NMR in the analysis of functional chemokine interactions and drug discovery

Joshua J. Ziarek, Brian F. Volkman*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

3 Scopus citations


The involvement of chemokines and chemokine receptors in a great variety of pathological indications underscores their utility as therapeutic targets. In general, chemokine-mediated migration and signaling requires three distinct interactions: self-association, glycosaminoglycan (GAG) binding and activation of G proteincoupled receptors (GPCRs). Solution-state nuclear magnetic resonance (NMR) spectroscopy has long been used to determine the apo structure of chemokines and monitor complex formation; however, it has never contributed directly to drug discovery efforts that are traditionally focused on the previously inaccessible chemokine receptors. Our lab recently demonstrated that NMR structures can be successfully utilized to direct drug discovery against chemokines. The ease of collecting chemokine structural data coupled with the increased efficiency of structure-based drug discovery campaigns makes chemokinedirected therapies particularly attractive. In addition, recent advances in sample preparation, spectrometer hardware and pulse program development are allowing researchers to examine interactions with previously inaccessible partners - including full-length chemokine receptors. These developments will facilitate exploration of novel ways to modulate chemokine activity using structure-guided drug discovery.

Original languageEnglish (US)
Pages (from-to)e293-e299
JournalDrug Discovery Today: Technologies
Issue number4
StatePublished - 2012

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery


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