FIELD: biotechnology.
SUBSTANCE: invention relates to bifunctional compounds represented by a chemical structure: PTM-L-ULM, where PTM is a small molecule of a protein-targeting fragment, which binds to intracellular target protein selected from a group consisting of focal adhesion kinase, tyrosine kinase, estrogen receptor, androgen receptor, BET protein containing bromodomain, Ras, Raf, and epidermal growth factor receptor; L is a chemical linker group binding ULM to PTM; and ULM is a small molecule of a binding fragment of ubiquitin ligase E3 Von Hippel Lindau (VHL).
EFFECT: obtaining compounds enhancing the degradation of target proteins.
16 cl, 19 dwg, 2 tbl, 1 ex
Title | Year | Author | Number |
---|---|---|---|
COMPOUNDS AND METHODS FOR ENHANCED DEGRADATION OF TARGET PROTEINS AND OTHER POLYPEPTIDES BY AN E3 UBIQUITIN LIGASE | 2013 |
|
RU2666530C2 |
COMPOUNDS AND METHODS FOR IMPROVED CLEAVAGE OF TARGET PROTEINS | 2016 |
|
RU2782063C2 |
PROTEOLYSIS MODULATORS AND RELATED USES | 2019 |
|
RU2805511C2 |
OXADIAZOLES AS MUSCARINIC RECEPTOR AGONISTS M AND/OR M | 2019 |
|
RU2817018C2 |
NITRILE-CONTAINING ANTIVIRAL COMPOUNDS | 2021 |
|
RU2820150C2 |
NITRILE-CONTAINING ANTIVIRAL COMPOUNDS | 2021 |
|
RU2786722C1 |
CONDENSED QUINOLINE DERIVATIVE AND USE THEREOF | 2005 |
|
RU2384571C2 |
BICYCLIC COMPOUNDS AS PD1/PD-L1 INTERACTION/ACTIVATION INHIBITORS | 2019 |
|
RU2777980C2 |
COMPOUNDS AND COMPOSITIONS USED FOR TREATMENT OF NTRK-RELATED DISORDERS | 2016 |
|
RU2744974C2 |
AZABENZOFURANYL COMPOUNDS AND METHODS OF USE | 2007 |
|
RU2448111C2 |
Authors
Dates
2022-10-12—Published
2013-01-11—Filed