Highly efficient GPCR immobilization with enhanced fouling resistance, salt tolerance, and chromatographic performance

Qiao, Sai; Zheng, Xinxin; Ou, Yuanyuan; Li, Ting; Zhao, Xue; Quan, Jia; Zhao, Xinfeng; Li, Qian

doi:10.1016/j.colsurfb.2024.113818

Cited by 2 publications

(1 citation statement)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Benefiting from high specificity and stability, immobilized receptor chromatography is considered the most robust and powerful method for investigating binding interactions between drugs and receptors. It is also highly effective for screening bioactive compounds targeting receptors from complex matrices (Li et al, 2022(Li et al, , 2024Qiao et al, 2024;Wang et al, 2022;Yuan et al, 2022). The angiotensin II type 1 receptor (AT 1 R) is a key target for drugs used to treat coronary heart disease, hypertension, congestive heart failure, and other cardiovascular diseases (Guyenet, 2006;Dupont and Brouwers, 2010;Legat et al, 2019).…”

Section: Introductionmentioning

confidence: 99%

Screening and analysis of the targeted compounds in Choerospondias axillaris extract by receptor chromatographic column with immobilized angiotensin II type 1 receptor

Ji,

Li,

Zhang

et al. 2024

Biomedical Chromatography

Self Cite

View full text Add to dashboard Cite

As a result of the lack of modern techniques, the study of Tibetan medicine has been hindered in identifying bioactive compounds. Herein, we established a chromatographic approach using an immobilized angiotensin II type 1 receptor (AT1R) via a one‐step method triggered by haloalkane dehalogenase. The bioactive compounds from Choerospondias axillaris (Guangzao) were screened and identified using the immobilized AT1R followed by MS. Frontal analysis (FA) and adsorption energy distribution (AED) were used to evaluate the association constants. Molecular docking was used to investigate the binding configurations, and the surface efficiency index, binding efficiency index, and ligand‐lipophilicity efficiency (LLE) were calculated to assess the drug‐like properties. The results identified naringenin, pinocembrin, and chrysin as the compounds that specifically bind to AT1R in Guangzao. FA and AED confirmed that there is only one type of binding site between these compounds and AT1R. The association constants were (2.40 ± 0.02) × 104 M−1 for naringenin (5.22 ± 0.26) × 104 M−1 for pinocembrin, and (4.27 ± 0.14) × 104 M−1 for chrysin, respectively. These compounds can bind with AT1R through the orthosteric binding pocket. Naringenin exhibited better LLE than pinocembrin and chrysin. These results confirmed the feasibility of using the immobilized AT1R column for screening and analyzing bioactive compounds in Tibetan medicines.

show abstract