World Library  


Add to Book Shelf
Flag as Inappropriate
Email this Book

Plos One : a Spiroligomer Α-helix Mimic That Binds Hdm2, Penetrates Human Cells and Stabilizes Hdm2 in Cell Culture, Volume 7

By Colombo, Giorgio

Click here to view

Book Id: WPLBN0003933156
Format Type: PDF eBook :
File Size:
Reproduction Date: 2015

Title: Plos One : a Spiroligomer Α-helix Mimic That Binds Hdm2, Penetrates Human Cells and Stabilizes Hdm2 in Cell Culture, Volume 7  
Author: Colombo, Giorgio
Volume: Volume 7
Language: English
Subject: Journals, Science, Medical Science
Collections: Periodicals: Journal and Magazine Collection (Contemporary)
Historic
Publication Date:
Publisher: Plos

Citation

APA MLA Chicago

Colombo, G. (n.d.). Plos One : a Spiroligomer Α-helix Mimic That Binds Hdm2, Penetrates Human Cells and Stabilizes Hdm2 in Cell Culture, Volume 7. Retrieved from http://www.nationalpubliclibrary.info/


Description
Description : We demonstrate functionalized spiroligomers that mimic the HDM2-bound conformation of the p53 activation domain. Spiroligomers are stereochemically defined, functionalized, spirocyclic monomers coupled through pairs of amide bonds to create spiro-ladder oligomers [1]. Two series of spiroligomers were synthesized, one of structural analogs and one of stereochemical analogs, from which we identified compound 1, that binds HDM2 with a Kd value of 400 nM. The spiroligomer 1 penetrates human liver cancer cells through passive diffusion and in a dose-dependent and time-dependent manner increases the levels of HDM2 more than 30-fold in Huh7 cells in which the p53/HDM2 negative feed-back loop is inoperative. This is a biological effect that is not seen with the HDM2 ligand nutlin-3a. We propose that compound 1 modulates the levels of HDM2 by stabilizing it to proteolysis, allowing it to accumulate in the absence of a p53/HDM2 feedback loop.

 

Click To View

Additional Books


  • Plos One : Inhibition of Pbgp43 Expressi... (by )
  • Plos One : Long-term Artificial Sweetene... (by )
  • Plos One : Improved Learning in U.S. His... (by )
  • Plos One : In-vitro Archaeacidal Activit... (by )
  • Plos One : Possible Involvement of Cone ... (by )
  • Plos One : Soil Respiration and Organic ... (by )
  • Plos One : Vitamin D Status, Filaggrin G... (by )
  • Plos One : ‘‘rational’’ Management of Di... (by )
  • Plos One : Transcription Factor Klf4, In... (by )
  • Plos One : Some Pneumococcal Serotypes A... (by )
  • Plos One : a Quantitative Proteomic Prof... (by )
  • Plos One : Whole Number, Distribution an... (by )
Scroll Left
Scroll Right

 



Copyright © World Library Foundation. All rights reserved. eBooks from National Public Library are sponsored by the World Library Foundation,
a 501c(4) Member's Support Non-Profit Organization, and is NOT affiliated with any governmental agency or department.