Comparison of cell-based assays for the identification and evaluation of competitive CXCR4 inhibitors

PLoS ONE

Volumn 12, Issue 4, 2017, Pages

  Van Hout, Anneleen ^a   D'Huys, Thomas ^a   Oeyen, Merel ^a   Schols, Dominique ^a   Van Loy, Tom ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

8 [(4 AMINOBUTYL)(2 BENZIMIDAZOLYLMETHYL)AMINO] 1,2,3,4 TETRAHYDROQUINOLINE; CALCIUM; CHEMOKINE RECEPTOR CXCR4; CHEMOKINE RECEPTOR CXCR4 ANTAGONIST; CTCE 9908; GAMBOGIC ACID; IT 1T; ME 6TREN; N [1,4,8,11 TETRAAZACYCLOTETRADECANYL 1,4 PHENYLENEBIS(METHYLENE)] 2 (AMINOMETHYL)PYRIDINE; PLERIXAFOR; STROMAL CELL DERIVED FACTOR 1; T 140; TC 14012; UNCLASSIFIED DRUG; WZ 811; [5,12 TYROSINE 7 LYSINE]POLYPHEMUSIN; AMINOPYRIDINE DERIVATIVE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; BENZYLAMINE DERIVATIVE; HETEROCYCLIC COMPOUND; N,N'-DI-2-PYRIDINYL-1,4-BENZENEDIMETHANAMINE; N-(1,4,8,11- TETRAAZACYCLOTETRADECANYL-1,4-PHENYLENEBIS(METHYLENE))-2-(AMINOMETHYL)- PYRIDINE; PROTEIN BINDING; PYRIDINE DERIVATIVE;

ANTIVIRAL ACTIVITY; ARTICLE; CALCIUM SIGNALING; CELL MIGRATION; CHEMOTAXIS ASSAY; COMPETITIVE BINDING ASSAY; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; EC50; ENDOCYTOSIS; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; IC50; IN VITRO STUDY; INTERMETHOD COMPARISON; INTERNALIZATION; NONHUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; T LYMPHOCYTE; VIRUS REPLICATION; ANTAGONISTS AND INHIBITORS; BINDING COMPETITION; CELL MOTION; CELL SURVIVAL; CHEMISTRY; COMPARATIVE STUDY; DRUG EFFECTS; JURKAT CELL LINE; METABOLISM; TUMOR CELL LINE;

AMINOPYRIDINES; ANTI-HIV AGENTS; BENZYLAMINES; BINDING, COMPETITIVE; CALCIUM SIGNALING; CELL LINE, TUMOR; CELL MOVEMENT; CELL SURVIVAL; CHEMOKINE CXCL12; HETEROCYCLIC COMPOUNDS; HUMANS; JURKAT CELLS; PROTEIN BINDING; PYRIDINES; RECEPTORS, CXCR4;

EID: 85017506755     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0176057     Document Type: Article

References (41)

1. Bachelerie F, Ben-Baruch A, Burkhardt AM, Combadiere C, Farber JM, Graham GJ, et al. International Union of Basic and Clinical Pharmacology. [corrected]. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev. 2014; 66: 1-79. https://doi.org/10.1124/pr.113.007724 PMID: 24218476
2. Raman D, Sobolik-Delmaire T, Richmond A. Chemokines in health and disease. Exp Cell Res. 2011; 317: 575-589. https://doi.org/10.1016/j.yexcr.2011.01.005 PMID: 21223965
3. Vandercappellen J, Van Damme J, Struyf S. The role of CXC chemokines and their receptors in cancer. Cancer Lett. 2008; 267: 226-244. https://doi.org/10.1016/j.canlet.2008.04.050 PMID: 18579287
4. Balkwill F. The significance of cancer cell expression of the chemokine receptor CXCR4. Semin Cancer Biol. 2004; 14: 171-179. https://doi.org/10.1016/j.semcancer.2003.10.003 PMID: 15246052
5. Busillo JM, Benovic JL. Regulation of CXCR4 signaling. Biochim Biophys Acta. 2007; 1768: 952-963. https://doi.org/10.1016/j.bbamem.2006.11.002 PMID: 17169327
6. Bleul CC, Farzan M, Choe H, Parolin C, Clark-Lewis I, Sodroski J, et al. The lymphocyte chemoattractant SDF-1 is a ligand for LESTR/fusin and blocks HIV-1 entry. Nature. 1996; 382: 829-833. https://doi. org/10.1038/382829a0 PMID: 8752280
7. Deng H, Liu R, Ellmeier W, Choe S, Unutmaz D, Burkhart M, et al. Identification of a major co-receptor for primary isolates of HIV-1. Nature. 1996; 381: 661-666. https://doi.org/10.1038/381661a0 PMID: 8649511
8. Domanska UM, Kruizinga RC, Nagengast WB, Timmer-Bosscha H, Huls G, de Vries EG, et al. A review on CXCR4/CXCL12 axis in oncology: no place to hide. Eur J Cancer. 2013; 49: 219-230. https://doi. org/10.1016/j.ejca.2012.05.005 PMID: 22683307
9. Hernandez PA, Gorlin RJ, Lukens JN, Taniuchi S, Bohinjec J, Francois F, et al. Mutations in the chemokine receptor gene CXCR4 are associated with WHIM syndrome, a combined immunodeficiency disease. Nat Genet. 2003; 34: 70-74. https://doi.org/10.1038/ng1149 PMID: 12692554
10. Nanki T, Hayashida K, El-Gabalawy HS, Suson S, Shi K, Girschick HJ, et al. Stromal cell-derived factor-1-CXC chemokine receptor 4 interactions play a central role in CD4+ T cell accumulation in rheumatoid arthritis synovium. J Immunol. 2000; 165: 6590-6598. PMID: 11086103
11. Flomenberg N, DiPersio J, Calandra G. Role of CXCR4 chemokine receptor blockade using AMD3100 for mobilization of autologous hematopoietic progenitor cells. Acta Haematol. 2005; 114: 198-205. https://doi.org/10.1159/000088410 PMID: 16269859
12. Schols D, Struyf S, Van Damme J, Este JA, Henson G, De Clercq E. Inhibition of T-tropic HIV strains by selective antagonization of the chemokine receptor CXCR4. J Exp Med. 1997; 186: 1383-1388. PMID: 9334378
13. Debnath B, Xu S, Grande F, Garofalo A, Neamati N. Small molecule inhibitors of CXCR4. Theranostics. 2013; 3: 47-75. https://doi.org/10.7150/thno.5376 PMID: 23382786
14. Zhang H, Kang D, Huang B, Liu N, Zhao F, Zhan P, et al. Discovery of non-peptide small molecular CXCR4 antagonists as anti-HIV agents: Recent advances and future opportunities. Eur J Med Chem. 2016; 114: 65-78. https://doi.org/10.1016/j.ejmech.2016.02.051 PMID: 26974376
15. Murakami T, Nakajima T, Koyanagi Y, Tachibana K, Fujii N, Tamamura H, et al. A small molecule CXCR4 inhibitor that blocks T cell line-tropic HIV-1 infection. J Exp Med. 1997; 186: 1389-1393. PMID: 9334379
16. Tamamura H, Xu Y, Hattori T, Zhang X, Arakaki R, Kanbara K, et al. A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140. Biochem Biophys Res Commun. 1998; 253: 877-882. https://doi.org/10.1006/bbrc.1998.9871 PMID: 9918823
17. Tamamura H, Omagari A, Hiramatsu K, Gotoh K, Kanamoto T, Xu Y, et al. Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001; 11: 1897-1902. PMID: 11459656
18. Faber A, Roderburg C, Wein F, Saffrich R, Seckinger A, Horsch K, et al. The many facets of SDF-1alpha, CXCR4 agonists and antagonists on hematopoietic progenitor cells. J Biomed Biotechnol. 2007; 2007: 26065. https://doi.org/10.1155/2007/26065 PMID: 17541466
19. Hatse S, Princen K, De Clercq E, Rosenkilde MM, Schwartz TW, Hernandez-Abad PE, et al. AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor. Biochem Pharmacol. 2005; 70: 752-761. https://doi.org/10.1016/j.bcp.2005.05.035 PMID: 16011832
20. Stone ND, Dunaway SB, Flexner C, Tierney C, Calandra GB, Becker S, et al. Multiple-dose escalation study of the safety, pharmacokinetics, and biologic activity of oral AMD070, a selective CXCR4 receptor inhibitor, in human subjects. Antimicrob Agents Chemother. 2007; 51: 2351-2358. https://doi.org/10. 1128/AAC.00013-07 PMID: 17452489
21. Thoma G, Streiff MB, Kovarik J, Glickman F, Wagner T, Beerli C, et al. Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo. J Med Chem. 2008; 51: 7915-7920. https://doi.org/10.1021/jm801065q PMID: 19053768
22. Zhan W, Liang Z, Zhu A, Kurtkaya S, Shim H, Snyder JP, et al. Discovery of small molecule CXCR4 antagonists. J Med Chem. 2007; 50: 5655-5664. https://doi.org/10.1021/jm070679i PMID: 17958344
23. Zhang J, Ren X, Shi W, Wang S, Chen H, Zhang B, et al. Small molecule Me6TREN mobilizes hematopoietic stem/progenitor cells by activating MMP-9 expression and disrupting SDF-1/CXCR4 axis. Blood. 2014; 123: 428-441. https://doi.org/10.1182/blood-2013-04-498535 PMID: 24196072
24. Pandey MK, Kale VP, Song C, Sung SS, Sharma AK, Talamo G, et al. Gambogic acid inhibits multiple myeloma mediated osteoclastogenesis through suppression of chemokine receptor CXCR4 signaling pathways. Exp Hematol. 2014; 42: 883-896. https://doi.org/10.1016/j.exphem.2014.07.261 PMID: 25034231
25. Princen K, Hatse S, Vermeire K, De Clercq E, Schols D. Establishment of a novel CCR5 and CXCR4 expressing CD4+ cell line which is highly sensitive to HIV and suitable for high-throughput evaluation of CCR5 and CXCR4 antagonists. Retrovirology. 2004; 1: 2. https://doi.org/10.1186/1742-4690-1-2 PMID: 15169555
26. Hatse S, Princen K, Liekens S, Vermeire K, De Clercq E, Schols D. Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studies. Cytometry A. 2004; 61: 178-188. PMID: 15382150
27. Vermeire K, Princen K, Hatse S, De Clercq E, Dey K, Bell TW, et al. CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro. AIDS. 2004; 18: 2115-2125. PMID: 15577644
28. Mosi RM, Anastassova V, Cox J, Darkes MC, Idzan SR, Labrecque J, et al. The molecular pharmacology of AMD11070: an orally bioavailable CXCR4 HIV entry inhibitor. Biochem Pharmacol. 2012; 83: 472-479. https://doi.org/10.1016/j.bcp.2011.11.020 PMID: 22146583
29. Gravel S, Malouf C, Boulais PE, Berchiche YA, Oishi S, Fujii N, et al. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem. 2010; 285: 37939-37943. https://doi.org/10.1074/jbc.C110.147470 PMID: 20956518
30. Boerrigter G, Lark MW, Whalen EJ, Soergel DG, Violin JD, Burnett JC Jr. Cardiorenal actions of TRV120027, a novel ss-arrestin-biased ligand at the angiotensin II type I receptor, in healthy and heart failure canines: a novel therapeutic strategy for acute heart failure. Circ Heart Fail. 2011; 4: 770-778. https://doi.org/10.1161/CIRCHEARTFAILURE.111.962571 PMID: 21835984
31. Magnan R, Escrieut C, Gigoux V, De K, Clerc P, Niu F, et al. Distinct CCK-2 receptor conformations associated with beta-arrestin-2 recruitment or phospholipase-C activation revealed by a biased antagonist. J Am Chem Soc. 2013; 135: 2560-2573. https://doi.org/10.1021/ja308784w PMID: 23323542
32. Violin JD, Crombie AL, Soergel DG, Lark MW. Biased ligands at G-protein-coupled receptors: promise and progress. Trends Pharmacol Sci. 2014; 35: 308-316. https://doi.org/10.1016/j.tips.2014.04.007 PMID: 24878326
33. Drenckhan A, Kurschat N, Dohrmann T, Raabe N, Koenig AM, Reichelt U, et al. Effective inhibition of metastases and primary tumor growth with CTCE-9908 in esophageal cancer. J Surg Res. 2013; 182: 250-256. https://doi.org/10.1016/j.jss.2012.09.035 PMID: 23117118
34. Kim SY, Lee CH, Midura BV, Yeung C, Mendoza A, Hong SH, et al. Inhibition of the CXCR4/CXCL12 chemokine pathway reduces the development of murine pulmonary metastases. Clin Exp Metastasis. 2008; 25: 201-211. https://doi.org/10.1007/s10585-007-9133-3 PMID: 18071913
35. Porvasnik S, Sakamoto N, Kusmartsev S, Eruslanov E, Kim WJ, Cao W, et al. Effects of CXCR4 antagonist CTCE-9908 on prostate tumor growth. Prostate. 2009; 69: 1460-1469. https://doi.org/10.1002/ pros.21008 PMID: 19588526
36. Richert MM, Vaidya KS, Mills CN, Wong D, Korz W, Hurst DR, et al. Inhibition of CXCR4 by CTCE-9908 inhibits breast cancer metastasis to lung and bone. Oncol Rep. 2009; 21: 761-767. PMID: 19212637
37. Kawatkar SP, Yan M, Gevariya H, Lim MY, Eisold S, Zhu X, et al. Computational analysis of the structural mechanism of inhibition of chemokine receptor CXCR4 by small molecule antagonists. Exp Biol Med (Maywood). 2011; 236: 844-850.
38. Jung SH, Won KJ, Lee KP, Lee DH, Yu S, Lee DY, et al. DJ-1 protein regulates CD3+ T cell migration via overexpression of CXCR4 receptor. Atherosclerosis. 2014; 235: 503-509. https://doi.org/10.1016/j. atherosclerosis.2014.05.955 PMID: 24953490
39. De Clercq E, Yamamoto N, Pauwels R, Balzarini J, Witvrouw M, De Vreese K, et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob Agents Chemother. 1994; 38: 668-674. PMID: 7913308
40. Juarez J, Bradstock KF, Gottlieb DJ, Bendall LJ. Effects of inhibitors of the chemokine receptor CXCR4 on acute lymphoblastic leukemia cells in vitro. Leukemia. 2003; 17: 1294-1300. PMID: 12835717
41. Wu B, Chien EY, Mol CD, Fenalti G, Liu W, Katritch V, et al. Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists. Science. 2010; 330: 1066-1071. https://doi.org/10. 1126/science.1194396 PMID: 20929726