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1995 1
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216 results

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Page 1
DCAF1 regulates Treg senescence via the ROS axis during immunological aging.
Guo Z, Wang G, Wu B, Chou WC, Cheng L, Zhou C, Lou J, Wu D, Su L, Zheng J, Ting JP, Wan YY. Guo Z, et al. J Clin Invest. 2020 Nov 2;130(11):5893-5908. doi: 10.1172/JCI136466. J Clin Invest. 2020. PMID: 32730228 Free PMC article.
Furthermore, we revealed that DDB1- and CUL4-associated factor 1 (DCAF1) was downregulated in aged Tregs and was critical to restrain Treg aging via reactive oxygen species (ROS) regulated by glutathione-S-transferase P (GSTP1). ...Therefore, our studies uncover an importa …
Furthermore, we revealed that DDB1- and CUL4-associated factor 1 (DCAF1) was downregulated in aged Tregs and was critical to restrain …
DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance.
Schröder M, Renatus M, Liang X, Meili F, Zoller T, Ferrand S, Gauter F, Li X, Sigoillot F, Gleim S, Stachyra TM, Thomas JR, Begue D, Khoshouei M, Lefeuvre P, Andraos-Rey R, Chung B, Ma R, Pinch B, Hofmann A, Schirle M, Schmiedeberg N, Imbach P, Gorses D, Calkins K, Bauer-Probst B, Maschlej M, Niederst M, Maher R, Henault M, Alford J, Ahrne E, Tordella L, Hollingworth G, Thomä NH, Vulpetti A, Radimerski T, Holzer P, Carbonneau S, Thoma CR. Schröder M, et al. Nat Commun. 2024 Jan 4;15(1):275. doi: 10.1038/s41467-023-44237-4. Nat Commun. 2024. PMID: 38177131 Free PMC article.
Here we show that the essential E3 ligase receptor DCAF1 can be harnessed for TPD utilizing a selective, non-covalent DCAF1 binder. We confirm that this binder can be functionalized into an efficient DCAF1-BRD9 PROTAC. Chemical and genetic rescue experiments …
Here we show that the essential E3 ligase receptor DCAF1 can be harnessed for TPD utilizing a selective, non-covalent DCAF1 bi …
DCAF1 interacts with PARD3 to promote hepatocellular carcinoma progression and metastasis by activating the Akt signaling pathway.
Zhang J, Shi Y, Ding K, Yu W, He J, Sun B. Zhang J, et al. J Exp Clin Cancer Res. 2024 May 6;43(1):136. doi: 10.1186/s13046-024-03055-2. J Exp Clin Cancer Res. 2024. PMID: 38711082 Free PMC article.
However, the function of DCAF1 in HCC development and the underlying mechanism are still unknown. This study aimed to explore the effect of DCAF1 in HCC and the corresponding molecular mechanism. ...CONCLUSIONS: Our study illustrates that DCAF1 plays a crucia …
However, the function of DCAF1 in HCC development and the underlying mechanism are still unknown. This study aimed to explore the eff …
DCAF1 inhibits the NF-kappaB pathway by targeting p65.
Huang F, Yao W, Sun B, Fujinaga K. Huang F, et al. Immunol Lett. 2022 Sep;249:33-42. doi: 10.1016/j.imlet.2022.08.005. Epub 2022 Aug 31. Immunol Lett. 2022. PMID: 36055411
Here, we revealed that activation of NF-kappaB by virion-associated Vpr proteins highly depends on DCAF1, and that exogenous DCAF1 is capable of restraining NF-kappaB induction by external stimuli. Depletion of DCAF1 augments NF-kappaB activation. DCAF1 …
Here, we revealed that activation of NF-kappaB by virion-associated Vpr proteins highly depends on DCAF1, and that exogenous DCAF1 …
Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity.
Mabanglo MF, Wilson B, Noureldin M, Kimani SW, Mamai A, Krausser C, González-Álvarez H, Srivastava S, Mohammed M, Hoffer L, Chan M, Avrumutsoae J, Li ASM, Hajian T, Tucker S, Green S, Szewczyk M, Barsyte-Lovejoy D, Santhakumar V, Ackloo S, Loppnau P, Li Y, Seitova A, Kiyota T, Wang JG, Privé GG, Kuntz DA, Patel B, Rathod V, Vala A, Rout B, Aman A, Poda G, Uehling D, Ramnauth J, Halabelian L, Marcellus R, Al-Awar R, Vedadi M. Mabanglo MF, et al. Nat Commun. 2024 Nov 23;15(1):10165. doi: 10.1038/s41467-024-54500-x. Nat Commun. 2024. PMID: 39580491 Free PMC article.
We recently developed potent ligands for DCAF1, a substrate receptor of EDVP and CUL4 E3 ligases. Here, we focus on DCAF1 toward the development of PROTACs for WDR5, a drug target in various cancers. We report four DCAF1-based PROTACs with endogenous and exog …
We recently developed potent ligands for DCAF1, a substrate receptor of EDVP and CUL4 E3 ligases. Here, we focus on DCAF1 towa …
CRL4-DCAF1 Ubiquitin Ligase Dependent Functions of HIV Viral Protein R and Viral Protein X.
Dobransky A, Root M, Hafner N, Marcum M, Sharifi HJ. Dobransky A, et al. Viruses. 2024 Aug 17;16(8):1313. doi: 10.3390/v16081313. Viruses. 2024. PMID: 39205287 Free PMC article. Review.
HIV Viral Protein R (Vpr) and the related HIV-2 Viral Protein X (Vpx), engage the CRL4-DCAF1 ubiquitin ligase complex to target numerous cellular proteins. In this review we describe the CRL4-DCAF1 ubiquitin ligase complex and its interactions with HIV Vpr and Vpx. …
HIV Viral Protein R (Vpr) and the related HIV-2 Viral Protein X (Vpx), engage the CRL4-DCAF1 ubiquitin ligase complex to target numer …
Glucose deprivation triggers DCAF1-mediated inactivation of Rheb-mTORC1 and promotes cancer cell survival.
Li M, Huang W, Zhang Y, Du Y, Zhao S, Wang L, Sun Y, Sha B, Yan J, Ma Y, Tang J, Shi J, Li P, Jia L, Hu T, Chen P. Li M, et al. Cell Death Dis. 2024 Jun 11;15(6):409. doi: 10.1038/s41419-024-06808-1. Cell Death Dis. 2024. PMID: 38862475 Free PMC article.
In this study, we demonstrate that glucose deprivation, while not amino acid or serum starvation, transactivates the expression of DCAF1. This enhances the K48-linked polyubiquitination and proteasome-dependent degradation of Rheb, inhibits mTORC1 activity, induces autopha …
In this study, we demonstrate that glucose deprivation, while not amino acid or serum starvation, transactivates the expression of DCAF1 …
DOT1L/H3K79me2 represses HIV-1 reactivation via recruiting DCAF1.
Liang F, Jin J, Li Q, Duan J, Jiang A, Chen X, Geng H, Wu K, Yu F, Zhao X, Zhou Y, Hu D, Chen L. Liang F, et al. Cell Rep. 2024 Jul 23;43(7):114368. doi: 10.1016/j.celrep.2024.114368. Epub 2024 Jun 20. Cell Rep. 2024. PMID: 38905100 Free article.
Following peptide affinity purification and proteomic analysis, we identified that DCAF1-a component of the E3 ligase complex involved in HIV regulation-is associated with H3K79me2 and DOT1L. ...Mechanistically, upon TNF-alpha/NF-kappaB activation, DCAF1 is recruite …
Following peptide affinity purification and proteomic analysis, we identified that DCAF1-a component of the E3 ligase complex involve …
Discovery of Nanomolar DCAF1 Small Molecule Ligands.
Li ASM, Kimani S, Wilson B, Noureldin M, González-Álvarez H, Mamai A, Hoffer L, Guilinger JP, Zhang Y, von Rechenberg M, Disch JS, Mulhern CJ, Slakman BL, Cuozzo JW, Dong A, Poda G, Mohammed M, Saraon P, Mittal M, Modh P, Rathod V, Patel B, Ackloo S, Santhakumar V, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Marcellus R, Guié MA, Keefe AD, Brown PJ, Halabelian L, Al-Awar R, Vedadi M. Li ASM, et al. J Med Chem. 2023 Apr 13;66(7):5041-5060. doi: 10.1021/acs.jmedchem.2c02132. Epub 2023 Mar 22. J Med Chem. 2023. PMID: 36948210 Free PMC article.
DCAF1 is a substrate receptor of two distinct E3 ligases (CRL4(DCAF1) and EDVP), plays a critical physiological role in protein degradation, and is considered a drug target for various cancers. ...OICR-8268 is an excellent tool compound to enable the development of …
DCAF1 is a substrate receptor of two distinct E3 ligases (CRL4(DCAF1) and EDVP), plays a critical physiological role in protei …
CRL4(DCAF1/VprBP) E3 ubiquitin ligase controls ribosome biogenesis, cell proliferation, and development.
Han XR, Sasaki N, Jackson SC, Wang P, Li Z, Smith MD, Xie L, Chen X, Zhang Y, Marzluff WF, Xiong Y. Han XR, et al. Sci Adv. 2020 Dec 18;6(51):eabd6078. doi: 10.1126/sciadv.abd6078. Print 2020 Dec. Sci Adv. 2020. PMID: 33355139 Free PMC article.
Inducible DCAF1 loss eliminates proliferating, but not quiescent, T cells and MEFs. We identify the ribosome assembly factor PWP1 as a substrate of the CRL4(DCAF1) ligase. ...Cumulatively, these results reveal a critical function for DCAF1 in ribosome biogene …
Inducible DCAF1 loss eliminates proliferating, but not quiescent, T cells and MEFs. We identify the ribosome assembly factor PWP1 as …
216 results