Results 141 to 150 of about 47,607 (250)

In-Cell Approach to Evaluate E3 Ligases for Use in Targeted Protein Degradation. [PDF]

open access: yesJ Am Chem Soc
Zheng Y   +13 more
europepmc   +1 more source

Regulation of inflammation and immunity in sepsis by E3 ligases. [PDF]

open access: yesFront Endocrinol (Lausanne), 2023
Shao S   +6 more
europepmc   +1 more source

Fibrillarin Resists Cellular Senescence Via SIRT1‐Dependent Nicotinamide Metabolism and Its Inhibition Sensitizes Senolytic Therapy in Esophageal Squamous Cell Carcinoma

open access: yesAdvanced Science, EarlyView.
FBL directly binds to and stabilizes SIRT1 by blocking its ubiquitin‐proteasome degradation, thereby sustaining nicotinamide metabolism and redox homeostasis to counteract cellular senescence in ESCC. Genetic and pharmacological suppression of FBL sensitizes tumor cells to senolytic therapy.
Xing Jin   +9 more
wiley   +1 more source

ATL2 Recruits TRAK1 to Promote Mitochondrial Transport at ER–Mitochondria Contact Sites

open access: yesAdvanced Science, EarlyView.
ABSTRACT Mitochondrial transport and distribution are crucial for cellular homeostasis, yet whether and how they are regulated by endoplasmic reticulum (ER)–mitochondria contact sites remains unclear. Here, we demonstrate that the ER protein atlastin‐2 (ATL2) orchestrates mitochondrial transport and distribution by promoting assembly of the transport ...
Yiru Cheng   +9 more
wiley   +1 more source

An alternative pocket for binding the N-degrons by the UBR1 and UBR2 ubiquitin E3 ligases. [PDF]

open access: yesProtein Sci
Huang ST   +8 more
europepmc   +1 more source

TRIM28‐Derived Peptide Exerts Anti‐Tumor Roles by Stabilizing Tumor Suppressive BRD7 Protein in Multiple Cancers

open access: yesAdvanced Science, EarlyView.
An α‐helical peptide, TAB12, designed to mimic the TRIM28 binding interface, competitively disrupts the TRIM28‐BRD7 interaction, thereby blocking ubiquitin‐mediated degradation of the tumor suppressor BRD7. This stabilization unleashes potent anti‐tumor effects across multiple tumor types with a favorable safety profile, offering a feasible strategy ...
Qingqing Wei   +10 more
wiley   +1 more source

Generalizable Strategies for the Synthesis of Cereblon‐Recruiting PROTAC Prodrugs

open access: yesAngewandte Chemie, EarlyView.
Cereblon‐recruiting PROTACs remain challenging to derivatize for prodrug‐based delivery. In this study, three complementary conjugation strategies enabled the efficient synthesis of cleavable PROTAC prodrugs with tunable release kinetics that can be incorporated into a library of PEGylated constructs and bottlebrush prodrugs.
Aiden X. Wang   +7 more
wiley   +2 more sources

Nanoparticle‐Mediated TIPE1 mRNA Delivery Enhances Paclitaxel Sensitivity in Triple‐Negative Breast Cancer by Modulating RAB7A Ubiquitination‐Associated Stability and Autophagy

open access: yesAdvanced Science, EarlyView.
TIPE1m NPs nanoparticles restore TIPE1 expression, promote RAB7A ubiquitination and degradation, suppress autophagic flux, and resensitize paclitaxel‐resistant triple‐negative breast cancer to therapy. ABSTRACT Acquired paclitaxel (PTX) resistance remains a major obstacle in triple‐negative breast cancer (TNBC) treatment.
Wei Hu   +9 more
wiley   +1 more source

Proteome‐Wide Target Identification Using Reactive Metallo‐Scaffolds (r‐mS): A Platform for Metallodrug Discovery

open access: yesAngewandte Chemie, EarlyView.
Re‐envisioning the Ligandable Proteome: Reactive Metallo‐Scaffolds (r‐mS) combine non‐covalent protein engagement by a metallo‐scaffold with covalent cysteine capture through a tethered chloroacetamide warhead. Chemoproteomic profiling reveals unique enzyme engagement including ligases, kinases and methyltransferases, highlighting opportunities for ...
Jessica E. Waters   +15 more
wiley   +2 more sources

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