Edward A. Doisy Department of Biochemistry and Molecular Biology, Saint Louis University School of Medicine, St. Louis, MO.
Washington University Center for Cellular Imaging, Washington University School of Medicine, St. Louis, MO.
Blood. 2023 Jun 29;141(26):3215-3225. doi: 10.1182/blood.2022019486.
Coagulation factor V (fV) is the precursor of activated fV (fVa), an essential component of the prothrombinase complex required for the rapid activation of prothrombin in the penultimate step of the coagulation cascade. In addition, fV regulates the tissue factor pathway inhibitor α (TFPIα) and protein C pathways that inhibit the coagulation response. A recent cryogenic electron microscopy (cryo-EM) structure of fV has revealed the architecture of its A1-A2-B-A3-C1-C2 assembly but left the mechanism that keeps fV in its inactive state unresolved because of an intrinsic disorder in the B domain. A splice variant of fV, fV short, carries a large deletion of the B domain that produces constitutive fVa-like activity and unmasks epitopes for the binding of TFPIα. The cryo-EM structure of fV short was solved at 3.2 Å resolution and revealed the arrangement of the entire A1-A2-B-A3-C1-C2 assembly. The shorter B domain stretches across the entire width of the protein, making contacts with the A1, A2, and A3 domains but suspended over the C1 and C2 domains. In the portion distal to the splice site, several hydrophobic clusters and acidic residues provide a potential binding site for the basic C-terminal end of TFPIα. In fV, these epitopes may bind intramolecularly to the basic region of the B domain. The cryo-EM structure reported in this study advances our understanding of the mechanism that keeps fV in its inactive state, provides new targets for mutagenesis and facilitates future structural analysis of fV short in complex with TFPIα, protein S, and fXa.
凝血因子 V(fV)是激活的 fV(fVa)的前体,是凝血级联反应倒数第二步中凝血酶原快速激活所必需的凝血酶原酶复合物的重要组成部分。此外,fV 还调节组织因子途径抑制剂 α(TFPIα)和蛋白 C 途径,抑制凝血反应。最近的一项冷冻电子显微镜(cryo-EM)结构研究揭示了 fV 的 A1-A2-B-A3-C1-C2 组装结构,但由于 B 结构域的固有无序性,仍未解决使 fV 保持非活性状态的机制。fV 的剪接变体 fV short 缺失了 B 结构域的大部分,导致其具有组成性的 fVa 样活性,并暴露出与 TFPIα 结合的表位。fV short 的 cryo-EM 结构以 3.2 Å 的分辨率解决,并揭示了整个 A1-A2-B-A3-C1-C2 组装的排列。较短的 B 结构域横跨整个蛋白质的宽度延伸,与 A1、A2 和 A3 结构域接触,但悬在 C1 和 C2 结构域之上。在远离剪接位点的部分,几个疏水区和酸性残基提供了 TFPIα 碱性 C 末端的潜在结合位点。在 fV 中,这些表位可能在分子内与 B 结构域的碱性区域结合。本研究报道的 cryo-EM 结构增进了我们对使 fV 保持非活性状态的机制的理解,为突变研究提供了新的靶点,并促进了未来 fV short 与 TFPIα、蛋白 S 和 fXa 复合物的结构分析。