Cell‐Selective Delivery of RIBOTACs via an Anti‐EGFR Nanobody for Pancreatic Cancer Treatment
This study introduces an innovative strategy for the tumor‐selective catalytic degradation of oncogenic non‐coding RNA by interfacing a ribonuclease‐recruiting small molecule (RIBOTAC) with an EGFR‐targeting nanobody via a CTSB (Cathepsin B)‐responsive linker.
Tianli Luo +15 more
wiley +1 more source
DNA-Templated Spatially Controlled Proteolysis Targeting Chimera for Cyclin D1-CDK4/6 Complex Protein Degradation. [PDF]
Zheng R +7 more
europepmc +1 more source
Imine Reductase‐Mediated Regio‐ and Stereoselective Reductive Amination of Diamines
Imine reductases (IREDs) have been employed as biocatalysts for the regioselective modification of diamines via reductive amination. The use of racemic diamines resulted in both regio‐ and enantio‐selective reductive amination via kinetic resolution. The application of this methodology has been demonstrated on a preparative scale by the synthesis of a ...
Arnau Rué Casamajo +7 more
wiley +1 more source
Identification of a Proteolysis-Targeting-Chimera that Addresses Activated Checkpoint Kinase-1 Reveals its Non-Catalytic Functions in Tumor Cells. [PDF]
Ashry R +13 more
europepmc +1 more source
Computational drug discovery integrates molecular docking, molecular dynamics simulations, and translational clinical targeting to identify next‐generation therapeutics that overcome endocrine resistance in ER‐positive breast cancer. Combined with multi‐omics, artificial intelligence, and biomarker‐guided precision oncology, these approaches accelerate
Emmanuel Ifeanyi Obeagu, Yaregal Asres
wiley +1 more source
PROteolysis TArgeting Chimera (PROTAC) Estrogen Receptor Degraders for Treatment of Estrogen Receptor-Positive Advanced Breast Cancer. [PDF]
Hamilton EP +3 more
europepmc +1 more source
Bioactive peptides in cancer and inflammation: Mechanisms, model systems and clinical translation
Bioactive peptides (BAPs) derived from host, marine, insect, plant and synthetic sources share cationic, amphipathic structures adopting α‐helical, β‐sheet or cyclic conformations. These features underlie anti‐cancer effects, including membrane disruption, apoptosis and cell‐cycle arrest, anti‐metastatic activity, reduced invasion and migration, and ...
Najwa Doha +4 more
wiley +1 more source
Abstract Richter transformation (RT), a highly aggressive lymphoma arising from a preexisting chronic lymphocytic leukemia, represents a major unmet clinical need. Recent data have shown that an antibody–drug conjugate (ADC) targeting the cell‐surface pseudokinase ROR1 is effective in RT patients.
Matilde Micillo +9 more
wiley +1 more source
DNA-Programmable Protein Degradation: Dynamic Control of Proteolysis-Targeting Chimera Activity via DNA Hybridization and Strand Displacement. [PDF]
Kashyap D, Haider S, Milne TA, Booth MJ.
europepmc +1 more source
ABSTRACT Background and Aims The phosphatidylinositol 3‐kinase (PI3K)/Akt signaling pathway is a central regulator of cellular properties that are essential for cancer progression, including cellular growth, survival, metabolism, and angiogenesis. Dysregulated PI3K/Akt signaling, often caused by genetic alterations in PIK3CA, loss of PTEN, or the ...
Md Mohiuddin
wiley +1 more source

