Fig. 1: Activation of parkin by the tetrahydropyrazolo-pyrazine (THPP) BIO-2007817 in the presence of pUb. | Nature Communications

Fig. 1: Activation of parkin by the tetrahydropyrazolo-pyrazine (THPP) BIO-2007817 in the presence of pUb.

From: Activation of parkin by a molecular glue

Fig. 1

a Domain structure of parkin. b Autoubiquitination assays show full-length parkin and the Ubl-ACT deletion (R0RBR) are activated by BIO-2007817 and phosphorylated ubiquitin (pUb). pUb without a C-terminal glycine (pUb∆G76) was used to prevent its incorporation by E1. No effect was observed on activated, phosphorylated human parkin (n = 1 assay). c Effect of mutations in the pUb-binding sites on RING1 (H302A A320R) and RING0 (K211N) on the parkin activation by BIO-2007817 (n = 1 assay). d Ubiquitin vinyl sulfone (Ub-VS) assay of parkin activation by BIO-2007817 in the presence of pUb. Formation of the parkin-Ub crosslink measures release of the Rcat ___domain from RING0 (n = 1 assay). e Chemical structures of BIO-2007817 and inactive diastereomer BIO-2007818.

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