2023年片段到先导物的药物化学出版物。
Fragment-to-Lead Medicinal Chemistry Publications in 2023.
作者信息
Holvey Rhian S, Erlanson Daniel A, de Esch Iwan J P, Farkaš Barbara, Jahnke Wolfgang, Nishiyama Tsuyoshi, Woodhead Andrew J
机构信息
Astex Pharmaceuticals, 436 Cambridge Science Park, Milton Road, Cambridge CB4 0QA, United Kingdom.
Frontier Medicines, 151 Oyster Point Blvd., South San Francisco, California 94080, United States of America.
出版信息
J Med Chem. 2025 Jan 23;68(2):986-1001. doi: 10.1021/acs.jmedchem.4c02593. Epub 2025 Jan 6.
This Perspective summarizes successful fragment-to-lead (F2L) studies that were published in 2023 and is the ninth installment in an annual series. A tabulated summary of the relevant articles published in 2023 is provided (17 entries from 16 articles), and a comparison of the target classes, screening methods, and overall fragment or lead property trends for 2023 examples and for the combined entries over the years 2015-2023 is discussed. In addition, we identify several trends and innovations in the 2023 literature that promise to further increase the success of fragment-based drug discovery (FBDD), particularly in the areas of NMR and virtual screening, fragment library design, and fragment linking.
本综述总结了2023年发表的成功的从片段到先导物（F2L）研究，这是该年度系列的第九篇文章。文中提供了2023年发表的相关文章的表格汇总（来自16篇文章的17个条目），并讨论了2023年实例以及2015 - 2023年所有条目的目标类别、筛选方法和整体片段或先导物性质趋势的比较。此外，我们还确定了2023年文献中的几个趋势和创新点，这些趋势和创新有望进一步提高基于片段的药物发现（FBDD）的成功率，特别是在核磁共振（NMR）和虚拟筛选、片段库设计以及片段连接等领域。
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