Isolation and characterization of β-transducin repeat-containing protein ligands screened using a high-throughput screening system.


Journal

Oncology research
ISSN: 1555-3906
Titre abrégé: Oncol Res
Pays: United States
ID NLM: 9208097

Informations de publication

Date de publication:
2023
Historique:
received: 28 03 2023
accepted: 19 05 2023
medline: 8 8 2023
pubmed: 7 8 2023
entrez: 7 8 2023
Statut: epublish

Résumé

β-transducin repeat-containing protein (β-TrCP) is an F-box protein subunit of the E3 Skp1-Cullin-F box (SCF) type ubiquitin-ligase complex, and provides the substrate specificity for the ligase. To find potent ligands of β-TrCP useful for the proteolysis targeting chimera (PROTAC) system using β-TrCP in the future, we developed a high-throughput screening system for small molecule β-TrCP ligands. We screened the chemical library utilizing the system and obtained several hit compounds. The effects of the hit compounds on

Identifiants

pubmed: 37547765
doi: 10.32604/or.2023.030240
pii: 30240
pmc: PMC10398414
doi:

Substances chimiques

beta-Transducin Repeat-Containing Proteins 0
SKP Cullin F-Box Protein Ligases EC 2.3.2.27
Ligands 0
Cullin Proteins 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

645-654

Informations de copyright

© 2023 Liu et al.

Déclaration de conflit d'intérêts

The authors declare that they have no conflicts of interest to report regarding the present study.

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Auteurs

Xintong Liu (X)

Chemical Resource Development Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.
Department of RIKEN Molecular and Chemical Somatology, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo, 113-8510, Japan.
Bioprobe Application Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.

Emiko Sanada (E)

Chemical Resource Development Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.
Bioprobe Application Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.
Chemical Biology Research Group, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.

Jiang Li (J)

Guangdong Engineering Research Center of Oral Restoration and Reconstruction, Affiliated Stomatology Hospital of Guangzhou Medical University, Guangzhou, 510180, China.

Xiaomeng Li (X)

KingMed School of Laboratory Medicine, Guangzhou Medical University, Guangzhou, 510182, China.

Hiroyuki Osada (H)

Chemical Resource Development Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.
Chemical Biology Research Group, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.
Department of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Shizuoka, 422-8526, Japan.

Nobumoto Watanabe (N)

Chemical Resource Development Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.
Department of RIKEN Molecular and Chemical Somatology, Graduate School of Medical and Dental Sciences, Tokyo Medical and Dental University, Bunkyo-ku, Tokyo, 113-8510, Japan.
Bioprobe Application Research Unit, RIKEN CSRS, Wako, Saitama, 351-0198, Japan.

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