Department of Biological Sciences, Indian Institute of Science Education and Research (IISER) Bhopal, Bhopal 462066, India.
Department of Biological Sciences, Indian Institute of Science Education and Research (IISER) Bhopal, Bhopal 462066, India.
Structure. 2024 Nov 7;32(11):2107-2122.e3. doi: 10.1016/j.str.2024.09.012. Epub 2024 Oct 4.
PINK1 and Parkin mutations lead to the early onset of Parkinson's disease. PINK1-mediated phosphorylation of ubiquitin (Ub), ubiquitin-like protein (NEDD8), and ubiquitin-like (Ubl) domain of Parkin activate autoinhibited Parkin E3 ligase. The mechanism of various phospho-Ubls' specificity and conformational changes leading to Parkin activation remain elusive. Herein, we show that compared to Ub, NEDD8 is a more robust binder and activator of Parkin. Structures and biophysical/biochemical data reveal specific recognition and underlying mechanisms of pUb/pNEDD8 and pUbl domain binding to the RING1 and RING0 domains, respectively. Also, pUb/pNEDD8 binding in the RING1 pocket promotes allosteric conformational changes in Parkin's catalytic domain (RING2), leading to Parkin activation. Furthermore, Parkinson's disease mutation K211N in the RING0 domain was believed to perturb Parkin activation due to loss of pUb binding. However, our data reveal allosteric conformational changes due to N211 that lock RING2 with RING0 to inhibit Parkin activity without disrupting pNEDD8/pUb binding.
PINK1 和 Parkin 突变导致帕金森病的早发。PINK1 介导的泛素 (Ub)、泛素样蛋白 (NEDD8) 和 Parkin 的泛素样 (Ubl) 结构域的磷酸化激活了自抑制的 Parkin E3 连接酶。导致 Parkin 激活的各种磷酸化 Ubl 的特异性和构象变化的机制仍不清楚。在此,我们表明与 Ub 相比,NEDD8 是 Parkin 的更强结合物和激活剂。结构和生物物理/生物化学数据揭示了 pUb/pNEDD8 和 pUbl 结构域分别与 RING1 和 RING0 结构域结合的特异性识别和潜在机制。此外,pUb/pNEDD8 在 RING1 口袋中的结合促进了 Parkin 催化结构域 (RING2) 的变构构象变化,导致 Parkin 激活。此外,由于 pUb 结合的丧失,RING0 结构域中的帕金森病突变 K211N 被认为会扰乱 Parkin 的激活。然而,我们的数据揭示了由于 N211 引起的变构构象变化,该变化锁定了 RING2 与 RING0 以抑制 Parkin 活性,而不破坏 pNEDD8/pUb 结合。