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Literature summary for 3.1.4.11 extracted from

  • Thyagarajan, B.; Benn, B.S.; Christakos, S.; Rohacs, T.
    Phospholipase C-mediated regulation of transient receptor potential vanilloid 6 channels: implications in active intestinal Ca2+ transport (2009), Mol. Pharmacol., 75, 608-616.
    View publication on PubMedView publication on EuropePMC
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Application

Application Comment Organism
pharmacology showing that pharmacological inhibition of PLC enhances intestinal Ca2+ transport. This raises the possibility that pharmacological tools targeting PLC can be used to enhance intestinal Ca2+ absorption. Given the prevalence of osteoporosis, which generally comes with negative Ca2+ balance, PLC can be a clinically relevant pharmacological target in the future Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(6-((17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione U73122, also inhibits Ca2+-induced inactivation of TRPV6 Homo sapiens
edelfosine ET-18-OCH3, also inhibits Ca2+-induced inactivation of TRPV6 Homo sapiens
additional information inactive analog U73343 also used Homo sapiens
U-73122 PLC inhibitor inhibits Ca2+-induced inactivation of TRPV6 in patch-clamp experiments Homo sapiens
U-73343 inactive analog of U-73122 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ Ca2+ flowing activates phospholipase C leading to the depletion of phosphatidylinositol 4,5-bisphosphate and formation of inositol 1,4,5-trisphosphate in TRPV6-expressing cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
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Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
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 Homo sapiens
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intestine TRPV6-expressing cell Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
phosphatidylinositol 4,5-bisphosphate demonstration of the role of PLC in Ca2+-induced inactivation of TRPV6 Homo sapiens inositol 1,4,5-trisphosphate
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