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Page 1
Showing results for ann degrade
Your search for Ann Degrande retrieved no results
Ferroptosis: machinery and regulation.
Chen X, Li J, Kang R, Klionsky DJ, Tang D. Chen X, et al. Autophagy. 2021 Sep;17(9):2054-2081. doi: 10.1080/15548627.2020.1810918. Epub 2020 Aug 26. Autophagy. 2021. PMID: 32804006 Free PMC article. Review.
Many metabolic (especially involving iron, lipids, and amino acids) and degradation pathways (macroautophagy/autophagy and the ubiquitin-proteasome system) orchestrate the complex ferroptotic response through direct or indirect regulation of iron accumulation or lipid pero …
Many metabolic (especially involving iron, lipids, and amino acids) and degradation pathways (macroautophagy/autophagy and the ubiqui …
Quality Control in the Endoplasmic Reticulum: Crosstalk between ERAD and UPR pathways.
Hwang J, Qi L. Hwang J, et al. Trends Biochem Sci. 2018 Aug;43(8):593-605. doi: 10.1016/j.tibs.2018.06.005. Epub 2018 Jun 29. Trends Biochem Sci. 2018. PMID: 30056836 Free PMC article. Review.
Endoplasmic reticulum (ER)-associated degradation (ERAD) and the unfolded protein response (UPR) are two key quality-control machineries in the cell. ERAD is responsible for the clearance of misfolded proteins in the ER for cytosolic proteasomal degradation, while U …
Endoplasmic reticulum (ER)-associated degradation (ERAD) and the unfolded protein response (UPR) are two key quality-control machiner …
A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo.
Bai L, Zhou H, Xu R, Zhao Y, Chinnaswamy K, McEachern D, Chen J, Yang CY, Liu Z, Wang M, Liu L, Jiang H, Wen B, Kumar P, Meagher JL, Sun D, Stuckey JA, Wang S. Bai L, et al. Cancer Cell. 2019 Nov 11;36(5):498-511.e17. doi: 10.1016/j.ccell.2019.10.002. Cancer Cell. 2019. PMID: 31715132 Free PMC article.
Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. Here we report the discovery of SD-36, a small-molecule degrader of STAT3. SD-36 potently induces the degradation of STAT3 protein in vitro and in vivo and demonst …
Signal transducer and activator of transcription 3 (STAT3) is an attractive cancer therapeutic target. Here we report the discovery of SD-36 …
PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy.
Kelm JM, Pandey DS, Malin E, Kansou H, Arora S, Kumar R, Gavande NS. Kelm JM, et al. Mol Cancer. 2023 Mar 30;22(1):62. doi: 10.1186/s12943-022-01707-5. Mol Cancer. 2023. PMID: 36991452 Free PMC article. Review.
Degraders offer several advantages for cancer therapy including resiliency to acquired mutations in the target protein, enhanced selectivity, lower dosing requirements, and the potential to abrogate oncogenic transcription factors and scaffolding proteins. ...The medicinal
Degraders offer several advantages for cancer therapy including resiliency to acquired mutations in the target protein, enhanced sele
Introduction.
Sun Y. Sun Y. Adv Exp Med Biol. 2020;1217:1-8. doi: 10.1007/978-981-15-1025-0_1. Adv Exp Med Biol. 2020. PMID: 31898218
Neddylation, like ubiquitylation, is also catalyzed by an E1/E2/E3 enzyme cascade to covalently attach the ubiquitin-like molecule NEDD8 to a lysine residue of a substrate, not for degradation, but for modulation of substrate activity. The best known neddylation substrates …
Neddylation, like ubiquitylation, is also catalyzed by an E1/E2/E3 enzyme cascade to covalently attach the ubiquitin-like molecule NEDD8 to …
SIRT5-mediated lysine desuccinylation impacts diverse metabolic pathways.
Park J, Chen Y, Tishkoff DX, Peng C, Tan M, Dai L, Xie Z, Zhang Y, Zwaans BM, Skinner ME, Lombard DB, Zhao Y. Park J, et al. Mol Cell. 2013 Jun 27;50(6):919-30. doi: 10.1016/j.molcel.2013.06.001. Mol Cell. 2013. PMID: 23806337 Free PMC article.
Our analysis reveals potential impacts of lysine succinylation on enzymes involved in mitochondrial metabolism; e.g., amino acid degradation, the tricarboxylic acid cycle (TCA) cycle, and fatty acid metabolism. ...Our data reveal widespread roles for lysine s …
Our analysis reveals potential impacts of lysine succinylation on enzymes involved in mitochondrial metabolism; e.g., amino acid d
SEL1L-HRD1 endoplasmic reticulum-associated degradation controls STING-mediated innate immunity by limiting the size of the activable STING pool.
Ji Y, Luo Y, Wu Y, Sun Y, Zhao L, Xue Z, Sun M, Wei X, He Z, Wu SA, Lin LL, Lu Y, Chang L, Chen F, Chen S, Qian W, Xu X, Chen S, Pan D, Zhou Z, Xia S, Hu CA, Liang T, Qi L. Ji Y, et al. Nat Cell Biol. 2023 May;25(5):726-739. doi: 10.1038/s41556-023-01138-4. Epub 2023 May 4. Nat Cell Biol. 2023. PMID: 37142791 Free PMC article.
Here we report that the SEL1L-HRD1 protein complex-the most conserved branch of ER-associated degradation (ERAD)-is a negative regulator of the STING innate immunity by ubiquitinating and targeting nascent STING protein for proteasomal degradation in the basal state …
Here we report that the SEL1L-HRD1 protein complex-the most conserved branch of ER-associated degradation (ERAD)-is a negative regula …
Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
Xiang W, Zhao L, Han X, Qin C, Miao B, McEachern D, Wang Y, Metwally H, Kirchhoff PD, Wang L, Matvekas A, He M, Wen B, Sun D, Wang S. Xiang W, et al. J Med Chem. 2021 Sep 23;64(18):13487-13509. doi: 10.1021/acs.jmedchem.1c00900. Epub 2021 Sep 2. J Med Chem. 2021. PMID: 34473519 Free PMC article.
We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC(50) values of 0.1 nM in the VCaP cell line with AR gene amplification and in the LNCaP cell line carryin …
We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR degraders with ARD-2585 being the most promi …
Loss of Optineurin Drives Cancer Immune Evasion via Palmitoylation-Dependent IFNGR1 Lysosomal Sorting and Degradation.
Du W, Hua F, Li X, Zhang J, Li S, Wang W, Zhou J, Wang W, Liao P, Yan Y, Li G, Wei S, Grove S, Vatan L, Zgodziński W, Majewski M, Wallner G, Chen H, Kryczek I, Fang JY, Zou W. Du W, et al. Cancer Discov. 2021 Jul;11(7):1826-1843. doi: 10.1158/2159-8290.CD-20-1571. Epub 2021 Feb 24. Cancer Discov. 2021. PMID: 33627378 Free PMC article.
Mechanistically, we observed that IFNGR1 was S-palmitoylated on Cys122, and AP3D1 bound with and sorted palmitoylated IFNGR1 to lysosome for degradation. Unexpectedly, optineurin interacted with AP3D1 to prevent palmitoylated IFNGR1 lysosomal sorting and degradation
Mechanistically, we observed that IFNGR1 was S-palmitoylated on Cys122, and AP3D1 bound with and sorted palmitoylated IFNGR1 to lysosome for …
The application of PROTAC in HDAC.
Chen S, Zheng Y, Liang B, Yin Y, Yao J, Wang Q, Liu Y, Neamati N. Chen S, et al. Eur J Med Chem. 2023 Nov 15;260:115746. doi: 10.1016/j.ejmech.2023.115746. Epub 2023 Aug 19. Eur J Med Chem. 2023. PMID: 37607440 Review.
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great opportunities for scientific research and industrial applications. Histone deacetylase (HDAC)-PROTAC has been widely developed since the first report of its ability to induce the d
Inducing protein degradation by proteolysis targeting chimera (PROTAC) has provided great opportunities for scientific research and i …
153,515 results
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