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Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

Alabi, Shanique B. ; Crews, Craig M.

The Journal of biological chemistry, 2021-01, Vol.296, p.100647-100647, Article 100647 [Periódico revisado por pares]

United States: Elsevier Inc

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  • Título:
    Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs
  • Autor: Alabi, Shanique B. ; Crews, Craig M.
  • Assuntos: AUTACs ; chemical biology ; drug action ; JBC Reviews ; lysosome ; LYTACs ; molecular glues ; PROTACs ; protein degradation ; ubiquitination
  • É parte de: The Journal of biological chemistry, 2021-01, Vol.296, p.100647-100647, Article 100647
  • Notas: ObjectType-Article-2
    SourceType-Scholarly Journals-1
    ObjectType-Feature-3
    content type line 23
    ObjectType-Review-1
  • Descrição: Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates complete removal of the protein molecules from within or outside the cell. While the pioneering Proteolysis-Targeting Chimera (PROTAC) technology and molecular glues hijack the ubiquitin-proteasome system, newer modalities co-opt autophagy or the endo-lysosomal pathway. Using this mechanism, TPD is posited to largely expand the druggable space far beyond small-molecule inhibitors. In this review, we discuss the major advances in TPD, highlight our current understanding, and explore outstanding questions in the field.
  • Editor: United States: Elsevier Inc
  • Idioma: Inglês

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