Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue

Alicia Megia-fernandez; Bethany Mills; Chesney Michels; Sunay V. Chankeshwara; Kevin Dhaliwal; Mark Bradley

doi:10.1039/C7OB00663B

Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue

Alicia Megia-fernandez, Bethany Mills, Chesney Michels, Sunay V. Chankeshwara, Kevin Dhaliwal, Mark Bradley

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

Abstract / Description of output

A library of FRET-based peptides were prepared and studied as Thrombin substrates. This identified probes that showed selective activation by Thrombin, low fluorescent background signals, stability to Factor Xa, matrix metalloproteases, and primary human inflammatory cell lysates and supernatant. These were selected for further optimization, creating a second generation of fluorogenic probes with improved solubility and Plasmin resistance. The optimised probe allowed the detection of Thrombin activity in ex vivo fibrotic human tissue.

Original language	English
Journal	Organic & Biomolecular chemistry
Early online date	28 Apr 2017
DOIs	https://doi.org/10.1039/C7OB00663B
Publication status	E-pub ahead of print - 28 Apr 2017

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10.1039/C7OB00663BLicence: Creative Commons: Attribution (CC-BY)

20170509 Bradley C7OB00663BFinal published version, 2.1 MBLicence: Creative Commons: Attribution (CC-BY)

http://xlink.rsc.org/?DOI=C7OB00663B

Multiplexed 'Touch and Tell' Optical Molecular Sensing and Imaging
Bradley, M.
EPSRC
1/10/13 → 31/03/19
Project: Research
Molecular Optical Imaging of Key Targets in the Fibrogenic Pathway in Man
Bradley, M., Dhaliwal, K., Haslett, C., Hirani, N. & McGorum, B.
MRC
1/09/12 → 31/12/15
Project: Research

Cite this

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title = "Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue",

abstract = "A library of FRET-based peptides were prepared and studied as Thrombin substrates. This identified probes that showed selective activation by Thrombin, low fluorescent background signals, stability to Factor Xa, matrix metalloproteases, and primary human inflammatory cell lysates and supernatant. These were selected for further optimization, creating a second generation of fluorogenic probes with improved solubility and Plasmin resistance. The optimised probe allowed the detection of Thrombin activity in ex vivo fibrotic human tissue.",

author = "Alicia Megia-fernandez and Bethany Mills and Chesney Michels and Chankeshwara, {Sunay V.} and Kevin Dhaliwal and Mark Bradley",

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doi = "10.1039/C7OB00663B",

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AU - Megia-fernandez, Alicia

AU - Mills, Bethany

AU - Michels, Chesney

AU - Chankeshwara, Sunay V.

AU - Dhaliwal, Kevin

AU - Bradley, Mark

PY - 2017/4/28

Y1 - 2017/4/28

N2 - A library of FRET-based peptides were prepared and studied as Thrombin substrates. This identified probes that showed selective activation by Thrombin, low fluorescent background signals, stability to Factor Xa, matrix metalloproteases, and primary human inflammatory cell lysates and supernatant. These were selected for further optimization, creating a second generation of fluorogenic probes with improved solubility and Plasmin resistance. The optimised probe allowed the detection of Thrombin activity in ex vivo fibrotic human tissue.

AB - A library of FRET-based peptides were prepared and studied as Thrombin substrates. This identified probes that showed selective activation by Thrombin, low fluorescent background signals, stability to Factor Xa, matrix metalloproteases, and primary human inflammatory cell lysates and supernatant. These were selected for further optimization, creating a second generation of fluorogenic probes with improved solubility and Plasmin resistance. The optimised probe allowed the detection of Thrombin activity in ex vivo fibrotic human tissue.

U2 - 10.1039/C7OB00663B

DO - 10.1039/C7OB00663B

M3 - Article

SN - 1477-0520

JO - Organic & Biomolecular chemistry

JF - Organic & Biomolecular chemistry

ER -

Highly selective and rapidly activatable fluorogenic Thrombin sensors and application in human lung tissue

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Projects

Multiplexed 'Touch and Tell' Optical Molecular Sensing and Imaging

Molecular Optical Imaging of Key Targets in the Fibrogenic Pathway in Man

Cite this