Phenotypic Discovery of Triazolo[1,5-

Bone Morphogenetic Protein 2 / metabolism Bone Morphogenetic Proteins / drug effects Cell Differentiation Osteogenesis Quinazolines / pharmacology Smad Proteins / metabolism Triazoles / pharmacology

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:
24 11 2022
Historique:
pubmed: 9 11 2022
medline: 26 11 2022
entrez: 8 11 2022
Statut: ppublish

Résumé

Phenotypic drug discovery (PDD) continues to fuel the research and development pipelines with first-in-class therapeutic modalities, but success rates critically depend on the quality of the underlying model system. Here, we employed a stem cell-based approach for the target-agnostic, yet pathway-centric discovery of small-molecule cytokine signaling activators to act as morphogens during development and regeneration. Unbiased screening identified triazolo[1,5-

Identifiants

DOI: 10.1021/acs.jmedchem.2c01199 PMID: 36346705
pubmed: 36346705
doi: 10.1021/acs.jmedchem.2c01199
doi:

Substances chimiques

Bone Morphogenetic Protein 2 0
Bone Morphogenetic Proteins 0
Quinazolines 0
Smad Proteins 0
Triazoles 0

Types de publication

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

Langues

eng

Sous-ensembles de citation

IM

Pagination

15263-15281

Auteurs

Fabian Wesseler (F)

Faculty of Chemistry and Chemical Biology, Technical University Dortmund, Otto-Hahn-Strasse 6, 44227Dortmund, Germany.
Compound Management and Screening Center COMAS, Max Planck Institute of Molecular Physiology (MPI), 44227Dortmund, Germany.
Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Christian-Albrechts University of Kiel, Gutenbergstrasse 76, 24118Kiel, Germany.

Stefan Lohmann (S)

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Christian-Albrechts University of Kiel, Gutenbergstrasse 76, 24118Kiel, Germany.

Daniel Riege (D)

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Christian-Albrechts University of Kiel, Gutenbergstrasse 76, 24118Kiel, Germany.

Jonas Halver (J)

Faculty of Chemistry and Chemical Biology, Technical University Dortmund, Otto-Hahn-Strasse 6, 44227Dortmund, Germany.

Aileen Roth (A)

Department of General and Visceral Surgery, University Hospital Ulm, Albert-Einstein-Allee 23, 89081Ulm, Germany.

Christian Pichlo (C)

Department of Chemistry, University of Cologne, Greinstraße 6, 50939Cologne, Germany.

Sabrina Weber (S)

Institute of Biological and Chemical Systems - Biological Information Processing at Karlsruhe Institute of Technology (KIT), 76344Eggenstein-Leopoldshafen, Germany.

Masanari Takamiya (M)

Institute of Biological and Chemical Systems - Biological Information Processing at Karlsruhe Institute of Technology (KIT), 76344Eggenstein-Leopoldshafen, Germany.

Eva Müller (E)

Department of Orthopedic Surgery, Otto-von-Guericke University, 39120Magdeburg, Germany.

Jana Ketzel (J)

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Christian-Albrechts University of Kiel, Gutenbergstrasse 76, 24118Kiel, Germany.

Jana Flegel (J)

Faculty of Chemistry and Chemical Biology, Technical University Dortmund, Otto-Hahn-Strasse 6, 44227Dortmund, Germany.

Adrian Gihring (A)

Department of General and Visceral Surgery, University Hospital Ulm, Albert-Einstein-Allee 23, 89081Ulm, Germany.

Sepand Rastegar (S)

Institute of Biological and Chemical Systems - Biological Information Processing at Karlsruhe Institute of Technology (KIT), 76344Eggenstein-Leopoldshafen, Germany.

Jessica Bertrand (J)

Department of Orthopedic Surgery, Otto-von-Guericke University, 39120Magdeburg, Germany.

Ulrich Baumann (U)

Department of Chemistry, University of Cologne, Greinstraße 6, 50939Cologne, Germany.

Uwe Knippschild (U)

Department of General and Visceral Surgery, University Hospital Ulm, Albert-Einstein-Allee 23, 89081Ulm, Germany.

Christian Peifer (C)

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Christian-Albrechts University of Kiel, Gutenbergstrasse 76, 24118Kiel, Germany.
ORCID: 0000-0003-1532-7826

Sonja Sievers (S)

Compound Management and Screening Center COMAS, Max Planck Institute of Molecular Physiology (MPI), 44227Dortmund, Germany.
Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227Dortmund, Germany.

Herbert Waldmann (H)

Faculty of Chemistry and Chemical Biology, Technical University Dortmund, Otto-Hahn-Strasse 6, 44227Dortmund, Germany.
Max-Planck-Institute of Molecular Physiology, Otto-Hahn-Strasse 11, 44227Dortmund, Germany.
ORCID: 0000-0002-9606-7247

Dennis Schade (D)

Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Christian-Albrechts University of Kiel, Gutenbergstrasse 76, 24118Kiel, Germany.
Partner Site Kiel, DZHK, German Center for Cardiovascular Research, 24105Kiel, Germany.
ORCID: 0000-0002-5515-1821

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Classifications MeSH

questionsmedicales.fr › Facteurs biologiques › Protéines et peptides de signalisation intercellulaire › Protéines de la superfamille du TGF bêta › Protéines morphogénétiques osseuses › Protéine morphogénétique osseuse de type 2 › Phenotypic Discovery of Triazolo[1,5-
questionsmedicales.fr › Facteurs biologiques › Protéines et peptides de signalisation intercellulaire › Protéines de la superfamille du TGF bêta › Protéines morphogénétiques osseuses › Phenotypic Discovery of Triazolo[1,5-
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Différenciation cellulaire › Phenotypic Discovery of Triazolo[1,5-
questionsmedicales.fr › Phénomènes physiologiques de l'appareil locomoteur et du système nerveux › Phénomènes physiologiques du système locomoteur › Développement locomoteur › Biominéralisation › Développement osseux › Ostéogenèse › Phenotypic Discovery of Triazolo[1,5-
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinazolines › Phenotypic Discovery of Triazolo[1,5-
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Facteurs de transcription › Protéines Smad › Phenotypic Discovery of Triazolo[1,5-
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Triazoles › Phenotypic Discovery of Triazolo[1,5-