HIV cell fusion assay: Phenotypic screening tool for the identification of HIV entry inhibitors via CXCR4

Journal of Biomolecular Screening

Volumn 19, Issue 1, 2014, Pages 108-118

  Smith, Elizabeth B ^a   Ogert, Robert A ^a   Pechter, David ^a   Villafania, Artjohn ^a   Abbondanzo, Susan J ^a   Lin, Karen ^a   Rivera Gines, Aida ^a   Rebsch Mastykarz, Cheryl ^a   Monsma, Frederick J ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

CXCR4; GPCR allosteric modulator; HIV cell fusion assay; phenotypic screening

Indexed keywords

BETA LACTAMASE; CD4 ANTIGEN; CHEMOKINE RECEPTOR CCR5; CHEMOKINE RECEPTOR CXCR4; ETOPOSIDE; GLYCOPROTEIN GP 120; HUMAN IMMUNODEFICIENCY VIRUS FUSION INHIBITOR; TRANSCRIPTION FACTOR GAL4;

ARTICLE; CELL FUSION; CELL STRUCTURE; CONTROLLED STUDY; CYTOMETRY; ENZYME ACTIVITY; FEMALE; FLUORESCENCE RESONANCE ENERGY TRANSFER; GENE REARRANGEMENT; HELA CELL; HOST CELL; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS; LASER; NONHUMAN; PHENOTYPE; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN EXPRESSION; VIRUS ENTRY; VIRUS IDENTIFICATION;

CXCR4; GPCR ALLOSTERIC MODULATOR; HIV CELL FUSION ASSAY; PHENOTYPIC SCREENING;

CELL LINE; GENE EXPRESSION; GENES, REPORTER; HIGH-THROUGHPUT SCREENING ASSAYS; HIV FUSION INHIBITORS; HUMANS; MICROBIAL SENSITIVITY TESTS; PHENOTYPE; RECEPTORS, CXCR4; RECOMBINANT FUSION PROTEINS; REPRODUCIBILITY OF RESULTS; VIRUS INTERNALIZATION;

EID: 84890822603     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057113500074     Document Type: Article

References (28)

1. Elzi L., Marzolini C., Furrer H., et al. Treatment Modification in Human Immunodeficiency Virus-Infected Individuals Starting Combination Antiretroviral Therapy between 2005 and 2008. Arch. Intern. Med. 2010 ; 170: 57-65
2. Choe H., Farzan M., Sun Y., et al. The β-Chemokine Receptors CCR3 and CCR5 Facilitate Infection by Primary HIV-1 Isolates. Cell. 1996 ; 85: 1135-1148
3. Deng H., Liu R., Ellmeier W., et al. Identification of a Major Co-receptor for Primary Isolates of HIV-1. Nature. 1996 ; 381: 661-666
4. Feng Y., Broder C. C., Kennedy P. E., et al. HIV-1 Entry Cofactor: Functional cDNA Cloning of a Seven-Transmembrane, G Protein-Coupled Receptor. Science. 1996 ; 272: 872-877
5. Pancera M., Majeed S., Ban Y.-E. A., et al. Structure of HIV-1 gp120 with gp41-Interactive Region Reveals Layered Envelope Architecture and Basis of Conformational Mobility. Proc. Natl. Acad. Sci. U. S. A. 2010 ; 107: 1166-1171
6. Liu R., Paxton W. A., Choe S., et al. Homozygous Defect in HIV-1 Coreceptor Accounts for Resistance of Some Multiply-Exposed Individuals to HIV-1 Infection. Cell. 1996 ; 86: 367-377
7. Nguyen G. T., Carrington M., Beeler J. A., et al. Phenotypic Expressions of CCR5-delta32/delta32 Homozygosity. J. AIDS. 1999 ; 22: 75-82
8. Muniz-Medina V. M., Jones S., Maglich J. M., et al. The Relative Activity of a Function Sparing HIV-1 Entry Inhibitors on Viral Entry and CCR5 Internalization: Is Allosteric Functional Selectivity a Valuable Therapeutic Property?. Mol. Pharmacol. 2009 ; 75: 490-501
9. Strizki J. M., Xu S., Wagner N. E., et al. SCH-C (SCH 351125), an Orally Bioavailable, Small Molecule Antagonist of the Chemokine Receptor CCR5, Is a Potent Inhibitor of HIV-1 Infection In Vitro and In Vivo. Proc. Natl. Acad. Sci. U. S. A. 2001 ; 98: 12718-12723
10. Dorr P., Westby M., Dobbs S., et al. Maraviroc (UK-427,857), a Potent, Orally Bioavailable, and Selective Small-Molecule Inhibitor of Chemokine Receptor CCR5 with Broad-Spectrum Anti-Human Immunodeficiency Virus Type 1 Activity. Antimicrob. Agents Chemother. 2005 ; 49: 4721-4732
11. Gulick R. M., Lalezari J., Goodrich J., et al. Maraviroc for Previously Treated Patients with R5 HIV-1 Infection. N. Engl. J. Med. 2008 ; 359: 1429-1441
12. De Clercq E., Yamamoto N., Pauwels R., et al. Potent and Selective Inhibition of Human Immunodeficiency Virus (HIV)-1 and HIV-2 Replication by a Class of Bicyclams Interacting with a Viral Uncoating Event. Proc. Natl. Acad. Sci. U. S. A. 1992 ; 89: 5286-5290
13. Donzella G. A., Schols D., Lin S. W., et al. AMD3100, a Small Molecule Inhibitor of HIV-1 Entry via the CXCR4 Co-receptor. Nat. Med. 1998 ; 4: 72-77
14. Bleul C. C., Farzan M., Choe H., et al. The Lymphocyte Chemoattractant SDF-1 Is a Ligand for LESTR/Fusin and Blocks HIV-1 Entry. Nature. 1996 ; 382: 829-833
15. Nussbaum O., Broder C. C., Berger E. A.. Fusogenic Mechanisms of Enveloped-Virus Glycoproteins Analyzed by a Novel Recombinant Vaccinia Virus-Based Assay Quantitating Cell Fusion-Dependent Reporter Gene Activation. J. Virol. 1994 ; 68: 5411-5422
16. Hong Y.-L., Wu L.-H., Cui M., et al. New Reporter Cell Lines to Study Macrophage-Tropic HIV Envelope Protein-Mediated Cell-Cell Fusion. AIDS Res. Hum. Retroviruses. 1999 ; 15: 1667-1672
17. Jenkinson S., Mc Coy D. C., Kerner S. A., et al. Development of a Novel High-Throughput Surrogate Assay to Measure HIV Envelope/CCR5/CD4-Mediated Viral/Cell Fusion Using BacMam Baculovirus Technology. J. Biomol. Screen. 2003 ; 8: 463-470
18. Lineberger J. E., Danzeisen R., Hazuda D. J., et al. Altering Expression Levels of Human Immunodeficiency Virus Type 1 gp120-gp41 Affects Efficiency but Not Kinetics of Cell-Cell Fusion. J. Virol. 2002 ; 76: 3522-3533
19. Zlokarnik G., Negulescu P. A., Knapp T. E., et al. Quantitation of Transcription and Clonal Selection of Single Living Cells with β-Lactamase as Reporter. Science. 1998 ; 279: 84-88
20. Coward P., Chan S. D. H., Wada H. G., et al. Chimeric G Proteins Allow a High-Throughput Signaling Assay of Gi-Coupled Receptors. Anal. Biochem. 1999 ; 270: 242-248
21. Zwier J. M., Roux T., Cottet M., et al. A Fluorescent Ligand-Binding Alternative Using Tag-lite® Technology. J. Biomol. Screen. 2010 ; 15: 1248-1259
22. Zhang J.-H., Chung T. D. Y., Oldenburg K. R.. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999 ; 4: 67-73
23. Hatse S., Princen K., Bridger G., et al. Chemokine Receptor Inhibition by AMD3100 Is Strictly Confined to CXCR4. FEBS Lett. 2002 ; 527: 255-262
24. Nagasawa T., Hirota S., Tachibana K., et al. Defects of B-Cell Lymphopoiesis and Bone-Marrow Myelopoiesis in Mice Lacking the CXC Chemokine PBSF/SDF-1. Nature. 1996 ; 382: 635-638
25. Tachibana K., Hirota S., Iizasa H., et al. The Chemokine Receptor CXCR4 Is Essential for Vascularization of the Gastrointestinal Tract. Nature. 1998 ; 393: 591-594
26. Zou Y.-R., Kottmann A. H., Kuroda M., et al. Function of the Chemokine Receptor CXCR4 in Haematopoiesis and in Cerebellar Development. Nature. 1998 ; 393: 595-599
27. Ma Q., Jones D., Borghesani P. R., et al. Impaired B-Lymphopoiesis, Myelopoiesis, and Derailed Cerebellar Neuron Migration in CXCR4- and SDF-1-Deficient Mice. Proc. Natl. Acad. Sci. U. S. A. 1998 ; 95: 9448-9453
28. Kucia M., Jankowski K., Reca R., et al. CXCR4-SDF-1 Signalling, Locomotion, Chemotaxis and Adhesion. J. Mol. Histol. 2004 ; 35: 233-245