دورية أكاديمية
Construction and application of H1R ligand screening materials based on SMA stabilization and his-tag covalent immobilization of membrane proteins.
| العنوان: | Construction and application of H1R ligand screening materials based on SMA stabilization and his-tag covalent immobilization of membrane proteins. |
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| المؤلفون: | Shan Y; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., Xia Z; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., An M; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., Yang W; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., Wang S; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., Yang F; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., He L; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China., Wang C; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China. Electronic address: chengwang@mail.xjtu.edu.cn., He H; School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, PR China. Electronic address: hehuaizhen@xjtu.edu.cn. |
| المصدر: | Journal of chromatography. A [J Chromatogr A] 2024 Aug 16; Vol. 1729, pp. 465057. Date of Electronic Publication: 2024 Jun 06. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Country of Publication: Netherlands NLM ID: 9318488 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-3778 (Electronic) Linking ISSN: 00219673 NLM ISO Abbreviation: J Chromatogr A Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Amsterdam ; New York : Elsevier, 1993- |
| مواضيع طبية MeSH: | Maleates*/chemistry , High-Throughput Screening Assays*/methods , Receptors, Histamine H1*/chemistry , Receptors, Histamine H1*/metabolism, Ligands ; Humans ; Histidine/chemistry ; Animals ; Immobilized Proteins/chemistry ; Immobilized Proteins/metabolism ; CHO Cells ; Membrane Proteins/chemistry ; Membrane Proteins/metabolism ; Histamine H1 Antagonists/chemistry ; Polystyrenes/chemistry ; Cricetulus ; Oligopeptides/chemistry |
| مستخلص: | The histamine H1 receptor (H1R) plays a pivotal role in allergy initiation and undergoes the necessity of devising a high-throughput screening approach centered on H1R to screen novel ligands effectively. This study suggests a method employing styrene maleic acid (SMA) extraction and His-tag covalent bonding to immobilize H1R membrane proteins, minimizing the interference of nonspecific proteins interference while preserving native protein structure and maximizing target exposure. This approach was utilized to develop a novel material for high-throughput ligand screening and implemented in cell membrane chromatography (CMC). An H1R-His-SMALPs/CMC model was established and its chromatographic performance (selectivity, specificity and lifespan) validated, demonstrating a significant enhancement in lifespan compared to previous CMC models. Subsequently, this model facilitated high-throughput screening of H1R ligands in the compound library and preliminary activity verification of potential H1R antagonists. Identification of a novel H1R antagonist laid the foundation for further development in this area. Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2024. Published by Elsevier B.V.) |
| فهرسة مساهمة: | Keywords: Cell membrane chromatography; His-tag; Histamine H1 receptor; Membrane protein immobilization; Styrene maleic acid (SMA) |
| المشرفين على المادة: | 0 (Ligands) 0 (Maleates) 0 (Receptors, Histamine H1) 4QD397987E (Histidine) 0 (Immobilized Proteins) 0 (Membrane Proteins) 0 (Histamine H1 Antagonists) 0 (Polystyrenes) 0 (Oligopeptides) 25300-64-5 (styrene-maleic acid polymer) |
| تواريخ الأحداث: | Date Created: 20240610 Date Completed: 20240615 Latest Revision: 20240628 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1016/j.chroma.2024.465057 |
| PMID: | 38857565 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1873-3778 |
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| DOI: | 10.1016/j.chroma.2024.465057 |