Identification of novel inhibitors of UDP-Glc4/-epimerase, a validated drug target for african sleeping sickness

M. D. Urbaniak; Jioji Natadra Tabudravu; A. Msaki; K. Mansfield Matera; R. Brenk; Marcel Jaspars; M. A. J. Ferguson

doi:10.1016/j.bmcl.2006.08.091

Identification of novel inhibitors of UDP-Glc4^/-epimerase, a validated drug target for african sleeping sickness

M. D. Urbaniak, Jioji Natadra Tabudravu, A. Msaki, K. Mansfield Matera, R. Brenk, Marcel Jaspars, M. A. J. Ferguson

Chemistry

Research output: Contribution to journal › Article › peer-review

34 Citations (Scopus)

Abstract

Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells. (c) 2006 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	5744-5747
Number of pages	3
Journal	Bioorganic & Medicinal Chemistry
Volume	16
DOIs	https://doi.org/10.1016/j.bmcl.2006.08.091
Publication status	Published - 2006

Keywords

epimerase
UDP-Glc 4 '-epimerase
UDP-glucose
UDP-galactose
Trypanosoma brucei
trypanosome
POLY-N-ACETYLLACTOSAMINE
TRYPANOSOMA-BRUCEI
GALACTOSE METABOLISM
GLYCOSYLATION
GLYCOPROTEINS

UN SDGs

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

Access to Document

10.1016/j.bmcl.2006.08.091

Cite this

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title = "Identification of novel inhibitors of UDP-Glc4/-epimerase, a validated drug target for african sleeping sickness",

abstract = "Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells. (c) 2006 Elsevier Ltd. All rights reserved.",

keywords = "epimerase, UDP-Glc 4 '-epimerase, UDP-glucose, UDP-galactose, Trypanosoma brucei, trypanosome, POLY-N-ACETYLLACTOSAMINE, TRYPANOSOMA-BRUCEI, GALACTOSE METABOLISM, GLYCOSYLATION, GLYCOPROTEINS",

author = "Urbaniak, {M. D.} and Tabudravu, {Jioji Natadra} and A. Msaki and {Mansfield Matera}, K. and R. Brenk and Marcel Jaspars and Ferguson, {M. A. J.}",

year = "2006",

doi = "10.1016/j.bmcl.2006.08.091",

language = "English",

volume = "16",

pages = "5744--5747",

journal = "Bioorganic & Medicinal Chemistry",

issn = "0968-0896",

publisher = "Elsevier Ltd",

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TY - JOUR

T1 - Identification of novel inhibitors of UDP-Glc4/-epimerase, a validated drug target for african sleeping sickness

AU - Urbaniak, M. D.

AU - Tabudravu, Jioji Natadra

AU - Msaki, A.

AU - Mansfield Matera, K.

AU - Brenk, R.

AU - Jaspars, Marcel

AU - Ferguson, M. A. J.

PY - 2006

Y1 - 2006

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AB - Novel inhibitors of Trypanosoma brucei and mammalian UDP-Glc 4'-epimerase were identified by screening a small library of natural products and commercially available drug-like molecules. The inhibitors possess low micromolar potency against the T brucei and human enzymes in vitro, display a degree of selectivity between the two enzymes, and are cytotoxic to cultured T. brucei and mammalian cells. (c) 2006 Elsevier Ltd. All rights reserved.

KW - epimerase

KW - UDP-Glc 4 '-epimerase

KW - UDP-glucose

KW - UDP-galactose

KW - Trypanosoma brucei

KW - trypanosome

KW - POLY-N-ACETYLLACTOSAMINE

KW - TRYPANOSOMA-BRUCEI

KW - GALACTOSE METABOLISM

KW - GLYCOSYLATION

KW - GLYCOPROTEINS

U2 - 10.1016/j.bmcl.2006.08.091

DO - 10.1016/j.bmcl.2006.08.091

M3 - Article

SN - 0968-0896

VL - 16

SP - 5744

EP - 5747

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

ER -