# Core 2: RXR Rexinoid Design and Synthesis

> **NIH NIH P01** · UNIVERSITY OF ALABAMA AT BIRMINGHAM · 2020 · $201,786

## Abstract

Non-melanoma skin cancers (NMSCs) are the most common skin malignancy and in organ
transplant patients the incidence of these cancers increase by 10 to 250 fold. The NMSCs in
transplant recipients are more aggressive in behavior. Therefore, prevention of NMSC in
transplant patients is a high priority. While retinoids are generally effective in prevention of
NMSC, these agents are associated with severe lipid toxicities thus precluding them from
chronic administration. The overall objective of the program project is to identify a potent and
safe rexinoid and translate it into clinical use for prevention of NMSCs. Towards achieving this
goal, Core 2 will synthesize rexinoids to support the aims of Project 2, Project 3 and Core 3.
Our laboratory has developed two separate structural classes of rexinoids, which are highly
effective in preventing cancers without increasing the lipid levels. One example of these new
rexinoids is UAB30, which is also being tested against NMSC and is effective in preclinical
models at preventing NMSC without increasing the lipid levels. In addition to UAB30, a second
structural class of retinoids is being developed which are also effective in cancers. Core 2 will
support projects 2, 3 and Core 3 by providing them with required quantities of UAB30 and
UAB110. Core 2 will also synthesize new 3rd generation rexinoids which are more potent and
have an excellent safety profile. The proposed new analogs will utilize structural templates of
UAB30 and UAB110, and add a limited number of substituents. The rationale for the placement
of the substituents is based on our hypothesis that a ‘hot-spot’ in the ligand binding pocket for
the rexinoid is important to initiate lipid biosynthesis. In the design of new rexinoids, the
Synthetic Core will employ x-ray crystallography, and quantum mechanical calculations.

## Key facts

- **NIH application ID:** 10007603
- **Project number:** 5P01CA210946-04
- **Recipient organization:** UNIVERSITY OF ALABAMA AT BIRMINGHAM
- **Principal Investigator:** Venkatram Reddy Atigadda
- **Activity code:** P01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $201,786
- **Award type:** 5
- **Project period:** 2017-09-01 → 2022-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10007603

## Citation

> US National Institutes of Health, RePORTER application 10007603, Core 2: RXR Rexinoid Design and Synthesis (5P01CA210946-04). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10007603. Licensed CC0.

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