Micro arrayed compound screening (μARCS) for inhibitors of methionine aminopeptidase type 2

Yihong Fan; Jieyi Wang; Pingping Lou; Jack Henkin; James L. Kofron; David J. Burns; Usha Warrior; Steven N. Anderson

doi:10.2174/1570180054771518

Micro arrayed compound screening (μARCS) for inhibitors of methionine aminopeptidase type 2

Yihong Fan, Jieyi Wang, Pingping Lou, Jack Henkin, James L. Kofron, David J. Burns, Usha Warrior^*, Steven N. Anderson

^*Corresponding author for this work

CLP - Chemistry of Life Processes Institute

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

Abstract

Methionine aminopeptidase type 2 catalyzes the removal of the amino-terminal methionine from newly translated polypeptides and has been shown to be a promising target for anti-angiogenesis and anticancer drugs. We describe a novel μARCS HTS method to identify inhibitors of this target utilizing porous matrices to introduce reagents throughout the assay. A library of 250,000 compounds was screened and compounds with IC₅₀ values of less than 10μM were identified. These compounds may serve as initial lead molecules for further medicinal chemistry optimization.

Original language	English (US)
Pages (from-to)	462-469
Number of pages	8
Journal	Letters in Drug Design and Discovery
Volume	2
Issue number	6
DOIs	https://doi.org/10.2174/1570180054771518
State	Published - Sep 2005

Keywords

Aminopeptidase
Cancer
Membranes
MetAP2
Methionine
μARCS

ASJC Scopus subject areas

Molecular Medicine
Pharmaceutical Science
Drug Discovery

UN SDGs

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

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10.2174/1570180054771518

Cite this

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title = "Micro arrayed compound screening (μARCS) for inhibitors of methionine aminopeptidase type 2",

abstract = "Methionine aminopeptidase type 2 catalyzes the removal of the amino-terminal methionine from newly translated polypeptides and has been shown to be a promising target for anti-angiogenesis and anticancer drugs. We describe a novel μARCS HTS method to identify inhibitors of this target utilizing porous matrices to introduce reagents throughout the assay. A library of 250,000 compounds was screened and compounds with IC50 values of less than 10μM were identified. These compounds may serve as initial lead molecules for further medicinal chemistry optimization.",

keywords = "Aminopeptidase, Cancer, Membranes, MetAP2, Methionine, μARCS",

author = "Yihong Fan and Jieyi Wang and Pingping Lou and Jack Henkin and Kofron, {James L.} and Burns, {David J.} and Usha Warrior and Anderson, {Steven N.}",

year = "2005",

month = sep,

doi = "10.2174/1570180054771518",

language = "English (US)",

volume = "2",

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publisher = "Bentham Science Publishers B.V.",

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TY - JOUR

T1 - Micro arrayed compound screening (μARCS) for inhibitors of methionine aminopeptidase type 2

AU - Fan, Yihong

AU - Wang, Jieyi

AU - Lou, Pingping

AU - Henkin, Jack

AU - Kofron, James L.

AU - Burns, David J.

AU - Warrior, Usha

AU - Anderson, Steven N.

PY - 2005/9

Y1 - 2005/9

N2 - Methionine aminopeptidase type 2 catalyzes the removal of the amino-terminal methionine from newly translated polypeptides and has been shown to be a promising target for anti-angiogenesis and anticancer drugs. We describe a novel μARCS HTS method to identify inhibitors of this target utilizing porous matrices to introduce reagents throughout the assay. A library of 250,000 compounds was screened and compounds with IC50 values of less than 10μM were identified. These compounds may serve as initial lead molecules for further medicinal chemistry optimization.

AB - Methionine aminopeptidase type 2 catalyzes the removal of the amino-terminal methionine from newly translated polypeptides and has been shown to be a promising target for anti-angiogenesis and anticancer drugs. We describe a novel μARCS HTS method to identify inhibitors of this target utilizing porous matrices to introduce reagents throughout the assay. A library of 250,000 compounds was screened and compounds with IC50 values of less than 10μM were identified. These compounds may serve as initial lead molecules for further medicinal chemistry optimization.

KW - Aminopeptidase

KW - Cancer

KW - Membranes

KW - MetAP2

KW - Methionine

KW - μARCS

UR - http://www.scopus.com/inward/record.url?scp=24744464136&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=24744464136&partnerID=8YFLogxK

U2 - 10.2174/1570180054771518

DO - 10.2174/1570180054771518

M3 - Article

AN - SCOPUS:24744464136

SN - 1570-1808

VL - 2

SP - 462

EP - 469

JO - Letters in Drug Design and Discovery

JF - Letters in Drug Design and Discovery

IS - 6

ER -

Micro arrayed compound screening (μARCS) for inhibitors of methionine aminopeptidase type 2

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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