Results 151 to 160 of about 753,077 (248)

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

open access: yesAdvanced 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   +8 more
wiley   +1 more source

Discovery of Highly Selective Noncovalent Macrocyclic Peptide Inhibitors Suppressing Both TMPRSS2 Protease Activity and Viral Receptor Function. [PDF]

open access: yesJ Med Chem
Tombling BJ   +14 more
europepmc   +1 more source

Topological Quantum Biomaterials Enable Pyroptosis‐Senescence Coupling for Enhanced Colorectal Cancer Therapy

open access: yesAdvanced Science, EarlyView.
This work reports conceptually unprecedented topological quantum biomaterials derived from engineered Pd3Sn nanostrips for oncological applications. Their near‐Fermi‐level electronic architecture and superior interfacial charge transport facilitate ultrasound‐amplified redox reactions and efficient ROS generation.
Zilu Chen   +10 more
wiley   +1 more source

Beyond Nature's Blueprint: Macrocyclic Peptides Containing Unnatural Amino Acids in Therapeutic Development

open access: yesAngewandte Chemie, EarlyView.
Strategic incorporation of unnatural amino acids transforms macrocyclic peptides into drug‐like molecules capable of engaging challenging targets. These building blocks enhance stability, permeability, and bioavailability, accelerating the development of next‐generation peptide therapeutics.
Krishna K. Sharma   +5 more
wiley   +2 more sources

Proteinase inhibitor candidates for therapy of enzyme-inhibitor imbalances [PDF]

open access: yes, 1992
Collins, John   +6 more
core   +1 more source

Galactokinase 1 Positively Regulates Mitochondrial Respiration by Phosphorylating TIMM13 as a Protein Kinase

open access: yesAdvanced Science, EarlyView.
GALK1 acts as a protein kinase beyond the phosphorylation of galactose. GALK1 phosphorylates TIMM13 at Y73 in the cytoplasm. This phosphorylation prevents premature oxidative folding of TIMM13 and ensures its entrance into the intermembrane space of mitochondrion, positively regulating mitochondrial respiration.
Chang Woo Ko   +5 more
wiley   +1 more source

Cysteine Thioaldehydes: Photolytic Generation, Reactivity, and Biological Implications

open access: yesAngewandte Chemie, EarlyView.
Photolysis of cysteine phenacylsulfides bearing non‐conjugating electron‐withdrawing substituents leads to high conversions into cysteine thioaldehydes through a Norrish type‐II pathway. This methodology enabled the study of the aqueous reactivity of these important biosynthetic intermediates, which, depending on peptide sequence, pH and buffer ...
Ardra Karthika   +9 more
wiley   +2 more sources

Huntingtin Aggregate‐Responsive Autophagy Gene Circuit Mitigates Disease Pathology in R6/2 Mice

open access: yesAdvanced Science, EarlyView.
CD98‐mediated receptor‐mediated transcytosis enables LIP‐CD98 nanocarriers to cross the blood–brain barrier and deliver ARAA to neurons. mHTT aggregates activate the 11G–NarX sensor, initiating Auto‐P and Trans‐P signaling through the VP48–NarL relay.
Jie Zhu   +8 more
wiley   +1 more source

Structure and Function of a Multi‐Megadalton Virus‐Like Proteolytic Dodecahedron

open access: yesAngewandte Chemie, EarlyView.
Zuzalysin, a virulence metallopeptidase of the periodontal pathogen Porphyromonas gingivalis, is secreted as a latent, flexible ≈95‐kDa monomer. Calcium triggers cysteine‐switch activation and hierarchical assembly into pentamers, bipentamers, tripentamers, and a ≈5.6‐MDa, ≈355‐Å dodecahedron. Structures at 1.8–3.6 Å reveal a virus‐sized catalytic cage
Mariusz Madej   +20 more
wiley   +2 more sources

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