Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates

Fu Sen Liang; Ashraf Brik; Ying Chuan Lin; John H. Elder; Chi Huey Wong

doi:10.1016/j.bmc.2005.09.026

Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates

Fu Sen Liang, Ashraf Brik, Ying Chuan Lin, John H. Elder, Chi Huey Wong

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Abstract

A method utilizing the strategy of epoxide opening by amine with water as co-solvent and screening in situ was developed for rapid discovery of protein inhibitors. Using this approach, HIV protease inhibitors with novel P1′ residues were identified in our study. This strategy should be applicable for the efficient assembly of diverse compound collections for inhibitors' discovery and optimization in other systems.

Original language	English
Pages (from-to)	1058-1062
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry
Volume	14
Issue number	4
DOIs	https://doi.org/10.1016/j.bmc.2005.09.026
State	Published - 15 Feb 2006
Externally published	Yes

Keywords

Epoxide opening
HIV protease inhibitors
In situ screening
In water

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

UN SDGs

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

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10.1016/j.bmc.2005.09.026

Cite this

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title = "Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates",

abstract = "A method utilizing the strategy of epoxide opening by amine with water as co-solvent and screening in situ was developed for rapid discovery of protein inhibitors. Using this approach, HIV protease inhibitors with novel P1′ residues were identified in our study. This strategy should be applicable for the efficient assembly of diverse compound collections for inhibitors' discovery and optimization in other systems.",

keywords = "Epoxide opening, HIV protease inhibitors, In situ screening, In water",

author = "Liang, {Fu Sen} and Ashraf Brik and Lin, {Ying Chuan} and Elder, {John H.} and Wong, {Chi Huey}",

note = "Funding Information: We thank the National Institutes of Health and The Skaggs Institute for Chemical Biology for financial support.",

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T1 - Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates

AU - Liang, Fu Sen

AU - Brik, Ashraf

AU - Lin, Ying Chuan

AU - Elder, John H.

AU - Wong, Chi Huey

N1 - Funding Information: We thank the National Institutes of Health and The Skaggs Institute for Chemical Biology for financial support.

PY - 2006/2/15

Y1 - 2006/2/15

N2 - A method utilizing the strategy of epoxide opening by amine with water as co-solvent and screening in situ was developed for rapid discovery of protein inhibitors. Using this approach, HIV protease inhibitors with novel P1′ residues were identified in our study. This strategy should be applicable for the efficient assembly of diverse compound collections for inhibitors' discovery and optimization in other systems.

AB - A method utilizing the strategy of epoxide opening by amine with water as co-solvent and screening in situ was developed for rapid discovery of protein inhibitors. Using this approach, HIV protease inhibitors with novel P1′ residues were identified in our study. This strategy should be applicable for the efficient assembly of diverse compound collections for inhibitors' discovery and optimization in other systems.

KW - Epoxide opening

KW - HIV protease inhibitors

KW - In situ screening

KW - In water

UR - http://www.scopus.com/inward/record.url?scp=30344449178&partnerID=8YFLogxK

U2 - 10.1016/j.bmc.2005.09.026

DO - 10.1016/j.bmc.2005.09.026

M3 - Article

AN - SCOPUS:30344449178

SN - 0968-0896

VL - 14

SP - 1058

EP - 1062

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 4

ER -

Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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