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鸟嘌呤核苷酸交换因子EPAC1中的一个SUMO相互作用基序是亚细胞定位和功能所必需的。

A SUMO-interacting motif in the guanine nucleotide exchange factor EPAC1 is required for subcellular targeting and function.

作者信息

Yang Wenli, Mei Fang, Lin Wei, Lee Jason E, Nie Si, Bley Christopher J, Hoelz André, Cheng Xiaodong

机构信息

Department of Integrative Biology and Pharmacology, The University of Texas Health Science Center, Houston, Texas, USA.

The Brown Foundation Institute of Molecular Medicine for the Prevention of Human Diseases, The University of Texas Health Science Center, Houston, Texas, USA.

出版信息

bioRxiv. 2025 May 3:2025.05.02.651912. doi: 10.1101/2025.05.02.651912.

Abstract

Exchange protein directly activated by cAMP (EPAC1), a multifunctional intracellular cAMP receptor, dynamically localizes to various cellular loci, engaging with diverse molecular partners to maintain cellular homeostasis. The study investigates the role of the SUMO interacting motif (SIM) in the subcellular targeting and cellular functions of EPAC1. It reveals that the SIM is a critical structural element for EPAC1's association with RanBP2/Nup358, a nucleoporin of the cytoplasmic filament component of the nuclear pore complex (NPC). Mutational disruption of EPAC1 SIM interferes with EPAC1's ability to activate its canonical effectors, small GTPases, Rap1 and Rap2, and non-canonical functions, such as the formation of nuclear condensates and cellular SUMOylation. Because SIM is also directly involved in cAMP binding, RanBP2's association with EPAC1 with the SIM attenuates EPAC1's cAMP binding affinity to generate an EPAC1 signaling microdomain with reduced cAMP sensitivity around the NPC. The coupling between EPAC1's scaffold association and cAMP binding enables EPAC1 to tune its sensitivity to stress stimuli spatially depending on the cellular locations. These findings provide novel structural insights into EPAC1 signaling, highlighting the importance of SIM in EPAC1's cellular functions and potential novel strategies for therapeutically targeting EPAC1.

摘要

环磷酸腺苷直接激活的交换蛋白(EPAC1)是一种多功能细胞内环磷酸腺苷受体,可动态定位于各种细胞位点,与多种分子伴侣相互作用以维持细胞内稳态。本研究调查了小泛素样修饰蛋白相互作用基序(SIM)在EPAC1亚细胞定位和细胞功能中的作用。研究表明,SIM是EPAC1与RanBP2/Nup358(核孔复合体(NPC)细胞质丝成分的一种核孔蛋白)结合的关键结构元件。EPAC1 SIM的突变破坏会干扰EPAC1激活其典型效应器小GTP酶Rap1和Rap2的能力,以及非典型功能,如核凝聚物的形成和细胞小泛素样修饰。由于SIM也直接参与环磷酸腺苷结合,RanBP2与带有SIM的EPAC1结合会减弱EPAC1的环磷酸腺苷结合亲和力,从而在NPC周围产生一个对环磷酸腺苷敏感性降低的EPAC1信号微区。EPAC1的支架结合与环磷酸腺苷结合之间的偶联使EPAC1能够根据细胞位置在空间上调节其对应激刺激的敏感性。这些发现为EPAC1信号传导提供了新的结构见解,突出了SIM在EPAC1细胞功能中的重要性以及靶向EPAC1治疗的潜在新策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/05a9/12247920/32869d798c6f/nihpp-2025.05.02.651912v1-f0001.jpg

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