A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding

Rene Jørgensen; Lena Lisbeth Grimm; Nora Sindhuwinata; Thomas Peters; Monica M. Palcic

doi:10.1002/anie.201108345

A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding

Rene Jørgensen^*, Lena Lisbeth Grimm, Nora Sindhuwinata, Thomas Peters, Monica M. Palcic

^*Korrespondierende/r Autor/-in für diese Arbeit

Institut für Chemie und Metabolomics

Carlsberg Laboratory

20 Zitate (Scopus)

Abstract

A fragmented approach: 3-Phenyl-5-piperazino-1,2,4-thiadiazole (designated "compound382" in the Ro5 Maybridge Fragment Library, see scheme) is demonstrated to be an effective inhibitor of human blood group glycosyltransferaseB. The compound interferes with both acceptor and donor binding and also displaces the Mn ²⁺ ion in the binding pocket.

Originalsprache	Englisch
Zeitschrift	Angewandte Chemie - International Edition
Jahrgang	51
Ausgabenummer	17
Seiten (von - bis)	4171-4175
Seitenumfang	5
ISSN	1433-7851
DOIs	https://doi.org/10.1002/anie.201108345
Publikationsstatus	Veröffentlicht - 23.04.2012

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title = "A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding",

abstract = "A fragmented approach: 3-Phenyl-5-piperazino-1,2,4-thiadiazole (designated {"}compound382{"} in the Ro5 Maybridge Fragment Library, see scheme) is demonstrated to be an effective inhibitor of human blood group glycosyltransferaseB. The compound interferes with both acceptor and donor binding and also displaces the Mn 2+ ion in the binding pocket.",

author = "Rene J{\o}rgensen and Grimm, \{Lena Lisbeth\} and Nora Sindhuwinata and Thomas Peters and Palcic, \{Monica M.\}",

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day = "23",

doi = "10.1002/anie.201108345",

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pages = "4171--4175",

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A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding. / Jørgensen, Rene; Grimm, Lena Lisbeth; Sindhuwinata, Nora et al.
in: Angewandte Chemie - International Edition, Jahrgang 51, Nr. 17, 23.04.2012, S. 4171-4175.

Publikation: Beiträge in Fachzeitschriften › Zeitschriftenaufsätze › Forschung › Begutachtung

TY - JOUR

T1 - A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding

AU - Jørgensen, Rene

AU - Grimm, Lena Lisbeth

AU - Sindhuwinata, Nora

AU - Peters, Thomas

AU - Palcic, Monica M.

PY - 2012/4/23

Y1 - 2012/4/23

N2 - A fragmented approach: 3-Phenyl-5-piperazino-1,2,4-thiadiazole (designated "compound382" in the Ro5 Maybridge Fragment Library, see scheme) is demonstrated to be an effective inhibitor of human blood group glycosyltransferaseB. The compound interferes with both acceptor and donor binding and also displaces the Mn 2+ ion in the binding pocket.

AB - A fragmented approach: 3-Phenyl-5-piperazino-1,2,4-thiadiazole (designated "compound382" in the Ro5 Maybridge Fragment Library, see scheme) is demonstrated to be an effective inhibitor of human blood group glycosyltransferaseB. The compound interferes with both acceptor and donor binding and also displaces the Mn 2+ ion in the binding pocket.

UR - https://www.scopus.com/pages/publications/84859982558

U2 - 10.1002/anie.201108345

DO - 10.1002/anie.201108345

M3 - Journal articles

C2 - 22407594

AN - SCOPUS:84859982558

SN - 1433-7851

VL - 51

SP - 4171

EP - 4175

JO - Angewandte Chemie - International Edition

JF - Angewandte Chemie - International Edition

IS - 17

ER -

A glycosyltransferase inhibitor from a molecular fragment library simultaneously interferes with metal ion and substrate binding

Abstract

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