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

^*Corresponding author for this work

Institute of Chemistry and Metabolomics

Carlsberg Laboratory

20 Citations (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.

Original language	English
Journal	Angewandte Chemie - International Edition
Volume	51
Issue number	17
Pages (from-to)	4171-4175
Number of pages	5
ISSN	1433-7851
DOIs	https://doi.org/10.1002/anie.201108345
Publication status	Published - 23.04.2012

Research Areas and Centers

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

UN SDGs

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

Access to Document

10.1002/anie.201108345

Cite this

@article{9f9d9a867c0f41f4aff1de14310b8c0a,

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.}",

year = "2012",

month = apr,

day = "23",

doi = "10.1002/anie.201108345",

language = "English",

volume = "51",

pages = "4171--4175",

journal = "Angewandte Chemie - International Edition",

issn = "1433-7851",

number = "17",

}

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 - http://www.scopus.com/inward/record.url?scp=84859982558&partnerID=8YFLogxK

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

Research Areas and Centers

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this