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Alzheimer’s Disease, the “One-Molecule, One-Target” Paradigm, and the Multitarget Directed Ligand Approach
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2018-02-21 00:00:00 , DOI: 10.1021/acschemneuro.8b00069
María Jesús Oset-Gasque 1, 2 , José Marco-Contelles 3
Affiliation  

No selective drugs exist, and we have been designing, synthesizing, and evaluating multitarget-directed ligands since the beginning of modern medicinal chemistry, without knowing it, most possibly. The challenge to discover the efficient Multi-Target Small Molecules (MTSMs) for Alzheimer’s disease (AD) therapy implies to identify the key combination of biological targets to modulate them, thus including in the design the corresponding pharmacophoric groups able to do it. Universal and polyvalent pharmacophoric groups, able to modulate diverse receptors or enzymatic systems, would simplify the drug discovery process leading to new and more efficient MTSMs for AD.

中文翻译:

阿尔茨海默氏病,“一分子,一靶标”范例和多靶标定向配体方法

自从现代药物化学开始以来,我们就一直不知道它是否存在选择性药物,并且自从我们设计,合成和评估多靶标定向配体以来,就一直不知道它是什么。寻找有效的用于阿尔茨海默氏病(AD)治疗的多靶标小分子(MTSM)的挑战意味着确定生物靶标的关键组合以调节它们,从而在设计中包括能够做到这一点的相应药效基团。能够调节多种受体或酶系统的通用和多价药效基团将简化药物发现过程,从而导致新的和更有效的AD MTSMs。
更新日期:2018-02-21
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