Department of Neuroscience and Physiology, Department of Biochemistry and Molecular Medicine, Zilkha Neurogenetic Institute, Keck School of Medicine, University of Southern California, Los Angeles, CA 90033, USA.
Department of Chemistry and Biochemistry, Department of Chemical Engineering, University of California Santa Barbara, Santa Barbara, CA 93106, USA.
Structure. 2019 Oct 1;27(10):1570-1580.e4. doi: 10.1016/j.str.2019.08.003. Epub 2019 Aug 26.
Huntington's disease is caused by a polyQ expansion in the first exon of huntingtin (Httex1). Membrane interaction of huntingtin is of physiological and pathological relevance. Using electron paramagnetic resonance and Overhauser dynamic nuclear polarization, we find that the N-terminal residues 3-13 of wild-type Httex1(Q25) form a membrane-bound, amphipathic α helix. This helix is positioned in the interfacial region, where it is sensitive to membrane curvature and electrostatic interactions with head-group charges. Residues 14-22, which contain the first five residues of the polyQ region, are in a transition region that remains in the interfacial region without taking up a stable, α-helical structure. The remaining C-terminal portion is solvent exposed. The phosphomimetic S13D/S16D mutations, which are known to protect from toxicity, inhibit membrane binding and attenuate membrane-mediated aggregation of mutant Httex1(Q46) due to electrostatic repulsion. Targeting the N-terminal membrane anchor using post-translational modifications or specific binders could be a potential means to reduce aggregation and toxicity in vivo.
亨廷顿病是由亨廷顿蛋白(Httex1)第一外显子中的 polyQ 扩展引起的。亨廷顿蛋白的膜相互作用具有生理和病理相关性。使用电子顺磁共振和 Overhauser 动态核极化,我们发现野生型 Httex1(Q25)的 N 端残基 3-13 形成一个膜结合的、两亲性的α螺旋。该螺旋位于界面区域,对膜曲率和与头部基团电荷的静电相互作用敏感。包含 polyQ 区域前五个残基的 14-22 残基位于过渡区域,该区域仍位于界面区域中,没有形成稳定的α螺旋结构。其余的 C 端部分是溶剂暴露的。已知磷酸模拟 S13D/S16D 突变可以保护免受毒性,由于静电排斥,它会抑制膜结合,并减弱突变型 Httex1(Q46)的膜介导聚集。使用翻译后修饰或特异性结合物靶向 N 端膜锚可能是减少体内聚集和毒性的一种潜在方法。