Studies of Ca2+ ATPase (SERCA) inhibition.
The Ca(2+) transport ATPase of intracellular membranes (SERCA) can be inhibited by a series of chemical compounds such as Thapsigargin (TG), 2,5-di(tert-butyl)hydroquinone (DBHQ) and 1,3-dibromo-2,4,6-tris (methyl-isothio-uronium) benzene (Br(2)-TITU). These compounds have specific binding sites in the ATPase protein, and different mechanisms of inhibition. On the other hand, SERCA gene silencing offers a convenient and specific method for suppression of SERCA activity in cells. The physiological and pharmacological implications of SERCA inhibition are discussed.
Inesi
Giuseppe
G
Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, Baltimore, Maryland 21201, USA. ginesi@umaryland.edu
Hua
Suming
S
Xu
Cheng
C
Ma
Hailun
H
Seth
Malini
M
Prasad
Anand M
AM
Sumbilla
Carlota
C
D001665:Binding Sites; D000252:Calcium-Transporting ATPases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000494:pharmacology; D020868:Gene Silencing / Q000187:drug effects; D034741:RNA, Small Interfering / Q000494:pharmacology
D004791:Enzyme Inhibitors; D034741:RNA, Small Interfering; D000252:Calcium-Transporting ATPases