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A CXCL8 receptor antagonist based on the structure of N-acetyl-proline-glycine-proline.

Jackson PL, Noerager BD, Jablonsky MJ, Hardison MT, Cox BD, Patterson JC, Dhanapal B, Blalock JE, Muccio DD.

Eur J Pharmacol. 2011 Oct 15;668(3):435-42. doi: 10.1016/j.ejphar.2011.02.045. Epub 2011 Mar 31.


N-acetylated Proline-Glycine-Proline induced G-protein dependent chemotaxis of neutrophils is independent of CXCL8 release.

Overbeek SA, Henricks PA, Srienc AI, Koelink PJ, de Kruijf P, Lim HD, Smit MJ, Zaman GJ, Garssen J, Nijkamp FP, Kraneveld AD, Folkerts G.

Eur J Pharmacol. 2011 Oct 15;668(3):428-34. doi: 10.1016/j.ejphar.2011.03.022. Epub 2011 Mar 31.


Targeting of a common receptor shared by CXCL8 and N-Ac-PGP as a therapeutic strategy to alleviate chronic neutrophilic lung diseases.

Snelgrove RJ.

Eur J Pharmacol. 2011 Sep 30;667(1-3):1-5. doi: 10.1016/j.ejphar.2011.05.073. Epub 2011 Jun 7. Review.


The collagen-breakdown product N-acetyl-Proline-Glycine-Proline (N-alpha-PGP) does not interact directly with human CXCR1 and CXCR2.

de Kruijf P, Lim HD, Overbeek SA, Zaman GJ, Kraneveld AD, Folkerts G, Leurs R, Smit MJ.

Eur J Pharmacol. 2010 Sep 15;643(1):29-33. doi: 10.1016/j.ejphar.2010.06.017. Epub 2010 Jun 21.


Bioactivity of peptide analogs of the neutrophil chemoattractant, N-acetyl-proline-glycine-proline.

Haddox JL, Pfister RR, Muccio DD, Villain M, Sommers CI, Chaddha M, Anantharamaiah GM, Brouillette WJ, DeLucas LJ.

Invest Ophthalmol Vis Sci. 1999 Sep;40(10):2427-9.


Extracellular matrix-derived tripeptide proline-glycine-proline inhibits keratinocyte proliferation and migration.

Ma Y, Kleinbeck K, Kao WJ.

Wound Repair Regen. 2011 Nov;19(6):718-26. doi: 10.1111/j.1524-475X.2011.00734.x. Epub 2011 Oct 12.


Probing the role of CXC motif in chemokine CXCL8 for high affinity binding and activation of CXCR1 and CXCR2 receptors.

Joseph PR, Sarmiento JM, Mishra AK, Das ST, Garofalo RP, Navarro J, Rajarathnam K.

J Biol Chem. 2010 Sep 17;285(38):29262-9. doi: 10.1074/jbc.M110.146555. Epub 2010 Jul 14.


CXCR2 antagonists block the N-Ac-PGP-induced neutrophil influx in the airways of mice, but not the production of the chemokine CXCL1.

Braber S, Overbeek SA, Koelink PJ, Henricks PA, Zaman GJ, Garssen J, Kraneveld AD, Folkerts G.

Eur J Pharmacol. 2011 Oct 15;668(3):443-9. doi: 10.1016/j.ejphar.2011.03.025. Epub 2011 Mar 31.


Synthetic complementary peptides inhibit a neutrophil chemoattractant found in the alkali-injured cornea.

Pfister RR, Haddox JL, Blalock JE, Sommers CI, Coplan L, Villain M.

Cornea. 2000 May;19(3):384-9.


A novel proteolytic cascade generates an extracellular matrix-derived chemoattractant in chronic neutrophilic inflammation.

Gaggar A, Jackson PL, Noerager BD, O'Reilly PJ, McQuaid DB, Rowe SM, Clancy JP, Blalock JE.

J Immunol. 2008 Apr 15;180(8):5662-9.


NMR conformational analysis of cis and trans proline isomers in the neutrophil chemoattractant, N-acetyl-proline-glycine-proline.

Lee YC, Jackson PL, Jablonsky MJ, Muccio DD, Pfister RR, Haddox JL, Sommers CI, Anantharamaiah GM, Chaddha M.

Biopolymers. 2001 May;58(6):548-61.


Key role of proline-rich tyrosine kinase 2 in interleukin-8 (CXCL8/IL-8)-mediated human neutrophil chemotaxis.

Di Cioccio V, Strippoli R, Bizzarri C, Troiani G, Cervellera MN, Gloaguen I, Colagrande A, Cattozzo EM, Pagliei S, Santoni A, Colotta F, Mainiero F, Bertini R.

Immunology. 2004 Apr;111(4):407-15.


A novel peptide CXCR ligand derived from extracellular matrix degradation during airway inflammation.

Weathington NM, van Houwelingen AH, Noerager BD, Jackson PL, Kraneveld AD, Galin FS, Folkerts G, Nijkamp FP, Blalock JE.

Nat Med. 2006 Mar;12(3):317-23. Epub 2006 Feb 12.


Cigarette smoke-induced collagen destruction; key to chronic neutrophilic airway inflammation?

Overbeek SA, Braber S, Koelink PJ, Henricks PA, Mortaz E, LoTam Loi AT, Jackson PL, Garssen J, Wagenaar GT, Timens W, Koenderman L, Blalock JE, Kraneveld AD, Folkerts G.

PLoS One. 2013;8(1):e55612. doi: 10.1371/journal.pone.0055612. Epub 2013 Jan 31. Erratum in: PLoS One. 2013;8(10). doi:10.1371/annotation/0faf4c12-4fd4-474c-b5a4-16e49370aff3.


Mechanisms mediating the biologic activity of synthetic proline, glycine, and hydroxyproline polypeptides in human neutrophils.

Weinberger B, Hanna N, Laskin JD, Heck DE, Gardner CR, Gerecke DR, Laskin DL.

Mediators Inflamm. 2005 Feb 24;2005(1):31-8.


Induction of lung emphysema is prevented by L-arginine-threonine-arginine.

van Houwelingen AH, Weathington NM, Verweij V, Blalock JE, Nijkamp FP, Folkerts G.

FASEB J. 2008 Sep;22(9):3403-8. doi: 10.1096/fj.07-096230. Epub 2008 Jun 12.


Neutrophil chemotaxis caused by chronic obstructive pulmonary disease alveolar macrophages: the role of CXCL8 and the receptors CXCR1/CXCR2.

Kaur M, Singh D.

J Pharmacol Exp Ther. 2013 Oct;347(1):173-80. doi: 10.1124/jpet.112.201855. Epub 2013 Aug 2.


Inhibition of interleukin-8 (CXCL8/IL-8) responses by repertaxin, a new inhibitor of the chemokine receptors CXCR1 and CXCR2.

Casilli F, Bianchini A, Gloaguen I, Biordi L, Alesse E, Festuccia C, Cavalieri B, Strippoli R, Cervellera MN, Di Bitondo R, Ferretti E, Mainiero F, Bizzarri C, Colotta F, Bertini R.

Biochem Pharmacol. 2005 Feb 1;69(3):385-94. Epub 2004 Dec 9.


Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist.

Gonsiorek W, Fan X, Hesk D, Fossetta J, Qiu H, Jakway J, Billah M, Dwyer M, Chao J, Deno G, Taveras A, Lundell DJ, Hipkin RW.

J Pharmacol Exp Ther. 2007 Aug;322(2):477-85. Epub 2007 May 11.


Treatment with DF 2162, a non-competitive allosteric inhibitor of CXCR1/2, diminishes neutrophil influx and inflammatory hypernociception in mice.

Cunha TM, Barsante MM, Guerrero AT, Verri WA Jr, Ferreira SH, Coelho FM, Bertini R, Di Giacinto C, Allegretti M, Cunha FQ, Teixeira MM.

Br J Pharmacol. 2008 May;154(2):460-70. doi: 10.1038/bjp.2008.94. Epub 2008 Mar 24.

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