Centre for Medicines Discovery, Nuffield Department of Medicine Research Building, University of Oxford, Roosevelt Drive, Oxford OX3 7FZ, UK.
Centre for Medicines Discovery, Nuffield Department of Medicine Research Building, University of Oxford, Roosevelt Drive, Oxford OX3 7FZ, UK.
Structure. 2024 Oct 3;32(10):1586-1593.e4. doi: 10.1016/j.str.2024.07.023. Epub 2024 Aug 26.
KCTD family proteins typically assemble into cullin-RING E3 ligases. KCTD1 is an atypical member that functions instead as a transcriptional repressor. Mutations in KCTD1 cause developmental abnormalities and kidney fibrosis in scalp-ear-nipple syndrome. Here, we present unexpected mechanistic insights from the structure of human KCTD1. Disease-causing mutation P20S maps to an unrecognized extension of the BTB domain that contributes to both its pentameric structure and TFAP2A binding. The C-terminal domain (CTD) shares its fold and pentameric assembly with the GTP cyclohydrolase I feedback regulatory protein (GFRP) despite lacking discernible sequence similarity. Most surprisingly, the KCTD1 CTD establishes a central channel occupied by alternating sodium and iodide ions that restrict TFAP2A dissociation. The elucidation of the structure redefines the KCTD1 BTB domain fold and identifies an unexpected ion-binding site for future study of KCTD1's function in the ectoderm, neural crest, and kidney.
KCTD 家族蛋白通常组装成 CUL3-RING E3 连接酶。KCTD1 是一种非典型成员,反而作为转录抑制剂发挥作用。KCTD1 突变会导致头皮-耳-乳头综合征的发育异常和肾脏纤维化。在这里,我们从人 KCTD1 的结构中提供了意想不到的机制见解。致病突变 P20S 映射到未被识别的 BTB 结构域延伸,该延伸有助于其五聚体结构和 TFAP2A 结合。尽管缺乏明显的序列相似性,但 C 末端结构域 (CTD) 与其折叠和五聚体组装共享 GTP 环水解酶 I 反馈调节蛋白 (GFRP)。最令人惊讶的是,KCTD1 CTD 建立了一个由交替的钠离子和碘离子占据的中央通道,限制了 TFAP2A 的解离。结构的阐明重新定义了 KCTD1 BTB 结构域的折叠,并确定了一个意想不到的离子结合位点,用于进一步研究 KCTD1 在外胚层、神经嵴和肾脏中的功能。