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Nat Commun ; 15(1): 4584, 2024 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-38811577

RESUMO

Stimulator of interferon genes (STING) is a central component of the cytosolic nucleic acids sensing pathway and as such master regulator of the type I interferon response. Due to its critical role in physiology and its' involvement in a variety of diseases, STING has been a focus for drug discovery. Targeted protein degradation (TPD) has emerged as a promising pharmacology for targeting previously considered undruggable proteins by hijacking the cellular ubiquitin proteasome system (UPS) with small molecules. Here, we identify AK59 as a STING degrader leveraging HERC4, a HECT-domain E3 ligase. Additionally, our data reveals that AK59 is effective on the common pathological STING mutations, suggesting a potential clinical application of this mechanism. Thus, these findings introduce HERC4 to the fields of TPD and of compound-induced degradation of STING, suggesting potential therapeutic applications.


Assuntos
Proteínas de Membrana , Proteólise , Ubiquitina-Proteína Ligases , Ubiquitina-Proteína Ligases/metabolismo , Ubiquitina-Proteína Ligases/genética , Humanos , Proteínas de Membrana/metabolismo , Proteínas de Membrana/genética , Proteólise/efeitos dos fármacos , Células HEK293 , Animais , Mutação , Complexo de Endopeptidases do Proteassoma/metabolismo , Ubiquitinação
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