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. 2019 Dec 23;9:19654. doi: 10.1038/s41598-019-56177-5

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© The Author(s) 2019

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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The disordered region of the targeted protein is required for efficient degradation by PROTACs. (A) HEK293T cells were treated with TD-165 (1 μM), the p97/VCP inhibitor DBeQ (10 μM), or both for 6 h. Whole-cell lysates were analyzed by immunoblotting for the indicated proteins. (B) N-terminal CRBN (a.a. 1–80) was inserted into the N- or C-terminus of His-SBP–tagged VHL plasmid, and plasmids were expressed in HEK293T cells. After 8 h, the cells were harvested and divided into four groups. Each group was then treated with increasing concentrations of TD-165 for 48 h. Whole-cell lysates were analyzed by immunoblotting for the indicated proteins. (C) Plasmids expressing the N-terminus of CRBN (a.a. 1–80) fused to D2, D3, or D4 were transfected into HEK293T cells. After 8 h, the cells were harvested and divided into four groups. Each group was then treated with increasing concentrations of TD-165 for 48 h. Whole-cell lysates were analyzed by immunoblotting for the indicated proteins. (D) Plasmids expressing full-length AR, N-terminally deleted AR (ΔN330), or the N-terminus of CRBN (a.a. 1–80) fused to ΔN330 (CRBN (a.a. 1–80) +ΔN330) were transfected into HEK293T cells. After 8 h, the cells were harvested and divided into four groups. Each group was then treated with increasing concentrations of ARCC4 for 24 h. Whole-cell lysates were analyzed by immunoblotting for the indicated proteins. (E) Plasmids expressing full-length CRBN, D1 deletion mutant, or N-terminus of AR (a.a. 1–170) fused to D1 (AR (1–170) +D1) were transfected into HEK293T cells. After 8 h, the cells were harvested and divided into four groups. Each group was then treated with increasing concentrations of TD-165 for 48 h. Whole-cell lysates were analyzed by immunoblotting for the indicated proteins.