Design and synthesis of new fluorogenic HIV protease substrates based on resonance energy transfer

✍ Scribed by Gary T. Wang; Edmund Matayoshi; H. Jan Huffaker; Grant A. Krafft

• Book ID: 104228393
• Publisher: Elsevier Science
• Year: 1990
• Tongue: French
• Weight: 344 KB
• Volume: 31
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)97099-0

✦ Synopsis

The design and synthesis of new fluceogenic substrate probes for HIV pmtease based on resonance energy transfer are described. These substrates permit sensitive, continuous meas urement of HIV proteam activity. Specially tailoml aganic pmbe n&cules ate playing an in creasingly signifkant role in efforts to elucidate important aspects of biological macromolecules. When coupled with spectroscopic techniqueq probe molecules provide functional and mechanistic information on hey enzymes, receptors, and structural proteins. Our recent interests have centemd on the design of specific substrate probes fa the human immunodeficiency virus (HIV) associated protease enzyme, now an important target for AIDS therapy.1 Recently, we described a rapid and continuous assay for tettoviral protease activity (including HIv) based on new fl~orogeni~ SU~~WC proti*3 and in this report, we describe molecular design considerations, synthesis and purification aspects of these new substrates.