Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.

Acrylamides Aniline Compounds / pharmacology Carcinoma, Non-Small-Cell Lung / pathology Drug Resistance, Neoplasm ErbB Receptors / genetics Humans Indoles Lung Neoplasms / pathology Mutation Protein Kinase Inhibitors / pharmacology Pyrimidines

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:
13 10 2022
Historique:
pubmed: 1 10 2022
medline: 15 10 2022
entrez: 30 9 2022
Statut: ppublish

Résumé

Addressing resistance to third-generation EGFR TKIs such as osimertinib via the EGFR

Identifiants

DOI: 10.1021/acs.jmedchem.2c00893 PMID: 36178776
pubmed: 36178776
doi: 10.1021/acs.jmedchem.2c00893
doi:

Substances chimiques

Acrylamides 0
Aniline Compounds 0
Indoles 0
Protein Kinase Inhibitors 0
Pyrimidines 0
osimertinib 3C06JJ0Z2O
EGFR protein, human EC 2.7.10.1
ErbB Receptors EC 2.7.10.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

13052-13073

Auteurs

Ulrike Obst-Sander (U)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Antonio Ricci (A)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Bernd Kuhn (B)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.
ORCID: 0000-0002-4301-562X

Thomas Friess (T)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Discovery Oncology, Roche Innovation Center Munich, Roche Diagnostics GmbH, Nonnenwald 2, Penzberg82377, Germany.

Philipp Koldewey (P)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Andreas Kuglstatter (A)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

David Hewings (D)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.
ORCID: 0000-0001-9451-8959

Annick Goergler (A)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Sandra Steiner (S)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Daniel Rueher (D)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Marie-Paule Imhoff (MP)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Noemi Raschetti (N)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Hans-Peter Marty (HP)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Aline Dietzig (A)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Cancer Targeted Therapies, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Caroline Rynn (C)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Pharmaceutical Sciences, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Andreas Ehler (A)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Dominique Burger (D)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Martin Kornacker (M)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Clinical Development Oncology, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Jeannine Petrig Schaffland (JP)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Frank Herting (F)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Discovery Oncology, Roche Innovation Center Munich, Roche Diagnostics GmbH, Nonnenwald 2, Penzberg82377, Germany.

William Pao (W)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

James R Bischoff (JR)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Cancer Targeted Therapies, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Bruno Martoglio (B)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Cancer Targeted Therapies, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.

Yvonne Alice Nagel (Y)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Cancer Targeted Therapies, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.
ORCID: 0000-0003-2296-8058

Georg Jaeschke (G)

F. Hoffmann-La Roche Ltd, Roche Pharmaceutical Research and Early Development, Therapeutic Modalities, Roche Innovation Center Basel, Grenzacherstrasse 124, Basel4070, Switzerland.
ORCID: 0000-0002-9393-6822

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Classifications MeSH

questionsmedicales.fr › Composés chimiques organiques › Acides carboxyliques › Acides acycliques › Acrylates › Acrylamides › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Composés chimiques organiques › Amines › Dérivés de l'aniline › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Maladies de l'appareil respiratoire › Tumeurs de l'appareil respiratoire › Tumeurs du poumon › Tumeurs des bronches › Carcinome bronchogénique › Carcinome pulmonaire non à petites cellules › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Résistance aux substances › Résistance aux médicaments antinéoplasiques › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs peptidiques › Récepteur facteur croissance › Récepteurs ErbB › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indoles › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Maladies de l'appareil respiratoire › Tumeurs de l'appareil respiratoire › Tumeurs du poumon › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Phénomènes génétiques › Variation génétique › Mutation › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Discovery of Novel Allosteric EGFR L858R...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrimidines › Discovery of Novel Allosteric EGFR L858R...