Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
PROTACs enable targeted protein degradation by recruiting an E3 ligase to a specific substrate but the determinants of selectivity are not fully understood. Here, the authors show that varying the linker between warhead and E3 ligand and the orientation of the E3 ligase allow tuning PROTAC selectivi...
Guardado en:
Autores principales: | Blake E. Smith, Stephen L. Wang, Saul Jaime-Figueroa, Alicia Harbin, Jing Wang, Brian D. Hamman, Craig M. Crews |
---|---|
Formato: | article |
Lenguaje: | EN |
Publicado: |
Nature Portfolio
2019
|
Materias: | |
Acceso en línea: | https://doaj.org/article/86ec9e4d91cb498bb96bd2e90667c3f4 |
Etiquetas: |
Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
|
Ejemplares similares
-
Mutant-selective degradation by BRAF-targeting PROTACs
por: Shanique Alabi, et al.
Publicado: (2021) -
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation
por: Chiara Maniaci, et al.
Publicado: (2017) -
Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
por: Wen-Hao Guo, et al.
Publicado: (2020) -
Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy
por: Chi Zhang, et al.
Publicado: (2021) -
Potential application of proteolysis targeting chimera (PROTAC) modification technology in natural products for their targeted protein degradation
por: Guliang Yang, et al.
Publicado: (2022)