GlyT
GlyTs mediate the uptake of glycine from the extracellular space into the cytosol. They belong to a large family of NaC/ClK-dependent transporter proteins, which includes transporters for monoamines (serotonin, norepinephrine and dopamine) and the inhibitory neurotransmitter g-aminobutyric acid (GABA). These polytopic membrane proteins share a common transmembrane topology with 12 transmembrane domains (TMDs) connected by six extracellular and five intracellular loops. Both GlyTs exist in multiple splice variants: three GlyT2 isoforms (a, b, c) differ in the N-terminal region, whereas three N-terminal (a, b, c) and two C-terminal (d, e) exons have been reported to generate different variants of GlyT1. The transporters GLYTla, GLYTlb and GLYTlc have been isolated from the CNS of both rodents and humans. Two isoforms of the GLYT2 gene product have been reported and have been named GLYT2a and GLYT2b. The uptake of glycine mediated by GlyTs is energetically coupled to the transmembrane sodium gradient maintained by the NaC/KC-ATPase. Pharmacological evidence indicates that GLYT 1 transports glycine in the cerebral cortex, but that in the cerebellum, it shares this function with GLYT2.
References
1.Eulenburg V, et al. Trends Biochem Sci. 2005;30(6):325–333.
2.Tunnicliff G. J Biomed Sci. 2003;10(1):30–36.
References
1.Eulenburg V, et al. Trends Biochem Sci. 2005;30(6):325–333.
2.Tunnicliff G. J Biomed Sci. 2003;10(1):30–36.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(62)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(64)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Potassium Channel(0)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
GlyT
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PF-03463275 B
产品货号 : M35572
cas no: 1173239-39-8
PF-03463275 是一种中枢神经系统渗透性、具有口服活性、选择性、竞争性甘氨酸转运蛋白-1 (GlyT1) 可逆抑制剂,Ki 为 11.6 nM。PF-03463275 有可能用于精神分裂症的研究。 -
Iclepertin
产品货号 : M34912
cas no: 1421936-85-7
Iclepertin (BI-425809) 是一种有效、选择性且具有口服活性的甘氨酸转运蛋白 1 (GlyT1) 抑制剂。Iclepertin 对 GlyT2 无活性。Iclepertin 可用于阿尔茨海默病和精神分裂症研究。 -
ALX-1393
产品货号 : M33260
cas no: 949164-09-4
ALX-1393 是一种选择性 GlyT2 抑制剂, 对大鼠急性疼痛模型中的热,机械和化学刺激具有抗伤害作用。 -
Org 25543 hydrochloride
产品货号 : M27512
cas no: 495076-64-7
Org 25543 Hydrochloride 是一种有效的选择性甘氨酸转运蛋白 2 型 (GlyT2) 抑制剂(对于 hGlyT2,IC50 = 16 nM)。在 CHO 细胞的甘氨酸摄取测定中,GlyT1 或 56 个其他常见生物靶标 (≥ 100 μM) 无活性。 -
LY2365109 hydrochloride
产品货号 : M26285
cas no: 1779796-27-8
LY2365109 盐酸盐是一种有效的选择性 GlyT1 抑制剂,在过度表达 hGlyT1a 的细胞中摄取甘氨酸的 IC50 为 15.8 nM。