Journal Article

FZJ-2021-02896

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Haematological effects of oral administration of bitopertin, a glycine transport inhibitor, in patients with non‐transfusion‐dependent β‐thalassaemia

Taher, A. T. (Corresponding author) ; Viprakasit, V. ; Cappellini, M. D. ; Kraus, D.Extern* ; Cech, P. ; Volz, D. ; Winter, E. ; Nave, S. ; Dukart, J.FZJ* ; Khwaja, O. ; Koerner, A. ; Hermosilla, R. ; Brugnara, C.

2021
Wiley-Blackwell Oxford [u.a.]

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Please use a persistent id in citations: http://hdl.handle.net/2128/28735  doi:10.1111/bjh.17479

Abstract: Bitopertin is a small molecule selective inhibitor of glycine transporter 1 (GlyT1), initially developed to increase brain extracellular levels of glycine in the vicinity of neuronal N-methyl-D-aspartate receptors for the treatment of schizophrenia. GlyT1, the pharmacological target of bitopertin, is also present as a transmembrane transporter in erythroid cells1 and accounts for 50–55% of glycine uptake in human red blood cells (RBCs).2, 3 Erythroid GlyT1 inhibition by bitopertin leads to reduced intracellular glycine availability, interfering with the first step of haem synthesis, in which 5-aminolevulinate synthase catalyses the condensation reaction between glycine and succinyl-coenzyme A, forming 5-aminolevulinic acid.1

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Contributing Institute(s):

1. Gehirn & Verhalten (INM-7)

Research Program(s):

1. 5252 - Brain Dysfunction and Plasticity (POF4-525) (POF4-525)

Appears in the scientific report 2021

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