Administration, Oral
Aged
Dichloroacetic Acid
/ administration & dosage
Drug Resistance, Neoplasm
/ genetics
Drugs, Investigational
/ administration & dosage
Female
Genotype
Glutathione Transferase
/ genetics
Half-Life
Humans
Male
Middle Aged
Multiple Myeloma
/ blood
Peripheral Nervous System Diseases
/ chemically induced
Polymorphism, Single Nucleotide
Promoter Regions, Genetic
/ genetics
Prospective Studies
Protein Kinase Inhibitors
/ administration & dosage
Pyruvate Dehydrogenase Acetyl-Transferring Kinase
/ antagonists & inhibitors
Chemotherapy
clinical pharmacology
drug metabolism
genetic polymorphism
toxicology
Journal
Pharmacology research & perspectives
ISSN: 2052-1707
Titre abrégé: Pharmacol Res Perspect
Pays: United States
ID NLM: 101626369
Informations de publication
Date de publication:
12 2019
12 2019
Historique:
received:
02
05
2019
revised:
08
08
2019
accepted:
29
08
2019
entrez:
19
10
2019
pubmed:
19
10
2019
medline:
7
7
2020
Statut:
epublish
Résumé
Dichloroacetate (DCA) is an investigational drug targeting the glycolytic hallmark of cancer by inhibiting pyruvate dehydrogenase kinases (PDK). It is metabolized by GSTZ1, which has common polymorphisms altering enzyme or promoter activity. GSTZ1 is also irreversibly inactivated by DCA. In the first clinical trial of DCA in a hematological malignancy, DiCAM (DiChloroAcetate in Myeloma), we have examined the relationship between DCA concentrations,
Identifiants
pubmed: 31624634
doi: 10.1002/prp2.526
pii: PRP2526
pmc: PMC6783648
doi:
Substances chimiques
Drugs, Investigational
0
Protein Kinase Inhibitors
0
Pyruvate Dehydrogenase Acetyl-Transferring Kinase
0
Dichloroacetic Acid
9LSH52S3LQ
GSTZ1 protein, human
EC 2.5.1.-
Glutathione Transferase
EC 2.5.1.18
Types de publication
Clinical Trial, Phase II
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
e00526Commentaires et corrections
Type : CommentIn
Informations de copyright
© 2019 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics.
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