Fragment-Based Design of a Potent MAT2a Inhibitor and

Allosteric Site Animals Cell Proliferation Drug Design Enzyme Inhibitors / chemistry Gene Knockout Techniques HCT116 Cells Half-Life Humans Methionine Adenosyltransferase / antagonists & inhibitors Mice Molecular Dynamics Simulation Neoplasms / drug therapy Quinazolines / chemistry Rats S-Adenosylmethionine / metabolism Structure-Activity Relationship Transplantation, Heterologous

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:
27 05 2021

Historique:

pubmed: 27 4 2021

medline: 22 6 2021

entrez: 26 4 2021

Statut: ppublish

Résumé

MAT2a is a methionine adenosyltransferase that synthesizes the essential metabolite

Identifiants

DOI: 10.1021/acs.jmedchem.1c00067 PMID: 33900758

pubmed: 33900758

doi: 10.1021/acs.jmedchem.1c00067

doi:

Substances chimiques

Enzyme Inhibitors 0

Quinazolines 0

S-Adenosylmethionine 7LP2MPO46S

MAT2A protein, human EC 2.5.1.6

Methionine Adenosyltransferase EC 2.5.1.6

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

6814-6826

Auteurs

Claudia De Fusco (C)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0001-8807-4976

Marianne Schimpl (M)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0003-2284-5250

Ulf Börjesson (U)

Discovery Sciences, R&D, AstraZeneca, Gothenburg SE-431 83, Sweden.

Tony Cheung (T)

Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.

Iain Collie (I)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Laura Evans (L)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Priyanka Narasimhan (P)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Christopher Stubbs (C)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Mercedes Vazquez-Chantada (M)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

David J Wagner (DJ)

Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.

ORCID: 0000-0002-5805-930X

Michael Grondine (M)

Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.

Matthew G Sanders (MG)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Sharon Tentarelli (S)

Oncology R&D, AstraZeneca, Boston, Massachusetts 02451, United States.

Elizabeth Underwood (E)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Argyrides Argyrou (A)

Discovery Sciences, R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0003-3141-9122

James M Smith (JM)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0002-6750-265X

James T Lynch (JT)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

Elisabetta Chiarparin (E)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0002-2998-1346

Graeme Robb (G)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0002-4531-4375

Sharan K Bagal (SK)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

James S Scott (JS)

Oncology R&D, AstraZeneca, Cambridge CB4 0WG, United Kingdom.

ORCID: 0000-0002-2263-7024

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Classifications MeSH

questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Sites de fixation › Site allostérique › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Eucaryotes › Animaux › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Phénomènes physiologiques › Croissance et développement › Croissance › Processus de croissance cellulaire › Prolifération cellulaire › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Techniques d'investigation › Techniques génétiques › Ciblage de gène › Techniques de knock-out de gènes › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Cellules HCT116 › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Phénomènes physiques › Temps › Période › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Transferases › Alkyl et aryl transferases › Methionine adenosyltransferase › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de dynamique moléculaire › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Tumeurs › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Quinazolines › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Acides nucléiques, nucléotides et nucléosides › Nucléosides › Ribonucléosides › Adénosine › Adémétionine › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Fragment-Based Design of a Potent MAT2a Inhibitor and

questionsmedicales.fr › Procédures de chirurgie opératoire › Transplantation › Transplantation hétérologue › Fragment-Based Design of a Potent MAT2a Inhibitor and