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.Info
- 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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102000004169 proteins and genes Human genes 0.000 title abstract 5
- 108090000623 proteins and genes Proteins 0.000 title abstract 5
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 title abstract 3
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 title abstract 3
- 230000015556 catabolic process Effects 0.000 title abstract 3
- 238000006731 degradation reaction Methods 0.000 title abstract 3
- 229920001184 polypeptide Polymers 0.000 title abstract 3
- 102000004196 processed proteins & peptides Human genes 0.000 title abstract 3
- 108090000765 processed proteins & peptides Proteins 0.000 title abstract 3
- 238000000034 method Methods 0.000 title 1
- 230000001588 bifunctional effect Effects 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000034512 ubiquitination Effects 0.000 abstract 1
- 238000010798 ubiquitination Methods 0.000 abstract 1
Classifications
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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.
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US201261585769P | 2012-01-12 | 2012-01-12 | |
PCT/US2013/021136 WO2013106643A2 (en) | 2012-01-12 | 2013-01-11 | Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase |
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MX358660B true MX358660B (es) | 2018-08-30 |
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MX2022009478A MX2022009478A (es) | 2012-01-12 | 2014-07-11 | Compuestos y metodos para degradacion mejorada de proteinas y otros polipeptidos elegidos como blanco mediante una ubiquitina ligasa e3. |
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US (2) | US10730862B2 (es) |
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BR (1) | BR112014017095A2 (es) |
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