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Synthesis and evaluation of the aldolase antibody-derived chemical-antibodies targeting α5β1 integrin

Academic Article
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Overview

authors

  • Goswami, R. K.
  • Liu, Y.
  • Liu, C.
  • Lerner, Richard
  • Sinha, Subhash

publication date

  • February 2013

journal

  • Molecular Pharmaceutics  Journal

abstract

  • Integrin α5β1 is an important therapeutic target that can be inhibited using an aldolase antibody (Ab)-derived chemical-Ab (chem-Ab) for the treatment of multiple human diseases, including cancers. A fairly optimized anti-integrin α5β1 chem-Ab 38C2-4e was obtained using an in situ convergent chemical programming (CP) approach, which minimized the time and effort needed to develop a chem-Ab. Multiple Ab-programming agents (PAs) 4a-e could be prepared rapidly using the Cu-catalyzed alkyne-azide coupling (Cu-AAC) reaction of an α5β1 inhibitor 2 with multiple linkers 3a-e, either before or after conjugating the linkers into Ab 38C2 binding sites. In these two-steps processes, the products after step 1 can be used in the next step without performing an extensive purification or analysis of the Ab-PAs or Ab-linker conjugates affording chem-Abs 38C2-(4a-e). Flow cytometry assay was used to determine the binding of the chem-Abs to U87 human glioblastoma cells expressing α5β1 integrin and identify 38C2-3e as the strongest binder. Further studies revealed that 38C2-3e strongly inhibited proliferation of U87 cells and tube formation of HUVEC in the matrigel assay, as well as tumor growth and metastasis of 4T1 cells in vivo.

subject areas

  • Antineoplastic Agents
  • Cell Line, Tumor
  • Cell Proliferation
  • Flow Cytometry
  • Fructose-Bisphosphate Aldolase
  • Humans
  • Immunoglobulin Fab Fragments
  • Integrin alpha5beta1
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Research

keywords

  • aldolase antibody
  • cancer
  • chemical programming integrin alpha 5 beta 1
  • chemical-antibody (chem-Ab)
  • in situ convergent strategy
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Identity

PubMed Central ID

  • PMC3596504

International Standard Serial Number (ISSN)

  • 1543-8384

Digital Object Identifier (DOI)

  • 10.1021/mp3004463

PubMed ID

  • 23102054
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Additional Document Info

start page

  • 538

end page

  • 543

volume

  • 10

issue

  • 2

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