Structure-activity relationship studies of targeting ligands against breast cancer cells.

Abstract

A series of LXY3 (1) analogues were designed and synthesized. Their binding affinity was demonstrated using MDA-MB-231 breast cancer cells adherence inhibition assay. Further structure-activity relationship was obtained. Analogue 29 was discovered to have 3.5-fold increase of the binding affinity. Fluorescent microscopy and in vivo and ex vivo imaging studies demonstrated that 29 is an efficient in vivo targeting agent against alpha3 integrin of MDA-MB-231 breast tumor xenograft implant.

• Authors: Nianhuan Yao, Wenwu Xiao, Leah Meza, Harry Tseng, Mathida Chuck, Kit S Lam
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 52 Issue 21 Pg. 6744-51 (Nov 12 2009) ISSN: 1520-4804 [Electronic] United States
• PMID: 19835381 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, U.S. Gov't, Non-P.H.S.)

Chemical References

• Antineoplastic Agents
• Integrin alpha3beta1
• Ligands
• Peptides, Cyclic

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Breast Neoplasms
• Cell Adhesion (drug effects)
• Cell Line, Tumor
• Drug Screening Assays, Antitumor
• Female
• Integrin alpha3beta1 (metabolism)
• Ligands
• Mice
• Mice, Nude
• Neoplasm Transplantation
• Peptides, Cyclic (chemical synthesis, chemistry, pharmacology)
• Protein Binding
• Structure-Activity Relationship
• Transplantation, Heterologous