Inhibitors of HIV-1 protease by using in situ click chemistry

Matthew Whiting, John Muldoon, Ying Chuan Lin, Steven M. Silverman, William Lindstrom, Arthur J. Olson, Hartmuth C. Kolb, M. G. Finn, K. Barry Sharpless, John H. Elder, Valery V. Fokin

Research output: Contribution to journalArticle

393 Citations (Scopus)

Abstract

(Chemical Equation Presented) Twice poor equals potent: HIV-1 Protease assembles its own potent inhibitor through formation of the triazole linkage from azide- and alkyne-containing fragments that are themselves poor binders.

Original languageEnglish
Pages (from-to)1435-1439
Number of pages5
JournalAngewandte Chemie - International Edition
Volume45
Issue number9
DOIs
Publication statusPublished - 20 Feb 2006
Externally publishedYes

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Triazoles
Alkynes
Azides
Binders
Human immunodeficiency virus 1 p16 protease
Peptide Hydrolases

Keywords

  • Click chemistry
  • Drug design
  • HIV-1 protease
  • Inhibitors
  • Triazoles

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Whiting, M., Muldoon, J., Lin, Y. C., Silverman, S. M., Lindstrom, W., Olson, A. J., ... Fokin, V. V. (2006). Inhibitors of HIV-1 protease by using in situ click chemistry. Angewandte Chemie - International Edition, 45(9), 1435-1439. https://doi.org/10.1002/anie.200502161

Inhibitors of HIV-1 protease by using in situ click chemistry. / Whiting, Matthew; Muldoon, John; Lin, Ying Chuan; Silverman, Steven M.; Lindstrom, William; Olson, Arthur J.; Kolb, Hartmuth C.; Finn, M. G.; Sharpless, K. Barry; Elder, John H.; Fokin, Valery V.

In: Angewandte Chemie - International Edition, Vol. 45, No. 9, 20.02.2006, p. 1435-1439.

Research output: Contribution to journalArticle

Whiting, M, Muldoon, J, Lin, YC, Silverman, SM, Lindstrom, W, Olson, AJ, Kolb, HC, Finn, MG, Sharpless, KB, Elder, JH & Fokin, VV 2006, 'Inhibitors of HIV-1 protease by using in situ click chemistry', Angewandte Chemie - International Edition, vol. 45, no. 9, pp. 1435-1439. https://doi.org/10.1002/anie.200502161
Whiting M, Muldoon J, Lin YC, Silverman SM, Lindstrom W, Olson AJ et al. Inhibitors of HIV-1 protease by using in situ click chemistry. Angewandte Chemie - International Edition. 2006 Feb 20;45(9):1435-1439. https://doi.org/10.1002/anie.200502161
Whiting, Matthew ; Muldoon, John ; Lin, Ying Chuan ; Silverman, Steven M. ; Lindstrom, William ; Olson, Arthur J. ; Kolb, Hartmuth C. ; Finn, M. G. ; Sharpless, K. Barry ; Elder, John H. ; Fokin, Valery V. / Inhibitors of HIV-1 protease by using in situ click chemistry. In: Angewandte Chemie - International Edition. 2006 ; Vol. 45, No. 9. pp. 1435-1439.
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