Protein degradation strategy offers new hope in cancer therapy
2 days ago · University of California - Riverside. "Protein degradation strategy offers new hope in cancer therapy." ScienceDaily. ScienceDaily, 11 November 2024. <www.sciencedaily.com / releases / 2024 / 11 ...
Molecular Crowbar Strategy Pulls Apart Protein's Hold on …
2 days ago · Scientists at the University of California, Riverside (UCR), have developed a “molecular crowbar” strategy to identify protein degraders that target Pin1, a protein involved in pancreatic ...
Protein Degradation Method Paves a Way for New Cancer Therapies
3 days ago · Scientists at the University of California, Riverside (UCR), are now using this method to pave a way for new cancer therapies. The scientists have developed a “molecular crowbar” strategy to identify protein degraders that target Pin1, a protein involved in pancreatic cancer development. The scientists designed agents that bind tightly to ...
Targeted degradation of Pin1 by protein-destabilizing compounds
Application of this strategy to the proline cis–trans isomerase Pin1 resulted in potent compounds that are effective in causing Pin1 degradation in several human cancer cell lines and that can be translated into potential anticancer agents. ... G. G. Xu, F. A. Etzkorn, Pin1 as an anticancer drug target. Drug News Perspect. 22, 399–407 (2009 ...
Stabilization of Pin1 by USP34 promotes Ubc9 isomerization and …
Jan 2, 2024 · The current study demonstrates that the peptidyl prolyl cis-trans isomerase Pin1 is deubiquitinated and stabilized by the DUB USP34, which further isomerizes the sole SUMO E2 enzyme Ubc9 to ...
Sulfopin is a covalent inhibitor of Pin1 that blocks Myc ... - Nature
May 10, 2021 · The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors. However, despite considerable efforts, Pin1 has remained an elusive drug...
News - Larkspur Bioscience
Mar 28, 2024 · Larkspur Biosciences to Present New Mechanistic Data on the Role of Pin1 in Modulating the Fibroblast – Cancer Axis at SITC 2023. Oct 25, 2023 • Press Release. Research emphasizes the significant role of Pin1 in influencing critical cancer mechanisms to drive a pro-immune response, re...
Ligand-specific conformational change drives interdomain allostery in Pin1
Aug 4, 2022 · Pin1 is a two-domain cell regulator that isomerizes peptidyl-prolines. The catalytic domain (PPIase) and the other ligand-binding domain (WW) sample extended and compact conformations.
Targeting Pin1 renders pancreatic cancer eradicable by ... - PubMed
Sep 2, 2021 · Unique proline isomerase Pin1 regulates multiple cancer pathways, but its role in the TME and cancer immunotherapy is unknown. Here, we find that Pin1 is overexpressed both in cancer cells and cancer-associated fibroblasts (CAFs) and …
Targeting Pin1 for Modulation of Cell Motility and Cancer Therapy
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) specifically binds and isomerizes the phosphorylated serine/threonine-proline (pSer/Thr-Pro) motif, which leads to changes in protein conformation and function.