Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.

Aminopyridines / pharmacology Antineoplastic Agents / pharmacology Cell Line, Tumor Organic Chemicals Phosphatidylinositol 3-Kinases Phosphoinositide-3 Kinase Inhibitors Protein Kinase Inhibitors / 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:
23 06 2022
Historique:
pubmed: 3 5 2022
medline: 25 6 2022
entrez: 2 5 2022
Statut: ppublish

Résumé

Balanced pan-class I phosphoinositide 3-kinase inhibition as an approach to cancer treatment offers the prospect of treating a broad range of tumor types and/or a way to achieve greater efficacy with a single inhibitor. Taking buparlisib as the starting point, the balanced pan-class I PI3K inhibitor

Identifiants

DOI: 10.1021/acs.jmedchem.2c00267 PMID: 35500094
pubmed: 35500094
doi: 10.1021/acs.jmedchem.2c00267
doi:

Substances chimiques

Aminopyridines 0
Antineoplastic Agents 0
CLR457 0
Organic Chemicals 0
Phosphoinositide-3 Kinase Inhibitors 0
Protein Kinase Inhibitors 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

8345-8379

Auteurs

Robin A Fairhurst (RA)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.
ORCID: 0000-0002-9924-6291

Pascal Furet (P)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Patricia Imbach-Weese (P)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Frédéric Stauffer (F)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.
ORCID: 0000-0003-0918-5147

Heinrich Rueeger (H)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Clive McCarthy (C)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Sebastien Ripoche (S)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Susanne Oswald (S)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Bertrand Arnaud (B)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.
ORCID: 0000-0001-9695-3997

Aline Jary (A)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Michel Maira (M)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Christian Schnell (C)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Daniel A Guthy (DA)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Markus Wartmann (M)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Michael Kiffe (M)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Sandrine Desrayaud (S)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Francesca Blasco (F)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Toni Widmer (T)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Frank Seiler (F)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

Sascha Gutmann (S)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.
ORCID: 0000-0002-4242-8510

Mark Knapp (M)

Novartis Institutes for BioMedical Research, Emeryville, California 94608, United States.

Giorgio Caravatti (G)

Novartis Institutes for BioMedical Research, Basel CH-4002, Switzerland.

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Classifications MeSH

questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyridines › Aminopyridines › Identification of NVP-CLR457 as an Orally...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Antinéoplasiques › Identification of NVP-CLR457 as an Orally...
questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Identification of NVP-CLR457 as an Orally...
questionsmedicales.fr › Composés chimiques organiques › Identification of NVP-CLR457 as an Orally...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Phosphatidylinositol 3-kinases › Identification of NVP-CLR457 as an Orally...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs des phosphoinositide-3 kinases › Identification of NVP-CLR457 as an Orally...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Identification of NVP-CLR457 as an Orally...