设计、合成和评估多聚（ADP-核糖）聚合酶成员 1 和 14 的潜在抑制剂。
Design, synthesis and evaluation of potential inhibitors for poly(ADP-ribose) polymerase members 1 and 14.
机构信息
Faculty of Health Sciences & Medicine, Bond University, Robina, QLD 4229, Australia.
出版信息
Future Med Chem. 2020 Dec;12(24):2179-2190. doi: 10.4155/fmc-2020-0218. Epub 2020 Nov 23.
Poly(ADP-ribose) polymerase (PARP) members PARP1 and PARP14 belong to an 18-member superfamily of post-translational modifying enzymes. A library of 9 novel non-NAD analog amine compounds was designed, synthesized and evaluated for inhibitory activity against PARP1 and PARP14. Both studies and assays identified compound as a potential PARP1 inhibitor, inhibiting activity by 93 ± 2% (PARP14 inhibition: 0 ± 6%), and as a potential PARP14 inhibitor, inhibiting activity by 91 ± 2% (PARP1 inhibition: 18 ± 4%), at 10-μm concentration. Key interactions with TYR907 in PARP1 and TYR1620 and TYR1646 in PARP14 have been identified. Compound and compound have been identified as potential leads for the development of selective PARP inhibitors.
多聚（ADP-核糖）聚合酶（PARP）成员 PARP1 和 PARP14 属于一个由 18 个成员组成的翻译后修饰酶超家族。设计、合成并评估了 9 种新型非 NAD 类似物胺化合物库，以评估其对 PARP1 和 PARP14 的抑制活性。两项研究和测定均将化合物 鉴定为潜在的 PARP1 抑制剂，在 10μm 浓度下，对 PARP1 的抑制活性为 93±2%（PARP14 抑制：0±6%），化合物 鉴定为潜在的 PARP14 抑制剂，对 PARP14 的抑制活性为 91±2%（PARP1 抑制：18±4%）。已经确定了与 PARP1 中的 TYR907 和 PARP14 中的 TYR1620 和 TYR1646 的关键相互作用。化合物 和化合物 已被鉴定为开发选择性 PARP 抑制剂的潜在先导化合物。
Zotero 插件