Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor

Cell Line, Tumor Dose-Response Relationship, Drug Drug Evaluation, Preclinical Enzyme Inhibitors / chemical synthesis Humans Indoles / chemical synthesis Models, Molecular Molecular Structure Phosphoglycerate Dehydrogenase / antagonists & inhibitors Serine / antagonists & inhibitors Structure-Activity Relationship

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 09 2019
Historique:
pubmed: 1 8 2019
medline: 1 7 2020
entrez: 1 8 2019
Statut: ppublish

Résumé

Phosphoglycerate dehydrogenase (PHGDH) is known to be the rate-limiting enzyme in the serine synthesis pathway in humans. It converts glycolysis-derived 3-phosphoglycerate to 3-phosphopyruvate in a co-factor-dependent oxidation reaction. Herein, we report the discovery of

Identifiants

DOI: 10.1021/acs.jmedchem.9b00718 PMID: 31365252
pubmed: 31365252
doi: 10.1021/acs.jmedchem.9b00718
doi:

Substances chimiques

Enzyme Inhibitors 0
Indoles 0
Serine 452VLY9402
Phosphoglycerate Dehydrogenase EC 1.1.1.95

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

7976-7997

Auteurs

Harald Weinstabl (H)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.
ORCID: 0000-0003-1308-2730

Matthias Treu (M)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Joerg Rinnenthal (J)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Stephan K Zahn (SK)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Peter Ettmayer (P)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.
ORCID: 0000-0002-8422-2625

Gerd Bader (G)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Georg Dahmann (G)

Boehringer Ingelheim Pharma GmbH & Co. KG , Birkendorfer Str. 65 , 88400 Biberach an der Riß , Germany.

Dirk Kessler (D)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Klaus Rumpel (K)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Nikolai Mischerikow (N)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Fabio Savarese (F)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Thomas Gerstberger (T)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Moriz Mayer (M)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Andreas Zoephel (A)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Renate Schnitzer (R)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Wolfgang Sommergruber (W)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Paola Martinelli (P)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Heribert Arnhof (H)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Biljana Peric-Simov (B)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Karin S Hofbauer (KS)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Géraldine Garavel (G)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Yvonne Scherbantin (Y)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Sophie Mitzner (S)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Thomas N Fett (TN)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Guido Scholz (G)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Jens Bruchhaus (J)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Michelle Burkard (M)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Roland Kousek (R)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Tuncay Ciftci (T)

Boehringer Ingelheim Pharma GmbH & Co. KG , Birkendorfer Str. 65 , 88400 Biberach an der Riß , Germany.

Bernadette Sharps (B)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Andreas Schrenk (A)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Christoph Harrer (C)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Daniela Haering (D)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Bernhard Wolkerstorfer (B)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Xuechun Zhang (X)

Shanghai ChemPartner Co., LTD. , No. 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , China.

Xiaobing Lv (X)

Shanghai ChemPartner Co., LTD. , No. 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , China.

Alicia Du (A)

Shanghai ChemPartner Co., LTD. , No. 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , China.

Dongyang Li (D)

Shanghai ChemPartner Co., LTD. , No. 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , China.

Yali Li (Y)

Shanghai ChemPartner Co., LTD. , No. 5 Building, 998 Halei Road, Zhangjiang Hi-Tech Park, Pudong New Area , Shanghai 201203 , China.

Jens Quant (J)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Mark Pearson (M)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Darryl B McConnell (DB)

Boehringer Ingelheim RCV GmbH & Co. KG , Dr.-Boehringer-Gasse 5-11 , 1121 Vienna , Austria.

Articles similaires

[Redispensing of expensive oral anticancer medicines: a practical application].

Lisanne N van Merendonk, Kübra Akgöl, Bastiaan Nuijen
1.00
Humans Antineoplastic Agents Administration, Oral Drug Costs Counterfeit Drugs

Smoking Cessation and Incident Cardiovascular Disease.

Jun Hwan Cho, Seung Yong Shin, Hoseob Kim et al.
1.00
Humans Male Smoking Cessation Cardiovascular Diseases Female

Evaluation of Low-Value Services Across Major Medicare Advantage Insurers and Traditional Medicare.

Ciara Duggan, Adam L Beckman, Ishani Ganguli et al.
1.00
Humans United States Aged Cross-Sectional Studies Medicare Part C

Effectiveness of Virtual Yoga for Chronic Low Back Pain: A Randomized Clinical Trial.

Hallie Tankha, Devyn Gaskins, Amanda Shallcross et al.
1.00
Humans Yoga Low Back Pain Female Male

Classifications MeSH

questionsmedicales.fr › Cellules › Cellules cultivées › Cellules cancéreuses en culture › Lignée cellulaire tumorale › Intracellular Trapping of the Selective...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Intracellular Trapping of the Selective...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Intracellular Trapping of the Selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Intracellular Trapping of the Selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Intracellular Trapping of the Selective...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indoles › Intracellular Trapping of the Selective...
questionsmedicales.fr › Techniques d'investigation › Modèles théoriques › Modèles moléculaires › Intracellular Trapping of the Selective...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Intracellular Trapping of the Selective...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Alcohol oxidoreductases › Carbohydrate dehydrogenases › Phosphoglycerate dehydrogenase › Intracellular Trapping of the Selective...
questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › Acides aminés neutres › Sérine › Intracellular Trapping of the Selective...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Intracellular Trapping of the Selective...