Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α

D.L. Buckley; J.L. Gustafson; I. Van-Molle; A.G. Roth; H.S. Tae; P.C. Gareiss; W.L. Jorgensen; Alessio Ciulli; C.M. Crews

doi:10.1002/anie.201206231

Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α

D.L. Buckley
, J.L. Gustafson
, I. Van-Molle
, A.G. Roth
, H.S. Tae
, P.C. Gareiss
, W.L. Jorgensen
, Alessio Ciulli
, C.M. Crews

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

283 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	11463-11467
Number of pages	5
Journal	Angewandte Chemie International Edition
Volume	51
Issue number	46
DOIs	https://doi.org/10.1002/anie.201206231
Publication status	Published - 12 Nov 2012

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10.1002/anie.201206231

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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.

PY - 2012/11/12

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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.

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Small-molecule inhibitors of the interaction between the E3 ligase VHL and HIF1α

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