Identification of Anticancer Drug Candidate Targeting Nuclear Receptor Retinoid X receptor‐α from Natural Products using Receptor‐Ligand Recognition

Abstract

Natural products (NP), especially medicinal plants, have been used worldwide to treat numerous diseases for thousands of years. However, drug discovery focus has been moving away from identifying lead compounds from complex mixtures of crude NP because this approach is technically difficult and inefficient. We here present a quick, accurate and practical method for screening leads targeting a nuclear receptor from NP mixtures. Using themethod, we rapidly identified erythrotriol as a new lead compoundfrom medicinal plant Hibiscus syriacus L.targeting RXRα for treating cancer with less side effects. This method can efficiently and profitably screen lead compounds targeting nuclear receptors and may reinvigorate interest in NP as sources of pharmaceutical agents.

Celastrol-regulated gut microbiota and bile acid metabolism alleviate hepatocellular carcinoma proliferation by regulating the interaction between FXR and RXRα in vivo and in vitro

“…A dual-luciferase reporter assay was performed as described in our previous study ( Hu et al, 2017 ; Luo et al, 2016 ). Briefly, after being transfected with pBind FXR LBD and pGL5 luc and treated with CDCA and/or GUDCA, HEK-293T cells were lysed with 50 μL 1× passive lysis buffer.…”