Structure of parkin reveals mechanisms for ubiquitin ligase activation

JF Trempe, V Sauvé, K Grenier, M Seirafi, MY Tang… - Science, 2013 - science.org
JF Trempe, V Sauvé, K Grenier, M Seirafi, MY Tang, M Ménade, S Al-Abdul-Wahid, J Krett…
Science, 2013science.org
Mutations in the PARK2 (parkin) gene are responsible for an autosomal recessive form of
Parkinson's disease. The parkin protein is a RING-in-between-RING E3 ubiquitin ligase that
exhibits low basal activity. We describe the crystal structure of full-length rat parkin. The
structure shows parkin in an autoinhibited state and provides insight into how it is activated.
RING0 occludes the ubiquitin acceptor site Cys431 in RING2, whereas a repressor element
of parkin binds RING1 and blocks its E2-binding site. Mutations that disrupted these …
Mutations in the PARK2 (parkin) gene are responsible for an autosomal recessive form of Parkinson’s disease. The parkin protein is a RING-in-between-RING E3 ubiquitin ligase that exhibits low basal activity. We describe the crystal structure of full-length rat parkin. The structure shows parkin in an autoinhibited state and provides insight into how it is activated. RING0 occludes the ubiquitin acceptor site Cys431 in RING2, whereas a repressor element of parkin binds RING1 and blocks its E2-binding site. Mutations that disrupted these inhibitory interactions activated parkin both in vitro and in cells. Parkin is neuroprotective, and these findings may provide a structural and mechanistic framework for enhancing parkin activity.
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