Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains

Chong-Jing Zhang; Chelsea Y. J. Tan; Jingyan Ge; Zhenkun Na; Grace Y. J. Chen; Mahesh Uttamchandani; Hongyan Sun; Shao Q. Yao

doi:10.1002/anie.201307803

Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains

Chong-Jing Zhang
, Chelsea Y. J. Tan
, Jingyan Ge
, Zhenkun Na
, Grace Y. J. Chen
, Mahesh Uttamchandani
, Hongyan Sun
, Shao Q. Yao

Research output: Journal Publications and Reviews › RGC 21 - Publication in refereed journal › peer-review

40 Citations (Scopus)

Abstract

Fast and efficient: A library of trans-cyclooctene (TCO)-modified small molecules were immobilized on tetrazine-functionalized glass slides by using the fastest bioorthogonal reaction known. The resulting small-molecule microarray was screened against a variety of human bromodomains to identify protein-protein interaction inhibitors. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Original language	English
Pages (from-to)	14060-14064
Journal	Angewandte Chemie - International Edition
Volume	52
Issue number	52
Online published	4 Nov 2013
DOIs	https://doi.org/10.1002/anie.201307803
Publication status	Published - 23 Dec 2013

Research Keywords

bioorthogonal chemistry
epigenetics
inhibitors
protein-protein interactions
small-molecule microarrays

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10.1002/anie.201307803

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Zhang, C.-J., Tan, C. Y. J., Ge, J., Na, Z., Chen, G. Y. J., Uttamchandani, M., Sun, H., & Yao, S. Q. (2013). Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains. Angewandte Chemie - International Edition, 52(52), 14060-14064. https://doi.org/10.1002/anie.201307803

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title = "Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains",

abstract = "Fast and efficient: A library of trans-cyclooctene (TCO)-modified small molecules were immobilized on tetrazine-functionalized glass slides by using the fastest bioorthogonal reaction known. The resulting small-molecule microarray was screened against a variety of human bromodomains to identify protein-protein interaction inhibitors. Copyright {\textcopyright} 2013 WILEY-VCH Verlag GmbH \& Co. KGaA, Weinheim.",

keywords = "bioorthogonal chemistry, epigenetics, inhibitors, protein-protein interactions, small-molecule microarrays",

author = "Chong-Jing Zhang and Tan, \{Chelsea Y. J.\} and Jingyan Ge and Zhenkun Na and Chen, \{Grace Y. J.\} and Mahesh Uttamchandani and Hongyan Sun and Yao, \{Shao Q.\}",

year = "2013",

month = dec,

day = "23",

doi = "10.1002/anie.201307803",

language = "English",

volume = "52",

pages = "14060--14064",

journal = "Angewandte Chemie - International Edition",

issn = "1433-7851",

publisher = "John Wiley \& Sons",

number = "52",

}

Zhang, C-J, Tan, CYJ, Ge, J, Na, Z, Chen, GYJ, Uttamchandani, M, Sun, H & Yao, SQ 2013, 'Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains', Angewandte Chemie - International Edition, vol. 52, no. 52, pp. 14060-14064. https://doi.org/10.1002/anie.201307803

Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains. / Zhang, Chong-Jing; Tan, Chelsea Y. J.; Ge, Jingyan et al.
In: Angewandte Chemie - International Edition, Vol. 52, No. 52, 23.12.2013, p. 14060-14064.

Research output: Journal Publications and Reviews › RGC 21 - Publication in refereed journal › peer-review

TY - JOUR

T1 - Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains

AU - Zhang, Chong-Jing

AU - Tan, Chelsea Y. J.

AU - Ge, Jingyan

AU - Na, Zhenkun

AU - Chen, Grace Y. J.

AU - Uttamchandani, Mahesh

AU - Sun, Hongyan

AU - Yao, Shao Q.

PY - 2013/12/23

Y1 - 2013/12/23

N2 - Fast and efficient: A library of trans-cyclooctene (TCO)-modified small molecules were immobilized on tetrazine-functionalized glass slides by using the fastest bioorthogonal reaction known. The resulting small-molecule microarray was screened against a variety of human bromodomains to identify protein-protein interaction inhibitors. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

AB - Fast and efficient: A library of trans-cyclooctene (TCO)-modified small molecules were immobilized on tetrazine-functionalized glass slides by using the fastest bioorthogonal reaction known. The resulting small-molecule microarray was screened against a variety of human bromodomains to identify protein-protein interaction inhibitors. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

KW - bioorthogonal chemistry

KW - epigenetics

KW - inhibitors

KW - protein-protein interactions

KW - small-molecule microarrays

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U2 - 10.1002/anie.201307803

DO - 10.1002/anie.201307803

M3 - RGC 21 - Publication in refereed journal

C2 - 24353229

SN - 1433-7851

VL - 52

SP - 14060

EP - 14064

JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 52

ER -

Zhang CJ, Tan CYJ, Ge J, Na Z, Chen GYJ, Uttamchandani M et al. Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains. Angewandte Chemie - International Edition. 2013 Dec 23;52(52):14060-14064. Epub 2013 Nov 4. doi: 10.1002/anie.201307803

Preparation of small-molecule microarrays by trans-cyclooctene tetrazine ligation and their application in the high-throughput screening of protein-protein interaction inhibitors of bromodomains

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