Results 131 to 140 of about 11,335 (243)
Molecular Glue Degraders Redefining Targeted Therapies From Discovery to Therapeutic Applications
Molecular glue degraders (MGDs) constitute an emerging class of therapeutic agents poised to revolutionize the paradigm of targeted drug discovery. By reprogramming E3 ubiquitin ligases to degrade proteins of interest (POI) via a transient formation of a ternary complex mediated by protein–protein interactions, MGDs surpass the intrinsic limitations of
Jinfeng Wen +3 more
wiley +1 more source
PTGES3 proteolysis using the liposomal peptide-PROTAC approach
Background Hepatocellular carcinoma (HCC) is the leading cause of cancer-related deaths worldwide, and the lack of effective biomarkers for early detection leads to poor therapeutic outcomes.
Shiwei Liu +6 more
doaj +1 more source
Multifacet Roles of Cellular Senescence in Cancer: Mechanisms and Therapeutic Implications
Cellular senescence shapes tumor progression through both antitumor and protumor mechanisms. Senescence triggered by telomere shortening restricts malignant transformation and limits tumor cell proliferation, while the senescence‐associated secretory phenotype (SASP) secretion enhances antitumor immunity by activating cytotoxic T cells.
Huajie Mao +5 more
wiley +1 more source
Covalent Peptide‐Based N‐Myc/Aurora‐A Inhibitors Bearing Sulfonyl Fluoride Warheads
N‐Myc‐derived peptidomimetics bearing aryl sulfonyl fluoride warheads were shown to act as effective N‐Myc/Aurora‐A PPI inhibitors, selectively labelling Aurora‐A in a recognition‐directed manner. ABSTRACT Orthosteric inhibition of the N‐Myc/Aurora‐A protein–protein interaction (PPI) represents a potential mechanism by which degradation of N‐Myc can be
Robert S. Dawber +6 more
wiley +1 more source
KCTD15 is upregulated in TNBC tissues and cells. It enhances TNBC stemness via KLF4/β‐catenin signaling, promotes proliferation, migration, and stemness while inhibiting apoptosis, and drives tumorigenesis in vivo. Collectively, Feng et al.' study reveals that KCTD15 acts as a key oncogenic driver in TNBC via the KLF4/β‐catenin axis, highlighting its ...
Liang Yao, Wei Sun, Jun Xing, Jing Feng
wiley +1 more source
A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova +15 more
wiley +1 more source
Direct‐to‐Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery
Crude yet clever: Direct‐to‐biology workflows exploit nanoscale synthesis and plate‐based assays to accelerate hit discovery, save precious intermediates, and rethink early drug discovery. Direct‐to‐biology (D2B) has emerged as a transformative concept in early drug discovery, defined by the direct on‐target screening of crude reaction mixtures without
Ariane F. Hübner, Fabian Barthels
wiley +1 more source
Peripheral RIPK2 degradation improves neurological outcomes after experimental ischemic stroke. [PDF]
Howell JA +7 more
europepmc +1 more source
Revolutionizing protein degradation: Harnessing nanoparticles for PROTAC delivery. [PDF]
Fan Y +7 more
europepmc +1 more source

