AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.
AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.
复制标题
DOI：
10.1002/trc2.12246
复制
发表时间：
2022
影响因子：
4.8
通讯作者：
Axtman, Alison D
中科院分区：
文献类型：
--
作者：
Potjewyd, Frances M;Annor-Gyamfi, Joel K;Aube, Jeffrey;Chu, Shaoyou;Conlon, Ivie L;Frankowski, Kevin J;Guduru, Shiva K R;Hardy, Brian P;Hopkins, Megan D;Kinoshita, Chizuru;Kireev, Dmitri B;Mason, Emily R;Moerk, Charles T;Nwogbo, Felix;Pearce, Kenneth H;Richardson, Timothy I;Rogers, David A;Soni, Disha M;Stashko, Michael;Wang, Xiaodong;Wells, Carrow;Willson, Timothy M;Frye, Stephen V;Young, Jessica E;Axtman, Alison D
治疗阿尔茨海默病(AD)的新靶点组合因阿尔茨海默病加速药物合作计划(AMP AD)计划而得到丰富。公开可用的资源，如文献和数据库，使数据驱动的努力能够确定由AMP AD提名的基因表达的许多蛋白质产品的现有小分子调节剂和适当的阳性对照化合物，以纳入该集合。用相关的公布、预测和/或实验数据手动选择和注释包含在该集合中的化合物。我们构建了一套带有注释的171个小分子调节剂，靶向98个独特的蛋白质，这些蛋白质已被AMP AD联盟成员提名为治疗AD的新靶点。包括在该集合中的大多数化合物都是抑制剂。这些小分子的质量各不相同，应该被认为是可以用于验证治疗假说的化学工具，但需要进一步优化。可以在Target Enablement to Accelerate Treatment Development for阿尔茨海默病(Treat-AD)网站上索取AD信息者集的物理副本。能够进行靶向验证的小分子是将新的假说转化为可行的AD治疗策略的重要工具。
The portfolio of novel targets to treat Alzheimer's disease (AD) has been enriched by the Accelerating Medicines Partnership Program for Alzheimer's Disease (AMP AD) program. Publicly available resources, such as literature and databases, enabled a data‐driven effort to identify existing small molecule modulators for many protein products expressed by the genes nominated by AMP AD and suitable positive control compounds to be included in the set. Compounds contained within the set were manually selected and annotated with associated published, predicted, and/or experimental data. We built an annotated set of 171 small molecule modulators targeting 98 unique proteins that have been nominated by AMP AD consortium members as novel targets for the treatment of AD. The majority of compounds included in the set are inhibitors. These small molecules vary in their quality and should be considered chemical tools that can be used in efforts to validate therapeutic hypotheses, but which will require further optimization. A physical copy of the AD Informer Set can be requested on the Target Enablement to Accelerate Therapy Development for Alzheimer's Disease (TREAT‐AD) website. Small molecules that enable target validation are important tools for the translation of novel hypotheses into viable therapeutic strategies for AD.