TY  - JOUR
AU  - Taher, Ali T.
AU  - Viprakasit, Vip
AU  - Cappellini, Maria Domenica
AU  - Kraus, Dominik
AU  - Cech, Patrick
AU  - Volz, Dietmar
AU  - Winter, Erica
AU  - Nave, Stephane
AU  - Dukart, Juergen
AU  - Khwaja, Omar
AU  - Koerner, Annette
AU  - Hermosilla, Ricardo
AU  - Brugnara, Carlo
TI  - Haematological effects of oral administration of bitopertin, a glycine transport inhibitor, in patients with non‐transfusion‐dependent β‐thalassaemia
JO  - British journal of haematology
VL  - 194
IS  - 2
SN  - 1365-2141
CY  - Oxford [u.a.]
PB  - Wiley-Blackwell
M1  - FZJ-2021-02896
SP  - 474–481
PY  - 2021
AB  - 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
LB  - PUB:(DE-HGF)16
C6  - pmid:33931857
UR  - <Go to ISI:>//WOS:000646154400001
DO  - DOI:10.1111/bjh.17479
UR  - https://juser.fz-juelich.de/record/893884
ER  -