Alanyl-tRNA synthetase 1 (AARS1) was recently identified as a lactyltransferase responsible for protein lactylation, a modification associated with epigenetic regulation and metabolic adaptation. Here, we report compound XY353, which covalently binds C184 of AARS1, inducing steric clashes with F175 and triggering struc...
Constitutive activation of STAT3 and dysregulation of the thioredoxin reductase 1 (TrxR1) system are deeply implicated in the pathogenesis, progression, and drug resistance of colorectal cancer (CRC). Herein, guided by a pharmacophore fusion strategy, we rationally designed and synthesized a novel series of STAT3/TrxR1...
A dual-targeting strategy aimed at simultaneously inhibiting the oncogenic protein-protein interaction between UBE2M and DCN1, which is critical for neddylation-dependent activation of cullin-RING ligases (CRLs) and histone deacetylase (HDAC) activity is developed.
Tao Zheng, Yi-Gui Li, Yun-Yuan Huang et al.· Journal of Medicinal Chemist...· 0 citations
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