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Macrocyclic peptides as a new class of targeted protein degraders.
RSC Chem Biol
January 2025
School of Chemistry, The University of Sydney Sydney NSW 2006 Australia
Targeted protein degraders, in the form of proteolysis targeting chimaeras (PROTACs) and molecular glues, leverage the ubiquitin-proteasome system to catalytically degrade specific target proteins of interest. Because such molecules can be extremely potent, they have attracted considerable attention as a therapeutic modality in recent years. However, while targeted degraders have great potential, they are likely to face many of the same challenges as more traditional small molecules when it comes to their development as therapeutics.
View Article and Find Full Text PDFAnti-proteolytic regulation of KRAS by USP9X/NDRG3 in KRAS-driven cancer development.
Nat Commun
January 2025
Personalized Genomic Medicine Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Daejeon, Korea.
Cancers with activating mutations of KRAS show a high prevalence but remain intractable, requiring innovative strategies to overcome the poor targetability of KRAS. Here, we report that KRAS expression is post-translationally up-regulated through deubiquitination when the scaffolding function of NDRG3 (N-Myc downstream-regulated gene 3) promotes specific interaction between KRAS and a deubiquitinating enzyme, USP9X. In KRAS-mutant cancer cells KRAS protein expression, downstream signaling, and cell growth are highly dependent on NDRG3.
View Article and Find Full Text PDFCoralyne Targets the Catalytic Domain of MMP9: An In Silico and In Vitro Investigation.
Crit Rev Oncog
January 2025
GITAM.
Coralyne (COR) is a protoberberine-like isoquinoline alkaloid, and it is known for double-stranded (ds) DNA intercalation and topoisomerase inhibition. It can also sensitize cancer cells through various mechanisms. COR reduces the proliferation and migration of breast cancer cells by inhibiting the expression and activity of matrix metalloproteinase 9 (MMP9).
View Article and Find Full Text PDFIdentification and Characterization of a Protease Producing Strain From Tannery Waste for Efficient Dehairing of Goat Skin.
Biomed Res Int
January 2025
Center for Personalized Nanomedicine, Australian Institute for Bioengineering & Nanotechnology (AIBN), The University of Queensland, Brisbane, Queensland, Australia.
Environmental pollution has been a significant concern for the last few years. The leather industry significantly contributes to the economy but is one of Bangladesh's most prominent polluting industries. It is also responsible for several severe diseases such as cancer, lung diseases, and heart diseases of leather workers because they use bleaching agents and chemicals, and these have numerous adverse effects on human health.
View Article and Find Full Text PDFThiol-Reactive or Redox-Active: Revising a Repurposing Screen Led to a New Invalidation Pipeline and Identified a True Noncovalent Inhibitor Against Papain-like Protease from SARS-CoV-2.
ACS Pharmacol Transl Sci
January 2025
Fraunhofer Institute for Translational Medicine and Pharmacology ITMP, Discovery Research ScreeningPort, Schnackenburgallee 114, 22525 Hamburg, Germany.
The SARS-CoV-2 papain-like protease PLpro has multiple roles in the viral replication cycle, related to both its polypeptide cleavage function and its ability to antagonize the host immune response. Targeting the PLpro function is recognized as a promising mechanism to modulate viral replication, while supporting host immune responses. However, the development of PLpro-specific inhibitors remains challenging.
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