フォスフォリピドの代謝産物1-パルミトイル-リソフォファディチルコレインは,ヒトのエーテル・ア・ゴー・ゴー関連遺伝子 (HERG) K(+) チャンネル機能を強化する
Circulation
|November 28, 2001
まとめ
リソファスファティディルコリン (LPC) は,ヒトのエーテル・ア・ゴー・ゴー関連遺伝子 (HERG) チャンネル電流を強化し,潜在的に心律不整に寄与します. この発見は,心不全性疾患における心律乱発達の新たなメカニズムを明らかにしている.
科学分野:
- バイオケミストリー バイオケミストリー
- 心血管生理学 心血管の生理学
- 分子生物学は分子生物学である.
背景:
- リスオファスファティディルコリン (LPC) は,心不全組織に蓄積する.
- LPCは心律不整に関与しているが,そのメカニズムは不明である.
研究 の 目的:
- 1-palmitoyl-LPC (Pal-LPC) がヒトのエーテル・ア・ゴー・ゴー関連遺伝子 (HERG) チャンネル電流に及ぼす影響を調査する.
主な方法:
- HERG.を発現するヒト胚性腎臓 (HEK) 細胞の全細胞パッチクランプ技術
- Pal-LPCの適用とHERG電流 (I(HERG)) 変化の評価.
主要な成果:
- Pal-LPCは,一貫して,可逆的に増加した I ((HERG).
- この薬は,HERGの不活性化曲線を,よりポジティブなポテンシャルにシフトさせた.
- Pal-LPCは,I ((HERG) のアクティベーション電圧依存性を変化させなかった.
結論:
- HERG電流は,Pal-LPC.のような天然物質によって強化することができます.
- I ((HERG) の増加は,K+の損失と異常な電気生理学につながる可能性があります.
- HERGに対するPal-LPCの作用は,心不全の心臓における不律に寄与する可能性があります.
さらに関連する動画
08:49Fluorescence-Based Measurements of Phosphatidylserine/Phosphatidylinositol 4-Phosphate Exchange Between Membranes
Published on: March 14, 2021
4.5K
10:41Capturing the Interaction Kinetics of an Ion Channel Protein with Small Molecules by the Bio-layer Interferometry Assay
Published on: March 7, 2018
8.5K
関連する概念動画
Synthesis of Phosphatidylcholine in the ER Membrane
3.8K
The ER synthesizes lipids for building cell membranes and performing cellular functions such as energy storage and signaling. The lipid synthesis machinery embedded in the ER membrane primarily collects all reactants from the cytosol. Following synthesis, the secretory pathway and the ER contact sites distribute these lipids to other cellular organelles. Additionally, the energy-rich triacylglycerides are transported from the ER via lipid droplets.
The major components of all eukaryotic cell...
The major components of all eukaryotic cell...
3.8K
IP3/DAG Signaling Pathway
13.6K
Membrane lipids such as phosphatidylinositol (PI) are precursors for several membrane-bound and soluble second messengers. Specific kinases phosphorylate PI and produce phosphorylated inositol phospholipids. One such inositol phospholipids are the phosphatidylinositol-4,5 bisphosphate [PI(4,5)P2], present in the inner half of the lipid bilayer. Upon ligand binding, GPCR stimulates Gq proteins to turn on phospholipase Cꞵ. Activated phospholipase Cꞵ cleaves PI(4,5)P2 and...
13.6K
Phosphoinositides and PIPs
9.8K
Phosphoinositides are a group of phospholipids containing a glycerol backbone with two fatty acid chains and a phosphate attached to a myoinositol sugar ring. The inositol head group extends into the cytoplasm, where it is modified by adding phosphate groups to form phosphatidylinositol phosphates or PIPs.
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
Different phosphoinositides are synthesized and recruited on the cytosolic face of the plasma membrane. The localization of specific phosphoinositides concentrated in separate membrane...
9.8K
Amplifying Signals via Second Messengers
7.8K
Many receptor binding ligands are hydrophilic; they do not cross the cell membrane but bind to cell-surface receptors. Thus, their message must be relayed by second messengers present in the cell cytoplasm. There are several second messenger pathways, each with its own way of relaying information. For example, the G protein-coupled receptors can activate both phosphoinositol and cyclic AMP (cAMP) second messenger pathways. The phosphoinositol pathway is active when the receptor induces...
7.8K
G-Protein Gated Ion Channels
5.3K
GPCRs are primarily responsible for our sense of smell, taste, and vision. The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
Sensory...
5.3K
cAMP-dependent Protein Kinase Pathways
7.5K
Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
7.5K
