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El desarrollo de inhibidores de interacciones proteína-proteína a través REEMPLAZAR: Aplicación al Diseño y Desarrollo para no ATP inhibidores de CDK Competitiva
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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El desarrollo de inhibidores de interacciones proteína-proteína a través REEMPLAZAR: Aplicación al Diseño y Desarrollo para no ATP inhibidores de CDK Competitiva

DOI:
10.3791/52441-v

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10:33 min

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October 26, 2015

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, ,
1Department of Drug Discovery and Biomedical Sciences,University of South Carolina

Chapters

  • 00:05Title
  • 01:57Computational Identification of Potential Small Molecule Capping Groups
  • 04:03Synthesis of Potential N-capping Groups
  • 06:25Solid Phase Synthesis for the Generation of FLIPs
  • 08:45Results: Identification of More Drug-like Inhibitors of CDK2 through the Cyclin Groove
  • 09:59Conclusion

Summary

자동 번역

자동 번역

We describe implementation of the REPLACE strategy for targeting protein-protein interactions. REPLACE is an iterative strategy involving synthetic and computational approaches for the conversion of optimized peptidic inhibitors into drug like molecules.

Tags

Protein-protein InteractionsREPLACE StrategyCyclin Dependent Kinases (CDK)Non-ATP Competitive InhibitorsCDK2/cyclin ACyclin Binding Groove (CBG)Cyclin Binding Motif (CBM)P21WafFragment Ligated Inhibitory Peptides (FLIPs)Anti-tumor Therapeutics

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