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首页> 外文期刊>Journal of mass spectrometry: JMS >Affinity selection-mass spectrometry for the discovery of pharmacologically active compounds from combinatorial libraries and natural products
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Affinity selection-mass spectrometry for the discovery of pharmacologically active compounds from combinatorial libraries and natural products

机译：亲和力选择 - 质谱，用于发现组合文库和天然产物的药理学活性化合物

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Invented to address the high-throughput screening (HTS) demands of combinatorial chemistry, affinity selection-mass spectrometry (AS-MS) utilizes binding interactions between ligands and receptors to isolate pharmacologically active compounds from mixtures of small molecules and then relies on the selectivity, sensitivity, and speed of mass spectrometry to identify them. No radiolabels, fluorophores, or chromophores are required. Although many variations of AS-MS have been devised, three approaches have emerged as the most flexible, productive, and popular, and they differ primarily in how ligand-receptor complexes are separated from nonbinding compounds in the mixture. These are pulsed ultrafiltration (PUF) AS-MS, size exclusion chromatography (SEC) AS-MS, and magnetic microbead affinity selection screening (MagMASS). PUF and SEC AS-MS are solution-phase screening approaches, and MagMASS uses receptors immobilized on magnetic microbeads. Because pools of compounds are screened using AS-MS, each containing hundreds to thousands of potential ligands, hundreds of thousands of compounds can be screened per day. AS-MS is also compatible with complex mixtures of chemically diverse natural products in extracts of botanicals and fungi and microbial cultures, which often contain fluorophores and chromophores that can interfere with convention HTS. Unlike conventional HTS, AS-MS may be used to discover ligands binding to allosteric as well as orthosteric receptor sites, and AS-MS has been useful for discovering ligands to targets that are not easily incorporated into conventional HTS such as membrane-bound receptors.
机译：亲和选择质谱（AS-MS）是为了满足组合化学的高通量筛选（HTS）要求而发明的，它利用配体和受体之间的结合作用，从小分子混合物中分离药理活性化合物，然后依靠质谱的选择性、灵敏度和速度来识别它们。不需要放射性标记、荧光团或发色团。虽然AS-MS有许多变体，但有三种方法是最灵活、最有效和最流行的，它们主要不同于配体-受体复合物与混合物中非结合化合物的分离方式。这些是脉冲超滤（PUF）AS-MS、尺寸排除色谱（SEC）AS-MS和磁性微球亲和选择筛选（MagMASS）。PUF和SEC AS-MS是溶液相筛选方法，MagMASS使用固定在磁性微球上的受体。由于使用AS-MS筛选化合物池，每个池都包含数百到数千个潜在配体，因此每天可以筛选数十万个化合物。AS-MS还可与植物、真菌和微生物培养物提取物中化学多样性天然产物的复杂混合物兼容，其中通常含有可干扰常规HTS的荧光团和发色团。与传统HTS不同，AS-MS可用于发现与变构和正构受体位点结合的配体，并且AS-MS可用于发现与不易并入传统HTS（如膜结合受体）的靶点结合的配体。

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