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人转化生长因子 β 型 I 受体与激酶抑制剂 SB505124 的复合物

Human transforming growth factor β type I receptor in complex with kinase inhibitor SB505124.

机构信息

Department of Chemistry, Umeå University, Linnaeus vag 10, 901 87 Umeå, Sweden.

Department of Medical Biosciences, Umeå University, 901 85 Umeå, Sweden.

出版信息

Acta Crystallogr F Struct Biol Commun. 2024 Nov 1;80(Pt 11):314-319. doi: 10.1107/S2053230X24010094. Epub 2024 Oct 23.

Abstract

The crystal structure of the intracellular domain of transforming growth factor β type I receptor (TβR1) in complex with the competitive inhibitor SB505124 is presented. The study provides insights into the structure and function of TβR1 in complex with SB505124, and as such offers molecular-level understanding of the inhibition of this critical signalling pathway. The potential of SB505124 as an avenue for therapy in cancer treatment is discussed on basis of the results.

摘要

转化生长因子β 型 I 受体(TβR1)胞内域与竞争性抑制剂 SB505124 复合物的晶体结构被呈现出来。该研究提供了 TβR1 与 SB505124 复合物的结构和功能的深入了解,从而为该关键信号通路的抑制提供了分子水平的理解。基于研究结果,讨论了 SB505124 作为癌症治疗治疗途径的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/625d/11533363/4b3bd61210a1/f-80-00314-fig1.jpg

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