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Affinity Fingerprinting - A novel approach to quantitative chemical classification proves useful in drug discovery

机译:亲和指纹-一种新的定量化学分类方法在药物发现中被证明是有用的

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摘要

We often think that a ligand binding to its target is finding the key that fits a lock. While this simile is useful for describing the complementarity of binding surfaces, it breaks -down when one considers that there are literally thousands of ligands that can bind to a particular target--with varying affinities. The emerging field of combinatoriai chemistry is now teaching us to think of ligand binding as a continuum of specificities; There is not just one key that fits the lock, but many and different keys may even have the same functionality. Drug developers have recognized the importance of this type of cross-reactivity for year's. Careful documentation of this phenomenon for known drugs is one explanation of their unwanted clinical side effects.
机译:我们通常认为配体与其目标结合是在寻找适合锁的钥匙。虽然这个比喻对于描述结合表面的互补性很有用,但当人们认为实际上有成千上万个可以结合到特定靶标上的配体具有不同的亲和力时,它就分解了。组合化学的新兴领域现在教会我们将配体结合视为特异性的连续体。不仅有一个适合锁的钥匙,而且许多不同的钥匙甚至可能具有相同的功能。药物开发人员已经认识到这种交叉反应对于一年的重要性。仔细记录已知药物的这种现象是其不良临床副作用的一种解释。

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