (Equipment Supplement)

> **NIH NIH R01** · UNIVERSITY OF CALIFORNIA, SAN DIEGO · 2020 · $84,000

## Abstract

SUMMARY
p53 is arguably one of the most important tumor suppressor proteins in humans. In almost 50%
of all human cancers, p53 is found to be nonfunctional mostly due to single point mutations. The
primary goals of this proposal are to gain a detailed understanding of the effect of most-frequent
p53 cancer mutations on the protein structure and dynamics, and to leverage a novel
computational methodology that identifies small molecules able to reactivate destabilized p53
cancer mutants—a method that represents a promising new approach to drug discovery. We aim
to extend our understanding of the structural dynamics of truncated and full-length p53 with state-
of-the-art molecular dynamics simulations in order to discovery novel druggable pockets that have
not yet been experimentally characterized. Subsequently we plan to use this new structural
information to identify small molecules with novel mechanisms of action and reveal new potential
therapeutic avenues targeting this vital transcription factor.

## Key facts

- **NIH application ID:** 10153341
- **Project number:** 3R01GM132826-02S1
- **Recipient organization:** UNIVERSITY OF CALIFORNIA, SAN DIEGO
- **Principal Investigator:** Rommie E Amaro
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $84,000
- **Award type:** 3
- **Project period:** 2019-04-01 → 2023-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10153341

## Citation

> US National Institutes of Health, RePORTER application 10153341, A MULTISCALE APPROACH TO TARGET THE ACHILLES HEEL OF P53 CANCER MUTANTS (Equipment Supplement) (3R01GM132826-02S1). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10153341. Licensed CC0.

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