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

doi:10.1002/cbic.200300724

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 › peer-review

161 Scopus citations

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 language	English
Pages (from-to)	1246-1248
Number of pages	3
Journal	ChemBioChem
Volume	4
Issue number	11
DOIs	https://doi.org/10.1002/cbic.200300724
State	Published - 7 Nov 2003
Externally published	Yes

Keywords

Click chemistry
Enzyme
HIV protease
Inhibitors
Screening

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Organic Chemistry

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/cbic.200300724

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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 = nov,

day = "7",

doi = "10.1002/cbic.200300724",

language = "English",

volume = "4",

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issn = "1439-4227",

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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 - https://www.scopus.com/pages/publications/0345306644

U2 - 10.1002/cbic.200300724

DO - 10.1002/cbic.200300724

M3 - Article

C2 - 14613121

AN - SCOPUS:0345306644

SN - 1439-4227

VL - 4

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JO - ChemBioChem

JF - ChemBioChem

IS - 11

ER -

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

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

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