Membrane Transporters/Ion Channels
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Na+/K+ ATPase modulator
Rostafuroxin (PST-2238)是一种哇巴因抑制剂,可对抗特定形式的高血压。
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CFTR modulator
VX-809 (Lumacaftor)是用于治疗囊性纤维化(CF)的第二种口服研究候选化合物,通过促进突变型CFTR(F508del-CFTR)的成熟,从而纠正囊性纤维症中常见的CFTR突变,在fisher大鼠甲状腺细胞中EC50为0.1 μM。
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- Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
- Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
- Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
- Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926
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intracellular Ca2+ handling modulator
Caldaret is an intracellular Ca2+ handling modulator that acts through reverse mode Na+/Ca2+ exchanger inhibition.
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Ca2+ signaling modulator
Astragaloside A是缺氧条件下人脐静脉内皮细胞HIF-1α和通过PI3K/Akt途径血管生成的一种新型调节因子。
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Kv3 potassium channel modulator
AUT1 is a Kv3 potassium channel modulator with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
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AMPA receptors positive allosteric modulator
CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ?? 4.2 nM/63.4 ?? 5.6 nM for GluA2i/GluA2o receptor.
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AMPA receptor positive allosteric modulator
PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.
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AMPAR negative modulator
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8.
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AMPA receptors allosteric modulator
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
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positive AMPAR modulator
CX546 is a selective positive AMPAR modulator; the prototypical ampakine agent.
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AMPA receptor modulator
Farampator是一种AMPA受体正调节剂,它可以改善短期记忆,但会损害情景记忆。
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P-gp modulator
Biricodar dicitrate (VX-710 dicitrate)是P-糖蛋白和MRP-1的调节剂;在多药耐药细胞中显示出有效的化学增敏活性。
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P-gp modulator
LY335979 (Zosuquidar trihydrochloride)是一种强效高选择性P-gp抑制剂。
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- Leo Shen, .et al. A forward genetic screen identifies modifiers of rocaglate responsiveness, Sci Rep, 2021, Sep 16;11(1):18516 PMID: 34531456
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P-glycoprotein/MRP-1 modulator
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
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TRPV1 modulator
MRS1477是TRPV1阳性变构调节剂。
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