Carl E. Wagner

TL;DR: It is shown that these novel derivatives were more effective agents than bexarotene for preventing lung carcinogenesis induced by a carcinogen and have an improved safety profile, and novel pyrimidinyl (Py) analogues of two known chemopreventive rexinoids are evaluated in a new paradigm.

TL;DR: The results suggest that certain structural motifs, particularly the basic frameworks found in analog 4 and analog 9, represent important starting points to exploit in generating additional rexinoids for future study and therapeutic applications.

TL;DR: These methods have general applicability beyond this NEt-TMN case study, and can be employed to characterize and biologically evaluate other putative RXR agonists (rexinoids), and benchmarked against perhaps the most common rexinoid known as bexarotene (Bex).

TL;DR: Experimental data supporting analysis of differential gene expression of human cutaneous T cell lymphoma cell culture cells treated with bexarotene or a variety of rexinoids and a novel method for analyzing gene expression in the context of a model of ligand mechanism, called the Divergence Score are presented.

TL;DR: The methods described in this chapter concern procedures for the design, synthesis, and in vitro biological evaluation of an array of potent retinoid-X-receptor (RXR) agonists employing 6-(ethyl(5,5,8,8-tetramethyl-5,6,7,8 -tetrahydronaphthalen-2-yl)amino)nicotinic acid (NEt- TMN), and recently reported NEt-TM