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Updated: Sep 13, 2025

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结构-活动关系引导的脚手架跳跃导致识别GLPG4970,一种高强度的双SIK2/SIK3抑制剂

Hans Kelgtermans1, Maxim De Wachter1, Stijn Heyndrickx1

  • 1Galapagos NV, 2800 Mechelen, Belgium.

Journal of medicinal chemistry
|July 25, 2025
PubMed
概括

研究人员开发了一种新型SIK2/SIK3抑制剂GLPG4970,作为自身免疫和炎症性疾病的潜在治疗方法. 这种化合物在临床前模型中显示出强大的抑制和有效性,克服了以前的基因毒性问题.

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Assembly of Signaling Complexes01:30

Assembly of Signaling Complexes

Multiprotein signaling complexes are formed in a dynamic process involving protein-protein interactions at the cytoplasmic domain of transmembrane receptors or enzymatic and non-enzymatic proteins associated with the receptor. These complexes ensure the activation and propagation of intracellular signals that regulate cell functions.
Interaction domains in cell signaling
Interaction domains recognize exposed features of their binding partners containing post-translationally modified sequences,...
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