Target type: biologicalprocess
The movement of a population of phospholipid molecules from one leaflet of the plasma membrane bilayer to the opposite leaflet, resulting in loss of lipid asymmetry and surface exposure of phosphatidylserine (PS) and phosphatidylethanolamine (PE). [GOC:cjm, PMID:20043909, PMID:20302864]
Plasma membrane phospholipid scrambling is a critical process in cellular signaling and membrane trafficking. It involves the rapid redistribution of phospholipids within the plasma membrane, specifically the movement of phosphatidylserine (PS) from the inner leaflet to the outer leaflet. This translocation typically occurs in response to various stimuli, including apoptotic signals, oxidative stress, and calcium influx.
The key enzyme responsible for phospholipid scrambling is scramblase. Scramblase is a transmembrane protein that facilitates the bidirectional movement of phospholipids across the membrane bilayer, independent of ATP hydrolysis. This means that scrambling is a passive process, driven by the concentration gradient of phospholipids.
When scramblase is activated, it allows the movement of PS, normally confined to the inner leaflet of the plasma membrane, to the outer leaflet. This exposes PS on the cell surface, which serves as a signal for various cellular processes. For example, in apoptosis, the exposure of PS on the outer leaflet acts as an "eat me" signal, attracting phagocytes to engulf the dying cell.
Phospholipid scrambling also plays a role in membrane fusion and vesicle trafficking. The redistribution of phospholipids can influence the curvature and fluidity of the membrane, facilitating the formation of vesicles and their fusion with other membranes.
The regulation of scramblase activity is complex and involves various signaling pathways. Calcium ions play a significant role in activating scramblase. Other factors, such as phosphorylation and interactions with other proteins, can also modulate scramblase activity.
In summary, plasma membrane phospholipid scrambling is a dynamic process that involves the redistribution of phospholipids, primarily PS, across the membrane bilayer. This process is regulated by various stimuli and plays a critical role in cellular signaling, membrane trafficking, and apoptosis.'
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Protein | Definition | Taxonomy |
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P2X purinoceptor 7 | A P2X purinoceptor 7 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q99572] | Homo sapiens (human) |
Compound | Definition | Classes | Roles |
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oxatomide | oxatomide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one substituted by a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group at position 1. It is an anti-allergic drug. oxatomide: structure; an anti-allergic & an anti-asthmatic | benzimidazoles; diarylmethane; N-alkylpiperazine | anti-allergic agent; anti-inflammatory agent; geroprotector; H1-receptor antagonist; serotonergic antagonist |
pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid | 5'-phosphopyridoxal-6-azobenzene-2,4-disulfonic acid : An arenesulfonic acid that is pyridoxal 5'-phosphate carrying an additional 2,4-disulfophenylazo substituent at position 6. pyridoxal phosphate-6-azophenyl-2',4'-disulfonic acid: a novel antagonist that selectively blocks P2 purinoceptor receptors; a useful tool to study co-transmission in tissues when ATP and coexisting neurotransmitters act in concert | arenesulfonic acid; azobenzenes; methylpyridines; monohydroxypyridine; organic phosphate; pyridinecarbaldehyde | purinergic receptor P2X antagonist |
suramin | suramin : A member of the class of phenylureas that is urea in which each of the amino groups has been substituted by a 3-({2-methyl-5-[(4,6,8-trisulfo-1-naphthyl)carbamoyl]phenyl}carbamoyl)phenyl group. An activator of both the rabbit skeletal muscle RyR1 and sheep cardiac RyR2 isoform ryanodine receptor channels, it has been used for the treatment of human African trypanosomiasis for over 100 years. Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties. | naphthalenesulfonic acid; phenylureas; secondary carboxamide | angiogenesis inhibitor; antinematodal drug; antineoplastic agent; apoptosis inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; GABA antagonist; GABA-gated chloride channel antagonist; purinergic receptor P2 antagonist; ryanodine receptor agonist; trypanocidal drug |
alpha,beta-methyleneadenosine 5'-triphosphate | alpha,beta-methyleneadenosine 5'-triphosphate: do not confuse with beta,gamma-methylene ATP; RN given refers to parent cpd | nucleoside triphosphate analogue | |
sb 203580 | imidazoles; monofluorobenzenes; pyridines; sulfoxide | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent | |
8-azidoadenosine 5'-triphosphate | |||
6-thioinosine-5'-triphosphate | organic molecule | ||
mrs2159 | MRS2159: an antagonist of both P2X1 and P2X7 receptors | ||
imd 0354 | N-(3,5-bis(trifluoromethyl)phenyl)-5-chloro-2-hydroxybenzamide: a cardioprotective agent that inhibits IkappaB kinase beta (IKKbeta); structure in first source | benzamides | |
kn 62 | KN 62: inhibitor of Ca/calmodulin-dependent protein kinase II | piperazines | |
az 11645373 | AZ 11645373: InChIKey: VQEHBLGYANQWEA-UHFFFAOYSA-N | ||
az10606120 | AZ10606120: a P2X7 receptor antagonist | ||
ce 224,535 | CE 224,535: structure in first source | ||
a-438079 | |||
af 353 | 5-(5-iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine: a P2X3 and P2X2/3 receptor antagonist; structure in first source | ||
gsk1482160 | |||
a-839977 | A-839977: a selective P2X7 receptor antagonist, analgesic; structure in first source | ||
jnj-47965567 | JNJ-47965567: a P2X7 purinergic receptor antagonist; structure in first source | ||
mk-8742 | elbasvir : A complex organic heterotetracyclic compound that is a hepatitis C virus nonstructural protein 5A inhibitor used in combination with grazoprevir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults. elbasvir: inhibits NS5A protein of hepatitis C virus | carbamate ester; imidazoles; L-valine derivative; N-acylpyrrolidine; organic heterotetracyclic compound; ring assembly | antiviral drug; hepatitis C virus nonstructural protein 5A inhibitor; hepatoprotective agent |