COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE

Craig M. Crews; Dennis L. Buckley; Alessio Ciulli; William L. Jorgensen; Peter C. Gareiss; Inge Van Molle; Jeffrey Gustafson; Hyun Seop Tae; Julien Michel; Dentin Hoyer; Anke Roth; John Harling; Ian Edward David Smith; Afjai Hussain Miah; Sebastian Campos; Joelle Le

COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE

Craig M. Crews (Inventor), Dennis L. Buckley (Inventor), Alessio Ciulli (Inventor), William L. Jorgensen (Inventor), Peter C. Gareiss (Inventor), Inge Van Molle (Inventor), Jeffrey Gustafson (Inventor), Hyun Seop Tae (Inventor), Julien Michel (Inventor), Dentin Hoyer (Inventor), Anke Roth (Inventor), John Harling (Inventor), Ian Edward David Smith (Inventor), Afjai Hussain Miah (Inventor), Sebastian Campos (Inventor), Joelle Le (Inventor)

Research output: Patent

Abstract / Description of output

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Original language	English
Publication status	Published - 18 Jul 2013

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title = "COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE",

abstract = "The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.",

author = "Crews, {Craig M.} and Buckley, {Dennis L.} and Alessio Ciulli and Jorgensen, {William L.} and Gareiss, {Peter C.} and {Van Molle}, Inge and Jeffrey Gustafson and Tae, {Hyun Seop} and Julien Michel and Dentin Hoyer and Anke Roth and John Harling and Smith, {Ian Edward David} and Miah, {Afjai Hussain} and Sebastian Campos and Joelle Le",

year = "2013",

month = jul,

day = "18",

language = "English",

type = "Patent",

}

TY - PAT

T1 - COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE

AU - Crews, Craig M.

AU - Buckley, Dennis L.

AU - Ciulli, Alessio

AU - Jorgensen, William L.

AU - Gareiss, Peter C.

AU - Van Molle, Inge

AU - Gustafson, Jeffrey

AU - Tae, Hyun Seop

AU - Michel, Julien

AU - Hoyer, Dentin

AU - Roth, Anke

AU - Harling, John

AU - Smith, Ian Edward David

AU - Miah, Afjai Hussain

AU - Campos, Sebastian

AU - Le, Joelle

PY - 2013/7/18

Y1 - 2013/7/18

N2 - The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

AB - The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

M3 - Patent

ER -

COMPOUNDS & METHODS FOR THE ENHANCED DEGRADATION OF TARGETED PROTEINS & OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE

Abstract / Description of output

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