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Titolo:
PROBLEMS AND PERSPECTIVES IN THE DESIGN OF ANTI-HIV-1 AGENTS
Autore:
MOHAN P;
Indirizzi:
UNIV ILLINOIS,COLL PHARM,DEPT MED CHEM & PHARMACOGNOSY M-C 781,BOX 6998 CHICAGO IL 60680
Titolo Testata:
Drug development research
fascicolo: 1, volume: 29, anno: 1993,
pagine: 1 - 17
SICI:
0272-4391(1993)29:1<1:PAPITD>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN-IMMUNODEFICIENCY-VIRUS; REVERSE-TRANSCRIPTASE INHIBITORS; INDUCED SYNCYTIUM FORMATION; RECOMBINANT SOLUBLE CD4; GIANT-CELL FORMATION; AIDS-RELATED COMPLEX; DEXTRAN SULFATE; HIV REPLICATION; ACID-DERIVATIVES; ANTIRETROVIRUS ACTIVITY;
Keywords:
HIV; ENZYME INHIBITORS AND DERIVATIVES; VIRAL BINDING;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
160
Recensione:
Indirizzi per estratti:
Citazione:
P. Mohan, "PROBLEMS AND PERSPECTIVES IN THE DESIGN OF ANTI-HIV-1 AGENTS", Drug development research, 29(1), 1993, pp. 1-17

Abstract

The human immunodeficiency virus (HIV) that produces the acquired immune deficiency syndrome (AIDS) continues to evade all strategies for potential therapeutic intervention. Global efforts in the search for potential anti-HIV-1 agents have mainly centered around the design of enzyme inhibitors and derivatives that inhibit viral binding or gene expression. Both nucleoside and non-nucleoside reverse transcriptase inhibitors have demonstrated potent anti-HIV-1 activity. However, toxicityconsiderations and the emergence of resistant strains will require further structural manipulations to diminish these undesirable properties. Protease inhibitors also exhibit activities at nanomolar concentrations, but many of these agents may suffer from problems of absorption and biodegradation. These apparent shortcomings have been circumventedby the preparation of peptidomimetic molecules. Similarly, smaller CD4 mimetics have emerged as alternatives to the larger soluble CD4 derivatives as inhibitors of viral binding. Other viral binding inhibitors, the anionic molecules, suffer from an inherent inability to enter cells and potential anticoagulant activity. These properties may be remedied by rational analog design and synthesis. Oligonucleotides can be constructed to inhibit specific segments of selected regulatory genes of the virus. These agents have been critiqued on the basis of stability, cellular uptake, and assurance of hybridization. Once again, structure activity relationship studies have revealed that many of these apparent problems can be overcome. The more recently discovered agents belong to the unique classes of tat antagonists or viral uncoating inhibitors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/11/20 alle ore 07:14:36