MX358660B - Compuestos y metodos para degradacion mejorada de proteinas y otros polipeptidos elegidos como blanco mediante una ubiquitina ligasa e3. - Google Patents

Compuestos y metodos para degradacion mejorada de proteinas y otros polipeptidos elegidos como blanco mediante una ubiquitina ligasa e3.

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Publication number
MX358660B
MX358660B MX2014008520A MX2014008520A MX358660B MX 358660 B MX358660 B MX 358660B MX 2014008520 A MX2014008520 A MX 2014008520A MX 2014008520 A MX2014008520 A MX 2014008520A MX 358660 B MX358660 B MX 358660B
Authority
MX
Mexico
Prior art keywords
polypeptides
present
compounds
ubiquitin ligase
methods
Prior art date
Application number
MX2014008520A
Other languages
English (en)
Other versions
MX2014008520A (es
Inventor
M Crews Craig
Buckley Dennis
Ciulli Alessio
Jorgensen William
C Gareiss Peter
Van Molle Inge
Gustafson Jeffrey
Tae Hyun-Seop
Michel Julien
Wade Hoyer Dentin
G Roth Anke
David Harling John
Edward David Smith Ian
Hussain Miah Afjal
Andre Campos Sebastien
Le Joelle
Original Assignee
Univ Yale
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Univ Yale filed Critical Univ Yale
Publication of MX2014008520A publication Critical patent/MX2014008520A/es
Publication of MX358660B publication Critical patent/MX358660B/es

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Abstract

La presente invención se refiere a compuestos bifuncionales, los cuales encuentran utilidad como moduladores de la modificación con ubiquitina dirigida, especialmente inhibidores de una variedad de polipéptidos y otras proteínas las cuales son degradadas y/o de alguna otra manera inhibidas por los compuestos bifuncionales de conformidad con la presente invención. En particular, la presente invención está dirigida a compuestos, los cuales contienen en un extremo un ligando de VHL el cual se une a la ubiquitina ligasa y en el otro extremo una porción que liga una proteína objetivo de modo tal que la proteína objetivo es colocada en proximidad a la ubiquitina ligasa para efectuar la degradación (e inhibición) de dicha proteína. La presente invención exhibe una amplia gama de actividades farmacológicas asociadas con los compuestos de conformidad con la presente invención, consistentes con la degradación/inhibición de los polipéptidos elegidos como blanco.
MX2014008520A 2012-01-12 2013-01-11 Compuestos y metodos para degradacion mejorada de proteinas y otros polipeptidos elegidos como blanco mediante una ubiquitina ligasa e3. MX358660B (es)

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