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Pure and Applied Chemistry

The Scientific Journal of IUPAC

Ed. by Burrows, Hugh / Weir, Ron / Stohner, Jürgen

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Volume 72, Issue 3 (Jan 2000)


The chelate effect in binding, catalysis, and chemotherapy

Ronald Breslow
  • Corresponding author
  • Department of Chemistry, Columbia University, New York, New York 10027, USA
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/ Sandro Belvedere
  • Corresponding author
  • Department of Chemistry, Columbia University, New York, New York 10027, USA
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/ Leland Gershell
  • Corresponding author
  • Department of Chemistry, Columbia University, New York, New York 10027, USA
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/ David Leung
  • Corresponding author
  • Department of Chemistry, Columbia University, New York, New York 10027, USA
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Published Online: 2009-01-01 | DOI: https://doi.org/10.1351/pac200072030333

Cyclodextrin (CD) dimers bind amino acid side chains, and such binding can dissociate aggregated proteins, including citrate synthase (dimer) and lactic dehydrogenase (tetramer). A CD dimer can bind a hydrophobic photosensitizer that, upon irradiation, generates singlet oxygen. This cleaves the dimer and releases the photosensitizer. CD dimers in a cytochrome P-450 mimic steer catalyzed hydroxylation to a bound steroid with geometric control. Chelate binding has also led to a group of cytodifferentiating agents whose mechanism has been recently established. They have promising anticancer properties, and are currently entering human trials as therapeutic agents.


International IUPAC Symposium on Bioorganic Chemistry (ISBOC-5), International Symposium on Bioorganic Chemistry, ISBOC, Bioorganic Chemistry, 5th, Pune, India, 2000-01-30–2000-02-04

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Published Online: 2009-01-01

Published in Print: 2000-01-01

Citation Information: Pure and Applied Chemistry, ISSN (Online) 1365-3075, ISSN (Print) 0033-4545, DOI: https://doi.org/10.1351/pac200072030333.

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