Compound class:
Peptide or derivative
Comment: This is a synthetic peptide designed as a long-acting CMKLR1 agonist. The construct tethers the potent chemerin receptor agonist chemerin C-terminal peptide to the outer surface of the cell membrane, in juxtaposition to the receptor [1].
Structural and sequence details are: 1-56 TNFα type II transmembrane domain 57-78 repetitive glycine-asparagine linker 79-88 myc epitope tag 89-99 repetitive glycine-asparagine linker 100-108 chemerin C-terminal peptide at the carboxy terminal of the construct [1-2]. In vivo delivery is achieved by lipidating the chemerin nonapeptide portion of the construct [1]. The potent chemoattractant mediating effects of CMKLR1 has lead to the development of chemerin agonists as candidate therapeutics to improve resolution of inflammation, particularly as has been established in asthma models [3]. 
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Doyle JR, Krishnaji ST, Zhu G, Xu ZZ, Heller D, Ji RR, Levy BD, Kumar K, Kopin AS. (2014)
Development of a membrane-anchored chemerin receptor agonist as a novel modulator of allergic airway inflammation and neuropathic pain. J Biol Chem, 289 (19): 13385-96. [PMID:24659779] |
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2. Harwood BN, Fortin JP, Gao K, Chen C, Beinborn M, Kopin AS. (2013)
Membrane tethered bursicon constructs as heterodimeric modulators of the Drosophila G protein-coupled receptor rickets. Mol Pharmacol, 83 (4): 814-21. [PMID:23340494] |
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3. Haworth O, Cernadas M, Yang R, Serhan CN, Levy BD. (2008)
Resolvin E1 regulates interleukin 23, interferon-gamma and lipoxin A4 to promote the resolution of allergic airway inflammation. Nat Immunol, 9 (8): 873-9. [PMID:18568027] |
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4. Wittamer V, Franssen JD, Vulcano M, Mirjolet JF, Le Poul E, Migeotte I, Brézillon S, Tyldesley R, Blanpain C, Detheux M, Mantovani A, Sozzani S, Vassart G, Parmentier M, Communi D. (2003)
Specific recruitment of antigen-presenting cells by chemerin, a novel processed ligand from human inflammatory fluids. J Exp Med, 198 (7): 977-85. [PMID:14530373] |
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5. Wittamer V, Grégoire F, Robberecht P, Vassart G, Communi D, Parmentier M. (2004)
The C-terminal nonapeptide of mature chemerin activates the chemerin receptor with low nanomolar potency. J Biol Chem, 279 (11): 9956-62. [PMID:14701797] |
