%0 Journal Article
%A Taher, Ali T.
%A Viprakasit, Vip
%A Cappellini, Maria Domenica
%A Kraus, Dominik
%A Cech, Patrick
%A Volz, Dietmar
%A Winter, Erica
%A Nave, Stephane
%A Dukart, Juergen
%A Khwaja, Omar
%A Koerner, Annette
%A Hermosilla, Ricardo
%A Brugnara, Carlo
%T Haematological effects of oral administration of bitopertin, a glycine transport inhibitor, in patients with non‐transfusion‐dependent β‐thalassaemia
%J British journal of haematology
%V 194
%N 2
%@ 1365-2141
%C Oxford [u.a.]
%I Wiley-Blackwell
%M FZJ-2021-02896
%P 474–481
%D 2021
%X 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
%F PUB:(DE-HGF)16
%9 Journal Article
%$ pmid:33931857
%U <Go to ISI:>//WOS:000646154400001
%R 10.1111/bjh.17479
%U https://juser.fz-juelich.de/record/893884