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

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

20 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	Angewandte Chemie - International Edition
Vol/bind	51
Udgave nummer	17
Sider (fra-til)	4171-4175
Antal sider	5
ISSN	1433-7851
DOI	https://doi.org/10.1002/anie.201108345
Status	Udgivet - 23 apr. 2012
Udgivet eksternt	Ja

Adgang til dokumentet

10.1002/anie.201108345

Citationsformater

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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.",

keywords = "glycosyltransferases, NMR spectroscopy, surface plasmon resonance, X-ray crystallography",

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

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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.
I: Angewandte Chemie - International Edition, Bind 51, Nr. 17, 23.04.2012, s. 4171-4175.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

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.

KW - glycosyltransferases

KW - NMR spectroscopy

KW - surface plasmon resonance

KW - X-ray crystallography

U2 - 10.1002/anie.201108345

DO - 10.1002/anie.201108345

M3 - Journal article

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 -