Ravichandran Aravind, Das Ranabir
National Center for Biological Sciences, Tata Institute of Fundamental Research, Bangalore 560065, India.
SASTRA University, Thirumalaisamudram, Thanjavur 613401, India.
ACS Omega. 2024 May 13;9(20):22265-22276. doi: 10.1021/acsomega.4c01396. eCollection 2024 May 21.
Degradation of proteins by the proteasome is crucial in regulating their levels in the cell. Post-translational modifications, such as ubiquitylation and Fat10ylation, trigger proteasomal degradation of the substrate proteins. While ubiquitylation regulates multiple cellular pathways, Fat10ylation functions explicitly in the inflammatory response pathway. At the proteasome, ubiquitin is recycled after being cleaved from the substrate, while Fat10 is degraded simultaneously with its substrate. Although the thermodynamic properties of the substrate are critical for effective proteasomal degradation, they remain poorly understood for the Fat10-proteasome pathway. We studied the thermodynamic properties of the Fat10∼substrate conjugate to uncover mechanistic details of the pathway. First, the mechanical unfolding of Fat10∼substrate was studied by molecular dynamics simulations, which suggested that the unfolding pathway and unfolding energy of the substrate depend on the site of Fat10 modification. We also investigated different pathways for the entry of the Fat10∼substrate into the proteasome core. Our analysis supports a model where the entry of Fat10, followed by the substrate, is the energetically preferred pathway. Further, we studied Fat10's effect on the thermodynamic properties of distinct substrates, considering their size, flexibility, and surface properties. The results uncovered significant entropic destabilization of substrates due to Fat10ylation, particularly in smaller substrates. For larger substrates, multi-monoFat10ylation is necessary to induce destabilization. Our study further reveals that Fat10 modification at negative patches on substrate surfaces is essential for optimal destabilization and subsequent degradation. These findings provide atomistic insights into the degradation mechanisms in the Fat10 proteasome pathway with potential implications for therapeutic interventions.
蛋白酶体对蛋白质的降解在调节细胞内蛋白质水平方面至关重要。翻译后修饰,如泛素化和Fat10ylation,会触发底物蛋白的蛋白酶体降解。虽然泛素化调节多种细胞途径,但Fat10ylation在炎症反应途径中具有明确的功能。在蛋白酶体中,泛素从底物上切割后会被循环利用,而Fat10则与其底物同时降解。尽管底物的热力学性质对有效的蛋白酶体降解至关重要,但对于Fat10-蛋白酶体途径,人们对其了解仍然很少。我们研究了Fat10∼底物共轭物的热力学性质,以揭示该途径的机制细节。首先,通过分子动力学模拟研究了Fat10∼底物的机械展开,结果表明底物的展开途径和展开能量取决于Fat10修饰的位点。我们还研究了Fat10∼底物进入蛋白酶体核心的不同途径。我们的分析支持一种模型,即Fat10先进入,随后底物进入,这是能量上更有利的途径。此外,我们考虑了不同底物的大小、柔韧性和表面性质,研究了Fat10对其热力学性质的影响。结果发现,由于Fat10ylation,底物出现了显著的熵失稳,特别是在较小的底物中。对于较大的底物,需要多次单Fat10ylation才能诱导失稳。我们的研究进一步表明,在底物表面的负电荷区域进行Fat10修饰对于最佳失稳和随后的降解至关重要。这些发现为Fat10蛋白酶体途径的降解机制提供了原子层面的见解,对治疗干预具有潜在意义。