A fibroblast activation protein (FAP)‐targeted small molecule–drug conjugate (SMDC) platform is developed to integrate PET imaging with synergistic radionuclide–chemotherapy. Linker chemistry governs stability, exposure, and tolerability, with the VC linker providing superior in vivo performance.
Ruitao Yang +6 more
wiley +1 more source
Tuning the hydrophobicity of glycine ester through <i>N</i>-acylation and introducing quaternary pyridinium groups enable the selectivity against Gram-positive bacteria. [PDF]
Pious A +7 more
europepmc +1 more source
Covalent Reprogramming of Kinase Binders to Modulate Protein Abundance
Electrophilic remodeling of a broad‐spectrum kinase binder reveals how subtle chemical changes reprogram protein fate. An acrylamide analog of a multi‐kinase binder selectively stabilizes Aurora kinase A (AURKA) by suppressing its ubiquitination, while a short‐linker variant converts this stabilizer into a degrader.
Chen Mozes +4 more
wiley +1 more source
Glycine Composition and Ion Valency Tune Phase Behavior and Drug Encapsulation in Designer Peptide Condensates. [PDF]
Veretnik S, Harris R, Lampel A.
europepmc +1 more source
This study identifies a FOSL2‐driven positive feedback loop that amplifies FSH/FSHR signaling. During FSH‐dependent follicle maturation, FSH induces Fosl2 expression via the cAMP‐PKA‐CREB cascade. FOSL2 in turn binds the promoters of Fshr and estrogen‐biosynthesis genes to enhance their transcription, thereby increasing Fshr mRNA level and amplifying ...
Hongru Shi +13 more
wiley +1 more source
Computational Repurposing and Experimental Validation of YBX1 Inhibitors in Hepatocellular Carcinoma. [PDF]
Karkoutly O +3 more
europepmc +1 more source
The Polymers of Life: Exploring Cellular Function Through Polymer Concepts
Biomolecular phase separation reveals that a hidden layer of cellular organization is governed by the principles of polymer science. This review bridges polymer physics and cell biology, offering a primer on fundamental concepts, proposing a framework for interrogating cellular function, and synthesizing biophysical methods for decoding macromolecular ...
Mark Chen, Ashutosh Chilkoti
wiley +1 more source
Multiple formation pathways for amino acids in the early Solar System based on carbon and nitrogen isotopes in asteroid Bennu samples. [PDF]
Baczynski AA +11 more
europepmc +1 more source
This study reveals a citrate–ACLY–H3K27ac metabolic–epigenetic axis driving inflammatory gene activation and kidney fibrosis, highlighting ACLY inhibition as a potential therapeutic strategy for chronic kidney disease (CKD). ABSTRACT The mechanisms by which metabolic stress drives epigenetic dysregulation and fibrosis in chronic kidney disease (CKD ...
Chunxiu Du +15 more
wiley +1 more source
UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors. [PDF]
Benton AJ +10 more
europepmc +1 more source

