Results 91 to 100 of about 504,547 (295)

Discovery of a KLHL41 Ligand for Muscle Specific Protein Degradation

Nature Communications
Despite the recent advancement of proteolysis-targeting chimera (PROTAC) development, they remain predominantly dependent on two E3 ligases, CRBN and VHL, which are ubiquitously expressed in all types of cells.
Junhyeong Yim, Jaeseok Lee, Solbi Kim, Jieun Choi, Soyoung Yoon, Hana Cho, Sunbin Jung, GaYeon Yoo, Sanghee Lee, Hankum Park, Juyong Lee, Jongmin Park   +11 more
doaj   +1 more source

Affinity selection mass spectrometry screening discovers new COP1 peptide binders [PDF]

RSC Chemical Biology
Targeting E3 ubiquitin ligases with chemical probes remains a major challenge, despite their central roles in cellular regulation and disease. Constitutive photomorphogenic 1 (COP1) is an E3 ligase whose complex, adaptor-dependent biology has made its ...
Harsha Negi, Noor Radhi, Nicolas Schiff, Sam A. Jamieson, Deanna Shea, Martin Middleditch, Robert Mullin, Renata Kowalczyk, Paul W. Harris, Peter D. Mace, Daniel Conole   +10 more
doaj   +1 more source

Development of Peptide Based E3 Ligase Reporter [PDF]

, 2017
This dissertation describes the development of a new analytical tool capable of analyzing E3 ligase activity, a critical element in the ubiquitin proteasome system.
Woss, Gregery
core   +1 more source

Epigenetic Silencing of CYYR1 Promotes Lung Adenocarcinoma Progression Through TRIM21‐Dependent Regulation of HMMR Stability

Advanced Science, EarlyView.
CYYR1 as an epigenetically dysregulated tumor‐suppressive factor that influences oncoprotein stability through TRIM21‐dependent HMMR regulation and reveals a potential therapeutic vulnerability in CYYR1‐deficient LUAD. The graphical illustration was created using FigDraw (www.figdraw.com).
Fengsheng Dai, Jingyi Tang, Huan Rong, Yu Wang, Xiangyi Zhou, Can Xu, Jianhua Wang, Lili Li, Yue Wu, Fei Deng, Dan Yang, Xiao Yang, Renyan Li, Yongzhong Wu, Dongxi Xiang, Tingxiu Xiang   +15 more
wiley   +1 more source

Principles of paralog-specific targeted protein degradation engaging the C-degron E3 KLHDC2

Nature Communications
PROTAC® (proteolysis-targeting chimera) molecules induce proximity between an E3 ligase and protein-of-interest (POI) to target the POI for ubiquitin-mediated degradation.
Daniel C. Scott, Suresh Dharuman, Elizabeth Griffith, Sergio C. Chai, Jarrid Ronnebaum, Moeko T. King, Rajendra Tangallapally, Chan Lee, Clifford T. Gee, Lei Yang, Yong Li, Victoria C. Loudon, Ha Won Lee, Jason Ochoada, Darcie J. Miller, Thilina Jayasinghe, Joao A. Paulo, Stephen J. Elledge, J. Wade Harper, Taosheng Chen, Richard E. Lee, Brenda A. Schulman   +21 more
doaj   +1 more source

A ligand discovery toolbox for the WWE domain family of human E3 ligases

Communications Biology
AbstractThe WWE domain is a relatively under-researched domain found in twelve human proteins and characterized by a conserved tryptophan-tryptophan-glutamate (WWE) sequence motif. Six of these WWE domain-containing proteins also contain domains with E3 ubiquitin ligase activity. The general recognition of poly-ADP-ribosylated substrates by WWE domains
Münzker, L, Kimani, SW, Fowkes, MM, Dong, A, Zheng, H, Li, Y, Dasovich, M, Zak, KM, Leung, AKL, Elkins, JM, Kessler, D, Arrowsmith, CH, Halabelian, L, Böttcher, J   +13 more
openaire   +5 more sources

TROP2‐Targeting Chimeras (TRTACs) for Tumor Cell‐Selective Membrane Protein Degradation and Enhanced Drug Delivery

Advanced Science, EarlyView.
TROP2 is identified as a novel tumor‐selective lysosomal‐targeting receptor with established clinical relevance. TROP2‐targeting chimeras (TRTACs) are developed by genetically fusing a TROP2‐binding nanobody to nanobodies against specific target proteins.
Luping Chen, Xinying Fu, Wenqian Dong, Xiaobei Deng, Simin Chen, Fujun Wang, Jian Zhao, Shiqun Shao, Liqiang Fan, Jingyu Zhang, Lixin Zhang   +10 more
wiley   +1 more source

Design and synthesis of inhibitors of the E3 ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 (SMURF1) as a treatment for lung remodeling in Pulmonary Arterial Hypertension (PAH)

, 2023
Design and synthesis of inhibitors of the E3 ligase SMAD Specific E3 Ubiquitin Protein Ligase 1 (SMURF1) as a treatment for lung remodeling in Pulmonary Arterial Hypertension (PAH) A series of selective SMURF1 ligase inhibitors have been identified ...
Sohal, Bindi, D'Souza, Anne-Marie, Smith, Nichola, Rynn, Caroline, Rowlands, David, Beerli, Rene, Guth-Gundel, Sabine, Cotesta, Simona, Lattmann, Rene, Williams, Gareth, Pulz, Robert, Shaw, Duncan, Troxler, Thomas J.   +12 more
core   +1 more source

Degrading GPX4 via Biomimetic Nanoparticle‐Mediated In Situ Synthesis of Deep‐Learning‐Designed Binder‐Degron Chimeras for Prostate Cancer Therapy

Advanced Science, EarlyView.
A deep‐learning‐designed binder is fused to a combinatorial degron to create a binder‐degron chimera (bdC) that recruits the CUL2‐RING ubiquitin ligase complex. Encapsulation in a prostate‐cancer‐targeted, CD47‐camouflaged nanocarrier enables tumor‐specific in situ bdC expression, triggering GPX4 degradation and ferroptosis, thereby establishing a ...
Si‐Han Zhang, Ye An, Na Zeng, Mei‐Cheng Liu, Jian‐Xuan Sun, Xi Gong, Jin‐Zhou Xu, Shao‐Gang Wang, Qi‐Dong Xia   +8 more
wiley   +1 more source

Discovering Uncharted Binding Pockets on E3 Ligases Leads to the Identification of FBW7 Allosteric Modulators

Advanced Science
E3 ligases are key regulators of the ubiquitin‐proteasome system (UPS) and have emerged as attractive drug target candidates for precise therapeutic intervention.
Míriam Martínez‐Cartró, Álvaro Serrano‐Morrás, Andrea Bertran‐Mostazo, Roger Castaño‐Muñiz, Salvatore Scaffidi, Varbina Ivanova, Noémi Csorba, József Simon, Péter Ábrányi‐Balogh, Yunfeng Li, György M. Keserü, Bing Hao, Xavier Barril, Carles Galdeano   +13 more
doaj   +1 more source