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Figure 1.

XIAP, cIAP1 and cIAP2 bind RIP1-4 proteins.

(A) In vitro-transcribed and -translated RIP1, 2, 3 and 4 labeled with 35S-methionine (Input) was incubated overnight with bacterially produced GST, GST-XIAP, GST-cIAP1, or GST-cIAP2 bound to Sepharose beads. The beads were washed extensively and run on an acrylamide gel. Binding of RIPs was revealed by autoradiography (pull-down). (B) In vitro-transcribed and -translated RIP1, 2, 3 and 4 labeled with 35S-methionine (Input) was incubated overnight with bacterially produced GST-XIAP, GST-cIAP1, or GST-cIAP2 bound to Sepharose beads in presence of BV6 (5 µM) or DMSO as a control. The beads were washed extensively and run on an acrylamide gel. Binding of RIPs was revealed by autoradiography. (C) HEK293T cells were transfected with VSV-tagged RIP plasmids in the absence or presence of a FLAG-tagged cIAP1 plasmid. cIAP1 was immunoprecipitated in NP-40 buffer using anti-FLAG antibody and coimmunoprecipitated RIPs were revealed by immunoblotting with anti-VSV antibody. Protein expression in the lysates is shown. (D) HEK293T cells were transfected with VSV-tagged RIP plasmids in the absence or presence of a Myc-tagged cIAP2 plasmid. cIAP2 was immunoprecipitated in NP-40 buffer using anti-Myc antibody and coimmunoprecipitated RIPs were revealed by immunoblotting with anti-VSV antibody. Protein expression in the lysates is shown.

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Figure 1 Expand

Figure 2.

cIAP1 and cIAP2 are direct E3 ubiquitin ligases for RIP1–4 proteins.

(A) In vitro ubiquitination assays were performed on in vitro-transcribed and -translated RIP1–4 proteins labeled with 35S-methionine. GST, GST-XIAP, GST-cIAP1, or GST-cIAP2 was used as E3 component, UbcH5a as the E2 component, and using wild-type ubiquitin. RIP ubiquitination was revealed by autoradiography and appears as a smear in the figure. (B) HEK293T cells were transfected with VSV-tagged RIP3 and RIP4 plasmids in the absence or presence of a Myc-tagged cIAP2 plasmid. cIAP2 was immunoprecipitated in NP-40 buffer using anti-Myc antibody and coimmunoprecipitated ubiquitinated RIP3 and RIP4 were revealed by immunoblotting with anti-VSV and anti-ubiquitin antibodies. Protein expression in the lysates is shown. (C) HEK293T cells were transfected with VSV-tagged RIP3 plasmid in the absence or presence of a cIAP2 plasmid. RIP3 was immunoprecipitated in RIPA buffer using anti-VSV antibody and ubiquitinated RIP3 was revealed by immunoblotting with anti-VSV and anti-ubiquitin antibodies. Protein expression in the lysates is shown.

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Figure 2 Expand

Figure 3.

cIAP1 conjugates RIP1–4 proteins with Lys48-, Lys63-, and linear ubiquitin chains.

(A) Schematic representation of the different ubiquitin mutants used in the experiments. (B–D) In vitro ubiquitination assays were performed on in vitro-transcribed and -translated RIP1–4 proteins labeled with 35S-methionine. GST or GST-cIAP1 was used as E3 component and UbcH5a as the E2 component. The reaction was carried out in presence of (B) wild-type (WT) ubiquitin, K48-only ubiquitin and K63-only ubiquitin; (C) no ubiquitin, wild-type (WT) ubiquitin and lysine free ubiquitin (KO); (D) no ubiquitin, wild-type (WT) ubiquitin and Myc-tagged ubiquitin. Ubiquitination of the RIPs was revealed by autoradiography.

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Figure 3 Expand

Figure 4.

Requirement of cIAP1/2 for RIP1–4-mediated NF-κB activation.

(A) NF-κB luciferase assays were performed on lysates from HEK293T cells transfected with a plasmid encoding the indicated RIP kinase or TAK1. Cells were left untreated or were treated with 1 µM of BV6. Stimulation with hTNF was used as a positive control. (B) Western blot showing expression of the tagged-RIP kinases, cIAP1 and TAK1 in the lysates. (C) Phosphorylation of RIP4 was revealed by λ-phosphatase treatment of immunopurified Flag-RIP4 overexpressed in HEK293T cells. Samples were analyzed by western blot using anti-Flag antibody.

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Figure 5.

Lysine residues K51 and K145 of RIP4 are critical for cIAP1-mediated ubiquitination and NF-κB activation.

(A) Flag-tagged wild type RIP4, K51R, K145R, K158R and K220/221R mutants were ectopically expressed in HEK293T cells together with a NF-κB luciferase reporter. 24h after transfection, lysates were prepared and tested for luciferase activity. Relative luciferase activity is depicted after correction for transfection efficiency, ± S.D. (B) Lysates described in (B) were used for western blotting analysis with an anti-Flag antibody in order to detect expression of the different Flag-tagged RIP4 variants. (C) HEK293T cells were transfected with FLAG-tagged wild-type RIP4, the K51R mutant or with empty vector. The medium was replaced 8h post-transfection with medium containing, or not, BV6 (1 µM). The RIP4 proteins were immunoprecipitated 18h later in RIPA buffer using anti-FLAG antibody and ubiquitinated RIP4 proteins were revealed by immunoblotting with anti-FLAG and anti-ubiquitin antibodies. (D) In vitro ubiquitination assays were performed on in vitro-transcribed and -translated wild-type RIP4, K51R, K145R, K158R and K220/221R mutants labeled with 35S-methionine. GST or GST-cIAP1 was used as E3 component and UbcH5a as E2 component. The reaction was carried out in presence of wild-type ubiquitin. RIP4 ubiquitination was revealed by autoradiography.

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