Asset Details
Do you wish to reserve the book?
Study on the design, synthesis and activity of MDM2/MDMX anti-tumor stapled peptide PROTAC
Hey, we have placed the reservation for you!
By the way, why not check out events that you can attend while you pick your title.
Oops! Something went wrong.
Looks like we were not able to place the reservation. Kindly try again later.
Are you sure you want to remove the book from the shelf?
Study on the design, synthesis and activity of MDM2/MDMX anti-tumor stapled peptide PROTAC
Do you wish to request the book?
Study on the design, synthesis and activity of MDM2/MDMX anti-tumor stapled peptide PROTAC
Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy
We have requested the book for you!
Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.
Oops! Something went wrong.
Looks like we were not able to place your request. Kindly try again later.
Journal Article
Study on the design, synthesis and activity of MDM2/MDMX anti-tumor stapled peptide PROTAC
2025
Overview
PROTAC is a drug development technology that uses the Ubiquitin-Proteasome System (UPS) to degrade target proteins, and enhances the degradation ability of target proteins through E3 ubiquitin ligase, which can further enhance the anti-tumor effect of targeted drug molecules. In this study, a series of dual-target MDM2/MDMX stapled peptide PROTAC based on SM3-4 were designed and synthesized, and the stapled peptide PROTAC DSM3-2 and DSM3-5 screened in the study inhibited tumor cell growth in vitro at low µM concentrations. The results showed that the enhancement of stapled peptide activity was positively correlated with the increase of helicity, which provided an effective research basis for the dual-target anti-tumor stapled peptide PROTAC. Molecular docking experiments have shown that the binding peptide DSM3-2 can effectively bind to the target proteins MDM2 and MDMX to exert a dual targeting effect on tumor cells.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ Antineoplastic Agents - chemical synthesis
/ Antineoplastic Agents - chemistry
/ Antineoplastic Agents - pharmacology
/ Cell Proliferation - drug effects
/ Humanities and Social Sciences
/ Humans
/ Ligands
/ Molecular Docking Simulation
/ Peptides
/ Peptides - chemical synthesis
/ Phenols
/ PROTAC
/ Proteins
/ Proto-Oncogene Proteins - chemistry
/ Proto-Oncogene Proteins - metabolism
/ Proto-Oncogene Proteins c-mdm2 - chemistry
/ Proto-Oncogene Proteins c-mdm2 - metabolism
/ Reagents
/ Science
/ Tumors
