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

Institut für Biochemie

58 Zitate (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.

Originalsprache	Englisch
Zeitschrift	Angewandte Chemie - International Edition
Jahrgang	47
Ausgabenummer	17
Seiten (von - bis)	3275-3278
Seitenumfang	4
ISSN	1433-7851
DOIs	https://doi.org/10.1002/anie.200704594
Publikationsstatus	Veröffentlicht - 14.04.2008

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Forschungsschwerpunkt: Infektion und Entzündung - Zentrum für Infektions- und Entzündungsforschung Lübeck (ZIEL)

Coronavirus-Bezug

Forschung zu SARS-CoV-2 / COVID-19

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10.1002/anie.200704594

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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.",

author = "Schmidt, \{Marco Florian\} and Albert Isidro-Llobet and Michael Lisurek and Adeeb El-Dahshan and Jinzhi Tan and Rolf Hilgenfeld and J{\"o}rg Rademann",

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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, Jahrgang 47, Nr. 17, 14.04.2008, S. 3275-3278.

Publikation: Beiträge in Fachzeitschriften › Zeitschriftenaufsätze › Forschung › Begutachtung

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 - https://www.scopus.com/pages/publications/44949155667

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

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Strategische Forschungsbereiche und Zentren

Coronavirus-Bezug

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