Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication

D Daelemans; A M Vandamme; S Shuto; A Matsuda; E De Clercq

doi:10.1080/07328319808005192

Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication

Nucleosides Nucleotides. 1998 Jan-Mar;17(1-3):479-86. doi: 10.1080/07328319808005192.

Authors

D Daelemans¹, A M Vandamme, S Shuto, A Matsuda, E De Clercq

Affiliation

¹ Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium. [email protected]

PMID: 9708357
DOI: 10.1080/07328319808005192

Abstract

The R- and S-isomers of 6'-C-neplanocin A analogues, which are all known as inhibitors of S-adenosylhomocysteine (AdoHcy) hydrolase, were studied for their inhibitory effects on Human Immunodeficiency Virus type 1 (HIV-1) replication and HIV-1 Tat-mediated transactivation. The R-isomers showed much greater activity against AdoHcy hydrolase than the S-isomers. The same differential activity was observed against the HIV-1 replication and the Tat transactivation.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adenosine / analogs & derivatives
Adenosine / pharmacology
Adenosylhomocysteinase
Anti-HIV Agents / chemistry*
Antibiotics, Antineoplastic / chemistry*
Cell Line
Enzyme Inhibitors / pharmacology*
Hydrolases / antagonists & inhibitors*
Molecular Conformation
Molecular Structure
Transcriptional Activation / drug effects

Substances

Anti-HIV Agents
Antibiotics, Antineoplastic
Enzyme Inhibitors
neplanocin C
Hydrolases
Adenosylhomocysteinase
Adenosine