Screening potential P-glycoprotein inhibitors by combination of a detergent-free membrane protein extraction with surface plasmon resonance biosensor

Cao, Yuhong; Fang, Jiahao; Shi, Yiwei; Wang, Hui; Chen, Xiaofei; Liu, Yue; Zhu, Zhenyu; Cao, Yan; Hong, Zhanying; Chai, Yifeng

doi:10.1016/j.apsb.2022.03.016

Cited by 13 publications

(7 citation statements)

References 35 publications

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“…As shown in Figure A–D, a significant increase in signal intensity of BBR was observed after coperfusion with three individual compounds in four intestinal segments as compared to BBR alone. Consistent with previous studies, EVO, TET, , and GIN Rg3 could act as potential P-gp inhibitors. In duodenum, all three potential P-gp inhibitors promoted the intestinal absorption of BBR.…”

Section: Resultssupporting

confidence: 91%

Evaluation of Intestinal Drug Absorption and Interaction Using Quadruple Single-Pass Intestinal Perfusion Coupled with Mass Spectrometry Imaging

Tang

Zhang

et al. 2023

Anal. Chem.

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Visualization and characterization of the intestinal membrane transporter-mediated drug absorption and interaction are challenging due to the complex physical and chemical environment. In this work, an integrated strategy was developed for in situ visualization and assessment of the drug absorption and interaction in rat intestines using quadruple single-pass intestinal perfusion (Q-SPIP) technique coupled with matrix-assisted laser desorption ionization mass spectrometry imaging (MALDI MSI). Compared with the traditional SPIP only available for perfusion of one single intestinal segment, the Q-SPIP model can simultaneously perfuse four individual segments of each rat intestine (duodenum, jejunum, ileum, and colon), enabling to obtain rich data from one rat. Subsequently, the drug distribution and absorption in rat intestinal tissue were accurately visualized by using an optimized MALDI MSI approach. The utility and versatility of this strategy were demonstrated via the examination of P-glycoprotein (P-gp)-mediated intestinal absorption of berberine (BBR) and its combination with natural products possessing inhibitory potency against P-gp. The change in the spatial distribution of BBR was resolved, and MALDI results showed that the signal intensity of BBR in defined regions was enhanced following coperfusion with P-gp inhibitors. However, enhanced absorption of BBR after coperfusion with the P-gp inhibitor was not observed in the ulcerative colitis rat model, which may be due to the damage to the intestinal barrier. This study exemplifies the availability and utility of Q-SPIP coupled with MALDI MSI in the examination of transporter-mediated intestinal drug absorption and interaction for fundamental inquiries into the preclinical prediction of oral absorption and drug interaction potential.

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Section: Resultssupporting

confidence: 91%

Evaluation of Intestinal Drug Absorption and Interaction Using Quadruple Single-Pass Intestinal Perfusion Coupled with Mass Spectrometry Imaging

Tang

Zhang

et al. 2023

Anal. Chem.

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“…SPR biosensor is special in the application of screening out bioactive molecules as it can measure the affinity and kinetics of bimolecular binding in a label-free fashion with low reagent consumption ( Cao et al, 2022 ). As shown in Fig.…”

Section: Resultsmentioning

confidence: 99%

Grifolamine A, a novel bis-γ-butyrolactone from Grifola frondosa exerted inhibitory effect on α-glucosidase and their binding interaction: Affinity and molecular dynamics simulation

Chen

Mu²,

Yong³

et al. 2022

Current Research in Food Science

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“…Nevertheless, SMALPs have been extensively used for characterizing binders to membrane proteins. For example, to identify inhibitors of P-glycoprotein (P-gp), which is highly expressed in cancer cells and responsible for multidrug resistance of anticancer drugs, Cao et al used P-gp SMALP-functionalized surface plasmon resonance (SPR) biosensors to screen fifty natural compounds, identifying five P-gp ligands that increased the cells' drug susceptibility [49]. To study the signaling of parathyroid hormone receptor 1 (PTH1R), Sarkar, et al used PTH1R-SMALPs and SPR to investigate its interaction with antibodies targeting the extracellular domain of PTH1R [50,51].…”

Section: Smalpsmentioning

confidence: 99%

Methods for Engineering Binders to Multi-Pass Membrane Proteins

Thomas,

Chockalingam,

Chen

2023

Bioengineering

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Numerous potential drug targets, including G-protein-coupled receptors and ion channel proteins, reside on the cell surface as multi-pass membrane proteins. Unfortunately, despite advances in engineering technologies, engineering biologics against multi-pass membrane proteins remains a formidable task. In this review, we focus on the different methods used to prepare/present multi-pass transmembrane proteins for engineering target-specific biologics such as antibodies, nanobodies and synthetic scaffold proteins. The engineered biologics exhibit high specificity and affinity, and have broad applications as therapeutics, probes for cell staining and chaperones for promoting protein crystallization. We primarily cover publications on this topic from the past 10 years, with a focus on the different formats of multi-pass transmembrane proteins. Finally, the remaining challenges facing this field and new technologies developed to overcome a number of obstacles are discussed.

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Screening potential P-glycoprotein inhibitors by combination of a detergent-free membrane protein extraction with surface plasmon resonance biosensor

Cited by 13 publications

References 35 publications

Evaluation of Intestinal Drug Absorption and Interaction Using Quadruple Single-Pass Intestinal Perfusion Coupled with Mass Spectrometry Imaging

Evaluation of Intestinal Drug Absorption and Interaction Using Quadruple Single-Pass Intestinal Perfusion Coupled with Mass Spectrometry Imaging

Grifolamine A, a novel bis-γ-butyrolactone from Grifola frondosa exerted inhibitory effect on α-glucosidase and their binding interaction: Affinity and molecular dynamics simulation

Methods for Engineering Binders to Multi-Pass Membrane Proteins

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