Development of stapled helical peptides to perturb the Cdt1-Mcm6 interaction.
Six all-hydrocarbon-stapled Cdt1 MBD-derived peptides have been designed and synthesized to perturb the Cdt1-Mcm6 interaction, which is involved in DNA replication. Inconsistency between the helicity of the obtained peptidomimetics and their binding affinity has been observed. The helicity of 13-amino acid stapled peptides increased, while their binding to Mcm6 was decreased. On the other hand, the 30-amino acid stapled peptides exhibited decreased helicity but increased binding affinity.
Department of Chemistry, The University of Hong Kong, Hong Kong, China.
Jonghan Peter
JP
Lee
Division of Life Science, The Hong Kong University of Sciences and Technology, Hong Kong, China.
Changdong
C
Liu
Department of Chemistry, The University of Hong Kong, Hong Kong, China.
Tianlu
T
Li
Division of Life Science, The Hong Kong University of Sciences and Technology, Hong Kong, China.
Guang
G
Zhu
Department of Chemistry, The University of Hong Kong, Hong Kong, China.|State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Hong Kong, China.
Xuechen
X
Li
D001665:Binding Sites; D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D064151:Minichromosome Maintenance Complex Component 6 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D008958:Models, Molecular; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry*; D057786:Peptidomimetics / Q000138:chemical synthesis / Q000737:chemistry*; D011485:Protein Binding; D017433:Protein Structure, Secondary
C467199:CDT1 protein, human; D018797:Cell Cycle Proteins; D010455:Peptides; D057786:Peptidomimetics; C103258:MCM6 protein, human; D064151:Minichromosome Maintenance Complex Component 6
Cdt1; Mcm6; peptidomimetics; stapled peptides