Design and Discovery of

Animals Antineoplastic Agents / chemistry Drug Design Drug Discovery / methods Humans Molecular Docking Simulation / methods Mutation / drug effects Protein Kinase Inhibitors / chemistry Proto-Oncogene Proteins B-raf / antagonists & inhibitors Xenograft Model Antitumor Assays / methods

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:
12 03 2020
Historique:
pubmed: 7 5 2019
medline: 20 8 2020
entrez: 7 5 2019
Statut: ppublish

Résumé

Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling, downstream of activated RAS, and the poor overall kinase selectivity of putative RAF inhibitors. Herein, we describe

Identifiants

DOI: 10.1021/acs.jmedchem.9b00161 PMID: 31059256
pubmed: 31059256
doi: 10.1021/acs.jmedchem.9b00161
doi:

Substances chimiques

Antineoplastic Agents 0
Protein Kinase Inhibitors 0
Proto-Oncogene Proteins B-raf EC 2.7.11.1

Types de publication

News

Langues

eng

Sous-ensembles de citation

IM

Pagination

2013-2027

Auteurs

Savithri Ramurthy (S)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.
ORCID: 0000-0002-2444-5309

Benjamin R Taft (BR)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Robert J Aversa (RJ)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.
ORCID: 0000-0002-9873-4381

Paul A Barsanti (PA)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Matthew T Burger (MT)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Yan Lou (Y)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Gisele A Nishiguchi (GA)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Alice Rico (A)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Lina Setti (L)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Aaron Smith (A)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Sharadha Subramanian (S)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Victoriano Tamez (V)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Huw Tanner (H)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Lifeng Wan (L)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Cheng Hu (C)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Brent A Appleton (BA)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Mulugeta Mamo (M)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Laura Tandeske (L)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

John E Tellew (JE)

Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Shenlin Huang (S)

Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Qin Yue (Q)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Apurva Chaudhary (A)

Process Research and Development, Chemical and Analytical Development, Novartis Institute for Biomedical Research, One Health Plaza, East Hanover, New Jersey 07936, United States.

Hung Tian (H)

Technical Research & Development, Global Drug Development, Novartis Pharmaceuticals Corp., One Health Plaza, East Hanover, New Jersey 07936, United States.

Raman Iyer (R)

Technical Research & Development, Global Drug Development, Novartis Pharmaceuticals Corp., One Health Plaza, East Hanover, New Jersey 07936, United States.

A Quamrul Hassan (AQ)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Lesley A Mathews Griner (LA)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Laura R La Bonte (LR)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Vesselina G Cooke (VG)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Anne Van Abbema (A)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Hanne Merritt (H)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Kalyani Gampa (K)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Fei Feng (F)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Jing Yuan (J)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Yuji Mishina (Y)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Yingyun Wang (Y)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Jacob R Haling (JR)

Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Sepideh Vaziri (S)

Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

Mohammad Hekmat-Nejad (M)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Valery Polyakov (V)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Richard Zang (R)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Vijay Sethuraman (V)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Payman Amiri (P)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

Mallika Singh (M)

Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States.

William R Sellers (WR)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Emma Lees (E)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Wenlin Shao (W)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Michael P Dillon (MP)

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

Darrin D Stuart (DD)

Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Design and Discovery of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Antinéoplasiques › Design and Discovery of
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Design and Discovery of
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Design and Discovery of
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Design and Discovery of
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Design and Discovery of
questionsmedicales.fr › Phénomènes génétiques › Variation génétique › Mutation › Design and Discovery of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Design and Discovery of
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines tumorales › Protéines oncogènes › Protéines proto-oncogènes › Kinases raf › Protéines proto-oncogènes B-raf › Design and Discovery of
questionsmedicales.fr › Techniques d'investigation › Transplantation tumorale › Tests d'activité antitumorale sur modèle de xénogreffe › Design and Discovery of