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Identification of a novel HASPIN inhibitor and its synergism with the PLK1 inhibitor
bioRxiv - Pharmacology and Toxicology Pub Date : 2022-09-03 , DOI: 10.1101/2022.09.01.506282
Eun-Ji Kwon , Karishma K. Mashelkar , Juhee Seo , Yoonze Shin , Kisu Sung , Sung Chul Jang , Sang Won Cheon , Haeseung Lee , Byung Woo Han , Sang Kook Lee , Lak Shin Jeong , Hyuk-Jin Cha

Background HASPIN, a mitotic kinase for Histone H3, is a promising target for anti-cancer therapy. However, as HASPIN is an atypical kinase with low similarity to eukaryotic protein kinases, development of a HASPIN inhibitor from the conventional pharmacophore of kinase inhibitors would be technically challenging.

中文翻译:

一种新型 HASPIN 抑制剂的鉴定及其与 PLK1 抑制剂的协同作用

背景HASPIN 是组蛋白 H3 的有丝分裂激酶,是一种有希望的抗癌治疗靶点。然而,由于 HASPIN 是一种非典型激酶,与真核蛋白激酶的相似性低,因此从激酶抑制剂的常规药效团开发 HASPIN 抑制剂在技术上具有挑战性。
更新日期:2022-09-07
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