Novel Potent Antagonists of Transient Receptor Potential Channel, Vanilloid Subfamily Member 1:  Structure−Activity Relationship of 1,3-Diarylalkyl Thioureas Possessing New Vanilloid Equivalents

2005 ◽  
Vol 48 (18) ◽  
pp. 5823-5836 ◽  
Author(s):  
Young-Ger Suh ◽  
Yong-Sil Lee ◽  
Kyung-Hoon Min ◽  
Ok-Hui Park ◽  
Jin-Kwan Kim ◽  
...  
Keyword(s):  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Transient Receptor Potential Channel ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Subfamily Member ◽  
Structure Activity ◽  
Transient Receptor ◽  
Relationship Of

scholarly journals Discrimination of intracellular calcium store subcompartments using TRPV1 (transient receptor potential channel, vanilloid subfamily member 1) release channel activity

2003 ◽  
Vol 371 (2) ◽  
pp. 341-350 ◽  
Author(s):  
Helen TURNER ◽  
Andrea FLEIG ◽  
Alexander STOKES ◽  
Jean-Pierre KINET ◽  
Reinhold PENNER
Keyword(s):  
Intracellular Calcium ◽  
Transient Receptor Potential ◽  
Receptor Potential ◽  
Transient Receptor Potential Channel ◽  
Calcium Stores ◽  
Calcium Store ◽  
Release Channel ◽  
Subfamily Member ◽  
Store Depletion ◽  
Transient Receptor

The store-operated calcium-release-activated calcium current, ICRAC, is a major mechanism for calcium entry into non-excitable cells. ICRAC refills calcium stores and permits sustained calcium signalling. The relationship between inositol 1,4,5-trisphosphate receptor (InsP3R)-containing stores and ICRAC is not understood. A model of global InsP3R store depletion coupling with ICRAC activation may be simplistic, since intracellular stores are heterogeneous in their release and refilling activities. Here we use a ligand-gated calcium channel, TRPV1 (transient receptor potential channel, vanilloid subfamily member 1), as a new tool to probe store heterogeneity and define intracellular calcium compartments in a mast cell line. TRPV1 has activity as an intracellular release channel but does not mediate global calcium store depletion and does not invade a store coupled with ICRAC. Intracellular TRPV1 localizes to a subset of the InsP3R-containing stores. TRPV1 sensitivity functionally subdivides the InsP3-sensitive store, as does heterogeneity in the sarcoplasmic/endoplasmic-reticulum Ca2+-ATPase isoforms responsible for store refilling. These results provide unequivocal evidence that a specific ‘CRAC store’ exists within the InsP3-releasable calcium stores and describe a novel methodology for manipulation of intracellular free calcium.

Structure-activity relationship of (-) mammea A/BB derivatives against Leishmania amazonensis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
MA Brenzan ◽  
CV Nakamura ◽  
BPD Filho ◽  
T Ueda-Nakamura ◽  
MCM Young ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Leishmania Amazonensis ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Of
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