Research output: Contribution to Journal/Magazine › Journal article › peer-review
Research output: Contribution to Journal/Magazine › Journal article › peer-review
}
TY - JOUR
T1 - Identification of novel inhibitors of UDP-Glc 4'-epimerase, a validated drug target for african sleeping sickness
AU - Urbaniak, Michael D.
AU - Tabudravu, Jioji N.
AU - Msaki, Aichi
AU - Matera, Kathy Mansfield
AU - Brenk, Ruth
AU - Jaspars, Marcel
AU - Ferguson, Michael A. J.
PY - 2006/11/15
Y1 - 2006/11/15
N2 - 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.
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.
KW - Animals
KW - Enzyme Inhibitors
KW - Humans
KW - Models, Chemical
KW - Trypanocidal Agents
KW - Trypanosoma brucei brucei
KW - Trypanosomiasis, African
KW - UDPglucose 4-Epimerase
U2 - 10.1016/j.bmcl.2006.08.091
DO - 10.1016/j.bmcl.2006.08.091
M3 - Journal article
C2 - 16962325
VL - 16
SP - 5744
EP - 5747
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 22
ER -