AI Article Synopsis
- Compound is a strong anticancer agent but raises serum triglycerides, leading to the synthesis of four new rexinoid analogs that do not cause this lipid toxicity.
- Two of these new rexinoids are found to be twice as effective as the original compound in binding to the Retinoid X receptor (RXR).
- Additionally, these new rexinoids effectively reduce inflammation and prevent UVB-induced nonmelanoma skin cancer without causing significant toxicity.
Article Abstract
Compound is a potent rexinoid that is highly effective in cancer chemoprevention but elevates serum triglycerides. In an effort to separate the lipid toxicity from the anticancer activity of , we synthesized four new analogs of rexinoid , of which three rexinoids did not elevate serum triglycerides. Rexinoids and are twice as potent as rexinoid in binding to Retinoid X receptor (RXR). retinoic acid (ATRA) plays a key role in maintaining skin homeostasis, and rexinoids are highly effective in upregulating the genes responsible for the biosynthesis of ATRA. Inflammation plays a key role in skin cancer, and rexinoids and are highly effective in diminishing LPS-induced inflammation. Rexinoids and are highly effective in preventing UVB-induced nonmelanoma skin cancer (NMSC) without displaying any overt toxicities. Biophysical studies of rexinoids and bound to hRXRα-ligand binding domain (LBD) reveal important conformational and dynamical differences in the ligand binding domain.
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Source |
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9942614 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.2c00735 | DOI Listing |
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