CRBN ligand expansion for hematopoietic prostaglandin D

Ligands Prostaglandins / metabolism Proteolysis Ubiquitin-Protein Ligases / chemistry Proteolysis Targeting Chimera / chemistry
ADME Docking study H-PGDS PROTAC Phenyl-glutarimide

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
15 04 2023
Historique:
received: 02 03 2023
revised: 17 03 2023
accepted: 20 03 2023
medline: 11 4 2023
pubmed: 6 4 2023
entrez: 5 4 2023
Statut: ppublish

Résumé

An increasing number of research reports are describing modifications of the E3 ligand, in particular, cereblon (CRBN) ligands, to improve the chemical and metabolic stabilities as well as the physical properties of PROTACs. In this study, phenyl-glutarimide (PG) and 6-fluoropomalidomide (6-F-POM), recently used as CRBN ligands for PROTAC design, were applied to hematopoietic prostaglandin D

Identifiants

DOI: 10.1016/j.bmc.2023.117259 PMID: 37018877
pubmed: 37018877
pii: S0968-0896(23)00107-4
doi: 10.1016/j.bmc.2023.117259
pii:
doi:

Substances chimiques

Ligands 0
Prostaglandins 0
Ubiquitin-Protein Ligases EC 2.3.2.27
CRBN protein, human 0
prostaglandin R2 D-isomerase EC 5.3.99.2
Proteolysis Targeting Chimera 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

117259

Informations de copyright

Copyright © 2023 Elsevier Ltd. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Hinata Osawa (H)

Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan; Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Division of Pharmaceutical Science of Okayama University, 1-1-1 Tsushimanaka, Kita 700-8530, Japan.

Takashi Kurohara (T)

Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.

Takahito Ito (T)

Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan; Graduate School of Medical Life Science, Yokohama City University, 1-7-29, Yokohama, Kanagawa 230-0045, Japan.

Norihito Shibata (N)

Division of Biochemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan.

Yosuke Demizu (Y)

Division of Organic Chemistry, National Institute of Health Sciences, 3-25-26, Tonomachi, Kawasaki, Kanagawa 210-9501, Japan; Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Division of Pharmaceutical Science of Okayama University, 1-1-1 Tsushimanaka, Kita 700-8530, Japan; Graduate School of Medical Life Science, Yokohama City University, 1-7-29, Yokohama, Kanagawa 230-0045, Japan. Electronic address: demizu@nihs.go.jp.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Ligands › CRBN ligand expansion for hematopoietic prostaglandin D
questionsmedicales.fr › Facteurs biologiques › Médiateurs de l'inflammation › Autacoïdes › Éicosanoïdes › Prostaglandines › CRBN ligand expansion for hematopoietic prostaglandin D
questionsmedicales.fr › Métabolisme › Protéolyse › CRBN ligand expansion for hematopoietic prostaglandin D
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Ligases › Ubiquitin-protein ligase complexes › Ubiquitin-protein ligases › CRBN ligand expansion for hematopoietic prostaglandin D
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Indicateurs et réactifs › Réactifs réticulants › Chimère ciblant la protéolyse › CRBN ligand expansion for hematopoietic prostaglandin D