Title: 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
Authors: De Clercq, Erik ×
Yamamoto, N
Pauwels, R
Baba, M
Schols, Dominique
Nakashima, H
Balzarini, Jan
Debyser, Zeger
Murrer, B A
Schwartz, D
Thornton, D
Bridger, G
Fricker, S
Henson, G
Abrams, M
Picker, D #
Issue Date: Jul-1992
Series Title: Proceedings of the National Academy of Sciences of the United States of America vol:89 issue:12 pages:5286-90
Abstract: A series of bicyclams have been shown to be potent and selective inhibitors of human immunodeficiency virus (HIV). The compounds are inhibitory to the replication of various HIV-1 and HIV-2 strains in various human T-cell systems, including peripheral blood lymphocytes, at 0.14-1.4 microM, without being toxic to the host cells at 2.2 mM. The bicyclam JM2763 is active against 3'-azido-3'-deoxythymidine (zidovudine; AZT)-resistant HIV-1 strains and acts additively with AZT. Mechanism of action studies revealed that the bicyclams (i.e., JM2763) interact with an early event of the retrovirus replicative cycle, which could be tentatively identified as a viral uncoating event.
ISSN: 0027-8424
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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