TY - JOUR
T1 - Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α
AU - Buckley, D.L.
AU - Gustafson, J.L.
AU - Van-Molle, I.
AU - Roth, A.G.
AU - Tae, H.S.
AU - Gareiss, P.C.
AU - Jorgensen, W.L.
AU - Ciulli, Alessio
AU - Crews, C.M.
N1 - Copyright 2012 Elsevier B.V., All rights reserved.
PY - 2012/11/12
Y1 - 2012/11/12
N2 - By design: Novel small-molecule inhibitors of the interaction between the von Hippel-Lindau ligase (VHL) and its molecular target HIF1a, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC50 value of 0.9-µM and is thus the first sub-micromolar inhibitor of the VHL-HIF1a interaction.
AB - By design: Novel small-molecule inhibitors of the interaction between the von Hippel-Lindau ligase (VHL) and its molecular target HIF1a, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC50 value of 0.9-µM and is thus the first sub-micromolar inhibitor of the VHL-HIF1a interaction.
UR - http://www.scopus.com/inward/record.url?scp=84868522211&partnerID=8YFLogxK
U2 - 10.1002/anie.201206231
DO - 10.1002/anie.201206231
M3 - Article
AN - SCOPUS:84868522211
SN - 1433-7851
VL - 51
SP - 11463
EP - 11467
JO - Angewandte Chemie International Edition
JF - Angewandte Chemie International Edition
IS - 46
ER -