Discovery of Potent and Selective Receptor-Interacting Serine/Threonine Protein Kinase 2 (RIPK2) Inhibitors for the Treatment of Inflammatory Bowel Diseases (IBDs).

Acetylmuramyl-Alanyl-Isoglutamine / metabolism Humans Inflammatory Bowel Diseases / drug therapy Protein Kinase Inhibitors / chemistry Receptor-Interacting Protein Serine-Threonine Kinase 2 Receptor-Interacting Protein Serine-Threonine Kinases Serine Threonine

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
14 07 2022
Historique:
pubmed: 17 6 2022
medline: 16 7 2022
entrez: 16 6 2022
Statut: ppublish

Résumé

Receptor-interacting serine/threonine protein kinase 2 (RIPK2) has been demonstrated to be a promising target for treating inflammatory diseases. Herein, we describe the discovery and optimization of a series of RIPK2 inhibitors derived from an FLT3 inhibitor, CHMFL-FLT3-165. Compound

Identifiants

DOI: 10.1021/acs.jmedchem.2c00604 PMID: 35709396
pubmed: 35709396
doi: 10.1021/acs.jmedchem.2c00604
doi:

Substances chimiques

Protein Kinase Inhibitors 0
Threonine 2ZD004190S
Serine 452VLY9402
Acetylmuramyl-Alanyl-Isoglutamine 53678-77-6
RIPK2 protein, human EC 2.7.11.1
Receptor-Interacting Protein Serine-Threonine Kinase 2 EC 2.7.11.1
Receptor-Interacting Protein Serine-Threonine Kinases EC 2.7.11.1

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

9312-9327

Auteurs

Xue Yuan (X)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Yong Chen (Y)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Minghai Tang (M)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Yuhan Wei (Y)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Mingsong Shi (M)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Yingxue Yang (Y)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Yanting Zhou (Y)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Tao Yang (T)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Jiang Liu (J)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Kongjun Liu (K)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Dexin Deng (D)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Chufeng Zhang (C)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.

Lijuan Chen (L)

Laboratory of Natural and Targeted Small Molecule Drugs, State Key Laboratory of Biotherapy and Cancer Center and Collaborative Innovation Center of Biotherapy, West China Hospital of Sichuan University, Chengdu 610041, China.
Chengdu Zenitar Biomedical Technology Co., Ltd., Chengdu 610041, China.
ORCID: 0000-0002-8076-163X

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Peptides › Glycopeptides › Acétylmuramyl alanyl isoglutamine › Discovery of Potent and Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of Potent and Selective...
questionsmedicales.fr › Maladies de l'appareil digestif › Maladies gastro-intestinales › Maladies intestinales › Maladies inflammatoires intestinales › Discovery of Potent and Selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Discovery of Potent and Selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protein-Serine-Threonine Kinases › Receptor-Interacting Protein Serine-Threonine Kinases › Receptor-Interacting Protein Serine-Threonine Kinase 2 › Discovery of Potent and Selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protein-Serine-Threonine Kinases › Receptor-Interacting Protein Serine-Threonine Kinases › Discovery of Potent and Selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › Acides aminés neutres › Sérine › Discovery of Potent and Selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › Acides aminés neutres › Thréonine › Discovery of Potent and Selective...