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

被引：242

作者：

DECLERCO, E

YAMAMOTO, N

PAUWELS, R

BABA, M

SCHOLS, D

NAKASHIMA, H

BALZARINI, J

DEBYSER, Z

MURRER, BA

SCHWARTZ, D

THORNTON, D

BRIDGER, G

FRICKER, S

HENSON, G

ABRAMS, M

PICKER, D

机构：

[1] JOHNSON MATTHEY TECHNOL CTR, READING RG4 9NH, ENGLAND

[2] JOHNSON MATTHEY PHARMACEUT RES, W CHESTER, PA 19380 USA

来源：

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1992年 / 89卷 / 12期

关键词：

D O I：

10.1073/pnas.89.12.5286

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

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-mu-M, 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.

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页码：5286 / 5290

页数：5

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