Smith Cameron, Hajisadeghian Mohsen, van Noort Gerbrand J van der Heden, Deery Michael J, Pinto-Fernández Adán, Kessler Benedikt M, Artavanis-Tsakonas Katerina
Department of Pathology, University of Cambridge, Cambridge, United Kingdom.
Department of Cell and Chemical Biology, Leiden University Medical Centre, Leiden, The Netherlands.
PLoS Pathog. 2025 Apr 18;21(4):e1013032. doi: 10.1371/journal.ppat.1013032. eCollection 2025 Apr.
The ubiquitin-proteasome system (UPS) is essential for Plasmodium falciparum survival and represents a potential target for antimalarial therapies. We utilised a ubiquitin- activity based probe (Ub-Dha) to capture active components of the ubiquitin conjugating machinery during asexual blood-stage development. Several E2 ubiquitin-conjugating enzymes, the E1 activating enzyme, and the HECT E3 ligase PfHEUL were identified and validated through in vitro ubiquitination assays. We also demonstrate selective functional interactions between PfHEUL and a subset of both human and P. falciparum E2s. Additionally, the Ub-Dha probe captured an uncharacterized protein, PF3D7_0811400 (C0H4U0) with no known homology to ubiquitin-pathway enzymes in other organisms. Through structural and biochemical analysis, we validate it as a novel E2 enzyme, capable of binding ubiquitin in a cysteine-specific manner. These findings contribute to our understanding of the P. falciparum UPS, identifying promising novel drug targets and highlighting the evolutionary uniqueness of the Ub-proteasome system in this parasite.
泛素-蛋白酶体系统(UPS)对恶性疟原虫的生存至关重要,是抗疟治疗的一个潜在靶点。我们利用一种基于泛素活性的探针(Ub-Dha)来捕获无性血液阶段发育过程中泛素结合机制的活性成分。通过体外泛素化试验鉴定并验证了几种E2泛素结合酶、E1激活酶和HECT E3连接酶PfHEUL。我们还证明了PfHEUL与人类和恶性疟原虫E2的一个子集之间存在选择性功能相互作用。此外,Ub-Dha探针捕获了一种未鉴定的蛋白质PF3D7_0811400(C0H4U0),它与其他生物体中的泛素途径酶没有已知的同源性。通过结构和生化分析,我们将其验证为一种新型E2酶,能够以半胱氨酸特异性方式结合泛素。这些发现有助于我们理解恶性疟原虫的UPS,确定有前景的新型药物靶点,并突出该寄生虫中泛素-蛋白酶体系统的进化独特性。