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Anti-HIV-1 activity of chemically modified heparins: correlation between binding to the V3 loop of gp120 and inhibition of cellular HIV-1 infection in vitro.
- Source :
-
Biochemistry [Biochemistry] 1994 Jun 07; Vol. 33 (22), pp. 6974-80. - Publication Year :
- 1994
-
Abstract
- Chemically modified heparins were tested for their activities in (i) inhibiting HIV-1 replication in vitro and (ii) inhibiting the binding to recombinant HIV-1 gp120 of monoclonal antibodies specific for the V3 loop. The results reveal that N-desulfation reduces activity, although this is largely restored on N-acetylation. Selective O-desulfation also markedly reduces activity, whereas carboxyl reduction has little effect. Overall these results show that the anti-HIV-1 activity of heparin does not depend simply on negative density, and indicate instead that particular structures, notably O-sulfates, are involved. Our studies reveal that for chemically modified heparins and heparin-derived fragments there is a striking correlation between anti-HIV-1 activity in vitro and binding to the V3 loop of gp120 in solid phase ELISA. This strongly suggests that the heparin exerts its anti-HIV-1 activity by binding to the V3 loop of gp120.
- Subjects :
- Acetylation
Amino Acid Sequence
Animals
Antiviral Agents metabolism
CD4-Positive T-Lymphocytes microbiology
Cattle
Enzyme-Linked Immunosorbent Assay
Heparin metabolism
Heparin pharmacology
Humans
Magnetic Resonance Spectroscopy
Molecular Sequence Data
Protein Binding
Structure-Activity Relationship
Sulfates
Swine
Antiviral Agents pharmacology
HIV Envelope Protein gp120 metabolism
HIV-1 drug effects
Heparin analogs & derivatives
Peptide Fragments metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0006-2960
- Volume :
- 33
- Issue :
- 22
- Database :
- MEDLINE
- Journal :
- Biochemistry
- Publication Type :
- Academic Journal
- Accession number :
- 7911328
- Full Text :
- https://doi.org/10.1021/bi00188a029