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Lipid Vesicle-mediated Affinity Chromatography using Magnetic Activated Cell Sorting LIMACS: a Novel Method to Analyze Protein-lipid Interaction

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Lipid-conjugated Smac analogues.

Ewa D Micewicz¹, Josephine A Ratikan¹, Alan J Waring²

¹Department of Radiation Oncology, University of California at Los Angeles, 10833 Le Conte Avenue, Los Angeles, CA 90095, USA.

Bioorganic & Medicinal Chemistry Letters

|September 19, 2015

Summary

Researchers developed novel Smac mimics, finding that lipid modification enhanced their effectiveness against metastatic breast cancer. The lead compound M11 demonstrated significant in vivo activity via multiple administration routes, suggesting a promising therapeutic strategy.

Keywords:

Anticancer agents Apoptosis Lipids-conjugated peptides S-Alkylation of peptides Smac mimics

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Solid Lipid Nanoparticles SLNs for Intracellular Targeting Applications

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Published on: November 17, 2015

Area of Science:

Medicinal Chemistry
Oncology
Drug Discovery

Background:

Smac (Second Mitochondria-derived Activator of Caspases) mimics are a class of therapeutic agents targeting apoptosis.
Developing effective Smac mimics for cancer therapy remains an area of active research.
Targeting the MDA-MB-231 metastatic human breast cancer cell line is crucial for advancing treatment strategies.

Purpose of the Study:

To synthesize and evaluate a library of novel monovalent and bivalent Smac mimics.
To investigate the impact of lipidation on the efficacy of Smac mimics.
To identify potent Smac mimics for potential therapeutic application against metastatic breast cancer.

Main Methods:

Synthesis of Smac mimics based on NMeAla-Xaa-Pro-BHA monomers (Xaa=Cys or Lys).
Dimerization of monomers using bis-reactive linkers and modification with lipids.
In vitro screening against MDA-MB-231 human breast cancer cells.
In vivo evaluation of selected lead compounds.

Main Results:

A library of monovalent and bivalent Smac mimics was successfully synthesized.
Lipid-conjugated Smac mimic M11 exhibited significant in vitro activity against MDA-MB-231 cells.
Compound M11 demonstrated in vivo efficacy following both subcutaneous and oral administration.

Conclusions:

Lipidation is a viable strategy for enhancing the therapeutic potential of Smac-based compounds.
The developed Smac mimics, particularly M11, represent promising leads for the development of novel anti-cancer therapeutics.
Further investigation into lipidation-modified Smac mimics could yield effective treatments for metastatic breast cancer.