Design of a selective chemical probe for class I PDZ domains

Naoaki Fujii; Anang Shelat; Randy A. Hall; R. Kiplin Guy

doi:10.1016/j.bmcl.2006.10.027

Design of a selective chemical probe for class I PDZ domains

Naoaki Fujii
, Anang Shelat
, Randy A. Hall
, R. Kiplin Guy

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

12 Scopus citations

Abstract

Covalent labeling has been widely used for structural and functional analyses of proteins. To target a wide range of PDZ domains, we designed a chemical scaffold mimicking the E/D-T/S-XV peptide, which is a PDZ domain that binds ligands in higher occurrence. A chemical probe (2) that contained this moiety alkylated diverse PDZ domains, including NHERF-1 PDZ2, and differentially visualized the cellular proteome.

Original language	English
Pages (from-to)	546-548
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	2
DOIs	https://doi.org/10.1016/j.bmcl.2006.10.027
State	Published - Jan 15 2007

Bibliographical note

Funding Information:
We thank Kathleen A. P. Novak for providing GST-MAGI3 PDZ2 protein and its H73A mutant; R. Mike Gage for providing HEK293 cells that express NHERF-1-HA; Amanda M. Castleberry for excellent technical assistance; and Angela McArthur for scientific editing of the manuscript. Financial support was provided in part by the American Lebanese Syrian Associated Charities (N.F., A.S., and R.K.G.).

Funding

We thank Kathleen A. P. Novak for providing GST-MAGI3 PDZ2 protein and its H73A mutant; R. Mike Gage for providing HEK293 cells that express NHERF-1-HA; Amanda M. Castleberry for excellent technical assistance; and Angela McArthur for scientific editing of the manuscript. Financial support was provided in part by the American Lebanese Syrian Associated Charities (N.F., A.S., and R.K.G.).

Funders
American Lebanese Syrian Associated Charities

Keywords

Chemical probe
NHERF
PDZ domain
Proteomics

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2006.10.027

Cite this

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title = "Design of a selective chemical probe for class I PDZ domains",

abstract = "Covalent labeling has been widely used for structural and functional analyses of proteins. To target a wide range of PDZ domains, we designed a chemical scaffold mimicking the E/D-T/S-XV peptide, which is a PDZ domain that binds ligands in higher occurrence. A chemical probe (2) that contained this moiety alkylated diverse PDZ domains, including NHERF-1 PDZ2, and differentially visualized the cellular proteome.",

keywords = "Chemical probe, NHERF, PDZ domain, Proteomics",

author = "Naoaki Fujii and Anang Shelat and Hall, \{Randy A.\} and \{Kiplin Guy\}, R.",

note = "Funding Information: We thank Kathleen A. P. Novak for providing GST-MAGI3 PDZ2 protein and its H73A mutant; R. Mike Gage for providing HEK293 cells that express NHERF-1-HA; Amanda M. Castleberry for excellent technical assistance; and Angela McArthur for scientific editing of the manuscript. Financial support was provided in part by the American Lebanese Syrian Associated Charities (N.F., A.S., and R.K.G.). ",

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T1 - Design of a selective chemical probe for class I PDZ domains

AU - Fujii, Naoaki

AU - Shelat, Anang

AU - Hall, Randy A.

AU - Kiplin Guy, R.

N1 - Funding Information: We thank Kathleen A. P. Novak for providing GST-MAGI3 PDZ2 protein and its H73A mutant; R. Mike Gage for providing HEK293 cells that express NHERF-1-HA; Amanda M. Castleberry for excellent technical assistance; and Angela McArthur for scientific editing of the manuscript. Financial support was provided in part by the American Lebanese Syrian Associated Charities (N.F., A.S., and R.K.G.).

PY - 2007/1/15

Y1 - 2007/1/15

N2 - Covalent labeling has been widely used for structural and functional analyses of proteins. To target a wide range of PDZ domains, we designed a chemical scaffold mimicking the E/D-T/S-XV peptide, which is a PDZ domain that binds ligands in higher occurrence. A chemical probe (2) that contained this moiety alkylated diverse PDZ domains, including NHERF-1 PDZ2, and differentially visualized the cellular proteome.

AB - Covalent labeling has been widely used for structural and functional analyses of proteins. To target a wide range of PDZ domains, we designed a chemical scaffold mimicking the E/D-T/S-XV peptide, which is a PDZ domain that binds ligands in higher occurrence. A chemical probe (2) that contained this moiety alkylated diverse PDZ domains, including NHERF-1 PDZ2, and differentially visualized the cellular proteome.

KW - Chemical probe

KW - NHERF

KW - PDZ domain

KW - Proteomics

UR - https://www.scopus.com/pages/publications/33846095971

UR - https://www.scopus.com/pages/publications/33846095971#tab=citedBy

U2 - 10.1016/j.bmcl.2006.10.027

DO - 10.1016/j.bmcl.2006.10.027

M3 - Article

C2 - 17074480

AN - SCOPUS:33846095971

SN - 0960-894X

VL - 17

SP - 546

EP - 548

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 2

ER -

Design of a selective chemical probe for class I PDZ domains

Abstract

Bibliographical note

Funding

Keywords

ASJC Scopus subject areas

Access to Document

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