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Comment
. 2011 Sep;3(9):510-2.
doi: 10.1002/emmm.201100161. Epub 2011 Aug 19.

Novel approach to inhibiting chemokine function

Morris F Ling  1 , Andrew D Luster
Affiliations
Comment

Novel approach to inhibiting chemokine function

Morris F Ling et al. EMBO Mol Med. 2011 Sep.
No abstract available

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Figures

Figure 1
Figure 1. Q1-CCL2, the mature uncyclized form of CCL2, is converted to cyclized pE1-CCL2 by iso-glutaminyl cyclase (isoQC)
Cyclized pE1-CCL2 is as potent a CCR2 ligand and inducer of moncyte chemotaxis as Q1-CCL2. However, Q1-CCL2 is susceptible to degradation by aminopeptidases, such as DDP-4, which generates products with much weaker biological activity (e.g. D3-CCL2). In contrast, cyclized pE1-CCL2 is resistant to N-terminal proteolytic processing and thus maintains its potency and activity. Inhibition of isoQC enzymatic activity using QC/isoQC inhibitors, results in decreased levels of pE1-CCL2, corresponding increased levels of Q1-CCL2 and subsequent degradation to less active CCL2 variants.
See this image and copyright information in PMC

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