Rational Design of Peptide-Based HIV Proteinase Inhibitors

A. Roberts, Noel; A. Martin, Joseph; Kinchington, Derek; V. Broadhurst, Anne; Craig, Jane; B. R. Duncan, I.; Galpin, S.; Handa, B.K.; Kay, John; Kröhn, Antonin; Lambert, Robert; H. Merrett, John; Mills, John; E. B. PARKES, K.; Redshaw, Sally; J. Ritchie, Alison; L. Taylor, Debra; J. Thomas, Gareth; J. Machin, Peter

doi:10.1126/science.2183354

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Rational Design of Peptide-Based HIV Proteinase Inhibitors

Published in Science • Apr 20, 1990

Authors:

Noel A. Roberts

Joseph A. Martin

Derek Kinchington

Abstract

A series of peptide derivatives based on the transition-state mimetic concept has been designed that inhibit the proteinase from the human immunodeficiency virus (HIV). The more active compounds inhibit both HIV-1 and HIV-2 proteinases in the nanomolar range with little effect at 10 micromolar again...

Subject

Peptide

Syncytium

Cytotoxicity

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