Background and Purpose In contrast to neurons in the central nervous system, neurons in the peripheral nervous system can regenerate axons after injury via activation of a pro‐regenerative transcriptional programme. Pathogenic mutations in leucine‐rich repeat kinase 2 (LRRK2) are the most common genetic cause of Parkinson's disease, and several small ...
Eun‐Hae Jang +11 more
wiley +1 more source
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
Targeted protein degradation dismantles undruggable targets to reverse immune evasion and therapy resistance in cancer. [PDF]
Zhang F +6 more
europepmc +1 more source
Copy number variation analysis in The Cancer Genome Atlas identified NTAQ1 as a potential driver of HCC progression. NTAQ1 accelerates tumor growth by promoting the degradation of the tumor suppressor protein PRDM2, thereby impairing DNA repair and suppressing apoptosis. These findings indicate that NTAQ1 could be a valuable target for the treatment of
Tomohiko Ikehara +21 more
wiley +1 more source
E3 Ubiquitin Ligases in MASH‐Associated Liver Fibrosis: Mechanisms and Therapeutic Opportunities
ABSTRACT Metabolic dysfunction‐associated steatohepatitis (MASH) is a major cause of progressive liver fibrosis and can ultimately lead to cirrhosis and hepatocellular carcinoma (HCC). MASH‐associated liver fibrosis develops through a complex interplay among lipotoxic hepatocyte injury, oxidative and endoplasmic reticulum stress, inflammatory ...
Ah‐Reum Oh +8 more
wiley +1 more source
Synthesis of RARα-PROTAC and its delivery via <i>Polygonatum sibiricum</i> exosome-like nanoparticles for the treatment of colorectal cancer. [PDF]
Zhu G +7 more
europepmc +1 more source
Intratumoral Mycobacterium abscessus promotes cytidine deaminase mutagenesis in non-small cell lung cancer. [PDF]
Li X +11 more
europepmc +1 more source
Evolving CRBN ligands enhance the drug-like properties of protein degraders. [PDF]
Ji XQ, Wang L, Dai XJ.
europepmc +1 more source
Advancing PROTAC therapeutics through chemistry-guided design of smart delivery systems. [PDF]
Yao TT, Zhou Z, Wang GJ, Zhu ZY, Li XN.
europepmc +1 more source
Design of Synthesizable PROTACs through Synthesis Constrained Generative Model and Reinforcement Learning. [PDF]
Xu M +12 more
europepmc +1 more source

