University System of Maryland

Vidya P Ramamurthy

Hannah W Mbatia

Vincent C O Njar

Lalji K Gediya

Vincent Njar

Senthilmurugan Ramalingam

Novel retinamides with unique properties and biological activities, including inhibition of retinoic acid metabolism and modulation of Mnk1/2-eIF4E and androgen receptor (AR) signaling pathways, are synthesized and developed. The novel retinamides are capable of effecting treatment of a variety of dermatological conditions while limiting adverse side effects.

Composition and method for treating dermatological disorders using retinamides

The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In prostate cancer cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. The consequences of these multiple activities resulted in inhibition of cell growth and migration and induction of apoptosis. Finally and importantly, the compounds demonstrate strong in vitro and in vivo anti-breast and anti-prostate cancer activities, with no apparent host toxicities.

Growing community of inventors

Ellicott City, MD, United States of America

Vidya P Ramamurthy