Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by dynamic ligation screening

Marco Florian Schmidt; Albert Isidro-Llobet; Michael Lisurek; Adeeb El-Dahshan; Jinzhi Tan; Rolf Hilgenfeld; Jörg Rademann

doi:10.1002/anie.200704594

Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by dynamic ligation screening

Marco Florian Schmidt, Albert Isidro-Llobet, Michael Lisurek, Adeeb El-Dahshan, Jinzhi Tan, Rolf Hilgenfeld, Jörg Rademann

Institute of Biochemistry

37 Citations (Scopus)

Abstract

(Chemical Presented) A potential anti-SARS drug has been developed by dynamic ligation screening (DLS), by which nucleophilic fragments are directed to the protein's active site by reversible reaction with an aldehyde inhibitor. Their inhibitory effect is detected by competition with a fluorogenic enzyme substrate. With this concept, low-affinity fragments binding specifically to the active site are quickly identified in a functional enzyme assay.

Original language	English
Journal	Angewandte Chemie - International Edition
Volume	47
Issue number	17
Pages (from-to)	3275-3278
Number of pages	4
ISSN	1433-7851
DOIs	https://doi.org/10.1002/anie.200704594
Publication status	Published - 14.04.2008

Research Areas and Centers

Academic Focus: Center for Infection and Inflammation Research (ZIEL)

Coronavirus related work

Research on SARS-CoV-2 / COVID-19

UN SDGs

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

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10.1002/anie.200704594

Cite this

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abstract = "(Chemical Presented) A potential anti-SARS drug has been developed by dynamic ligation screening (DLS), by which nucleophilic fragments are directed to the protein's active site by reversible reaction with an aldehyde inhibitor. Their inhibitory effect is detected by competition with a fluorogenic enzyme substrate. With this concept, low-affinity fragments binding specifically to the active site are quickly identified in a functional enzyme assay.",

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language = "English",

volume = "47",

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Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by dynamic ligation screening. / Schmidt, Marco Florian; Isidro-Llobet, Albert; Lisurek, Michael et al.
In: Angewandte Chemie - International Edition, Vol. 47, No. 17, 14.04.2008, p. 3275-3278.

Research output: Journal Articles › Journal articles › Research › peer-review

TY - JOUR

T1 - Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by dynamic ligation screening

AU - Schmidt, Marco Florian

AU - Isidro-Llobet, Albert

AU - Lisurek, Michael

AU - El-Dahshan, Adeeb

AU - Tan, Jinzhi

AU - Hilgenfeld, Rolf

AU - Rademann, Jörg

PY - 2008/4/14

Y1 - 2008/4/14

N2 - (Chemical Presented) A potential anti-SARS drug has been developed by dynamic ligation screening (DLS), by which nucleophilic fragments are directed to the protein's active site by reversible reaction with an aldehyde inhibitor. Their inhibitory effect is detected by competition with a fluorogenic enzyme substrate. With this concept, low-affinity fragments binding specifically to the active site are quickly identified in a functional enzyme assay.

AB - (Chemical Presented) A potential anti-SARS drug has been developed by dynamic ligation screening (DLS), by which nucleophilic fragments are directed to the protein's active site by reversible reaction with an aldehyde inhibitor. Their inhibitory effect is detected by competition with a fluorogenic enzyme substrate. With this concept, low-affinity fragments binding specifically to the active site are quickly identified in a functional enzyme assay.

UR - http://www.scopus.com/inward/record.url?scp=44949155667&partnerID=8YFLogxK

U2 - 10.1002/anie.200704594

DO - 10.1002/anie.200704594

M3 - Journal articles

C2 - 18348134

AN - SCOPUS:44949155667

SN - 1433-7851

VL - 47

SP - 3275

EP - 3278

JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 17

ER -

Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by dynamic ligation screening

Abstract

Research Areas and Centers

Coronavirus related work

UN SDGs

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