Development of Telintra as an Inhibitor of Glutathione S-Transferase P.
Handb Exp Pharmacol
; 264: 71-91, 2021.
Article
em En
| MEDLINE
| ID: mdl-32767141
ABSTRACT
Glutathione S-transferase P (GSTP) is a component of a complex series of pathways that provide cellular redox homeostasis. It is an abundant protein in certain tumors and is over-expressed in cancer drug resistance. It has diverse cellular functions that include, thiolase activities with small electrophilic agents or susceptible cysteine residues on the protein to mediate S-glutathionylation, and chaperone binding with select protein kinases. Preclinical and clinical testing of a nanomolar inhibitor of GSTP, TLK199 (Telintra; Ezatiostat) has indicated a role for the enzyme in hematopoiesis and utility for the drug in the treatment of patients with myelodysplastic syndrome.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Glutationa Transferase
/
Neoplasias
Limite:
Humans
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article