Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors

Ashraf Brik, John Muldoon, Ying Chuan Lin, John H. Elder, David S. Goodsell, Arthur J. Olson, Valery V. Fokin, K. Bary Sharpless, Chi Huey Wong

Research output: Contribution to journal › Article

136 Citations (Scopus)

Abstract

Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.

Original languageEnglish
Pages (from-to)1246-1248
Number of pages3
JournalChemBioChem
Volume4
Issue number11
DOIs
Publication statusPublished - 7 Nov 2003
Externally publishedYes

Fingerprint

HIV Protease Inhibitors
Triazoles
Screening
Click Chemistry
HIV Protease
Pharmaceutical Preparations

Keywords

  • Click chemistry
  • Enzyme
  • HIV protease
  • Inhibitors
  • Screening

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Biochemistry, Genetics and Molecular Biology(all)

Cite this

Brik, A., Muldoon, J., Lin, Y. C., Elder, J. H., Goodsell, D. S., Olson, A. J., ... Wong, C. H. (2003). Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors. ChemBioChem, 4(11), 1246-1248. https://doi.org/10.1002/cbic.200300724

Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors. / Brik, Ashraf; Muldoon, John; Lin, Ying Chuan; Elder, John H.; Goodsell, David S.; Olson, Arthur J.; Fokin, Valery V.; Sharpless, K. Bary; Wong, Chi Huey.

In: ChemBioChem, Vol. 4, No. 11, 07.11.2003, p. 1246-1248.

Research output: Contribution to journal › Article

Brik, A, Muldoon, J, Lin, YC, Elder, JH, Goodsell, DS, Olson, AJ, Fokin, VV, Sharpless, KB & Wong, CH 2003, 'Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors', ChemBioChem, vol. 4, no. 11, pp. 1246-1248. https://doi.org/10.1002/cbic.200300724
Brik A, Muldoon J, Lin YC, Elder JH, Goodsell DS, Olson AJ et al. Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors. ChemBioChem. 2003 Nov 7;4(11):1246-1248. https://doi.org/10.1002/cbic.200300724
Brik, Ashraf ; Muldoon, John ; Lin, Ying Chuan ; Elder, John H. ; Goodsell, David S. ; Olson, Arthur J. ; Fokin, Valery V. ; Sharpless, K. Bary ; Wong, Chi Huey. / Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors. In: ChemBioChem. 2003 ; Vol. 4, No. 11. pp. 1246-1248.
@article{a0b332c31a2c4a76aae9366091e32cb3,
title = "Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors",
abstract = "Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.",
keywords = "Click chemistry, Enzyme, HIV protease, Inhibitors, Screening",
author = "Ashraf Brik and John Muldoon and Lin, {Ying Chuan} and Elder, {John H.} and Goodsell, {David S.} and Olson, {Arthur J.} and Fokin, {Valery V.} and Sharpless, {K. Bary} and Wong, {Chi Huey}",
year = "2003",
month = "11",
day = "7",
doi = "10.1002/cbic.200300724",
language = "English",
volume = "4",
pages = "1246--1248",
journal = "ChemBioChem",
issn = "1439-4227",
publisher = "Wiley-VCH Verlag",
number = "11",

}

TY - JOUR

T1 - Rapid Diversity-Oriented Synthesis in Microtiter Plates for in Situ Screening of HIV Protease Inhibitors

AU - Brik, Ashraf

AU - Muldoon, John

AU - Lin, Ying Chuan

AU - Elder, John H.

AU - Goodsell, David S.

AU - Olson, Arthur J.

AU - Fokin, Valery V.

AU - Sharpless, K. Bary

AU - Wong, Chi Huey

PY - 2003/11/7

Y1 - 2003/11/7

N2 - Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.

AB - Click and go: By using click chemistry based on a new triazole forming reaction condition (see scheme), over 100 triazole compounds generated in microtiter plates from a core structure were screened for HIV protease inhibition in situ without product isolation. Potent inhibitors, active at nanomolar concentrations, against the wild type and drug resistant mutants were identified.

KW - Click chemistry

KW - Enzyme

KW - HIV protease

KW - Inhibitors

KW - Screening

UR - http://www.scopus.com/inward/record.url?scp=0345306644&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0345306644&partnerID=8YFLogxK

U2 - 10.1002/cbic.200300724

DO - 10.1002/cbic.200300724

M3 - Article

VL - 4

SP - 1246

EP - 1248

JO - ChemBioChem

JF - ChemBioChem

SN - 1439-4227

IS - 11

ER -

Access to Document