Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.
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.
Daelemans
D
D
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Belgium. Dirk.Daelemans@uz.kuleuven.ac.be
Vandamme
A M
AM
Shuto
S
S
Matsuda
A
A
De Clercq
E
E
D000241:Adenosine / Q000031:analogs & derivatives / Q000494:pharmacology; D043383:Adenosylhomocysteinase; D019380:Anti-HIV Agents / Q000737:chemistry*; D000903:Antibiotics, Antineoplastic / Q000737:chemistry*; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006867:Hydrolases / Q000037:antagonists & inhibitors*; D008968:Molecular Conformation; D015394:Molecular Structure; D015533:Transcriptional Activation / Q000187:drug effects
D019380:Anti-HIV Agents; D000903:Antibiotics, Antineoplastic; D004791:Enzyme Inhibitors; C031098:neplanocin C; D006867:Hydrolases; D043383:Adenosylhomocysteinase; D000241:Adenosine