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7.6.2.1: P-type phospholipid transporter

This is an abbreviated version!
For detailed information about P-type phospholipid transporter, go to the full flat file.

Word Map on EC 7.6.2.1

Reaction

ATP
+
H2O
+
phospholipid [side 1]
=
ADP
+
phosphate
+
phospholipid [side 2]

Synonyms

ABCB1, ABCB4, ALA1, ALA10, ALA11, ALA12, ALA2, ALA3, ALA4, ALA5, ALA7, ALA8, ALA9, aminophospholipid ATPase, aminophospholipid flippase, aminophospholipid flippase 10, aminophospholipid flippase 11, aminophospholipid flippase 12, aminophospholipid scramblase, aminophospholipid translocase, aminophospholipid translocase VC, aminophospholipid transporter, aminophospholipid-translocase, aminophosphoplipid translocase, APLT, ATP phosphohydrolase (phospholipid-flipping), ATP-dependent specific phospholipid flippase, ATP-independent flippase, ATP-independent long-chain phosphatidylcholine translocator, ATP10A, ATP10B, ATP10D, ATP11A, ATP11B, ATP11C, ATP8A1, Atp8a2, ATP8B1, ATP8B2, ATP8B3, ATP8B4, ATP8B5, ATP9A, ATP9B, ATPase II, ATPVC, ATPVD, CDC50A, Cdc50p-Drs2p, Cfs1p, Dnf1, Dnf1 |, Dnf1p, Dnf1p and Dnf2p, Dnf1p-Lem3p, Dnf2, Dnf2p, Dnf3, Dnf3p, Drs2, Drs2-dependent phosphatidylserine translocase, Drs2p, EC 3.6.3.1, EC 3.6.3.13, energy-dependent lipid flippase, energy-independent lipid flippase, EpsE, erythroid ATP-dependent aminophospholipid transporter, flippase, glycerophospholipid flippase, HUSSY-20, inward-directed phospholipid translocase, LdMT, LdRos3, lipid flippase, LMT translocase, M5-DLO flippase, Man5GlcNAc2-PP-dolichol flippase, MDR3 P-glycoprotein, Mg2+-ATPase, Mg2+-ATPase A, miltefosine transporter, More, MsbA, multidrug resistance 3 P-glycoprotein, MurJ, MviN, Neo1, Neo1p, P type aminophospholipid transporter, P-glycoprotein, P-gp, P4 ATPase ALA1, P4-ATPase, P4-type ATPase, PC-flippase, peptidoglycan lipid II flippase, phosphatidylserine flippase, phosphatidylserine translocase, phosphatidylserine translocase/ATPase, phospholipid flippase, phospholipid scramblase, phospholipid scramblase 1, phospholipid scramblase 3, phospholipid scrambling activity, phospholipid translocase, phospholipid-translocase, phospholipid-translocating ATPase, phospholipid-transporting ATPase IB, PL flippase, PL scramblase, PLS3, PLSCR1, PLSCR2, PLSCR3, PLSCR4, PS flippase, PS translocase, PS-flippase, scramblase, SCRM-1, sphingomyelin flippase, TAT-1, TAT-2, TAT-3, TAT-4, TAT-5, TAT-6, transbilayer amphipath transporter, transbilayer amphipath transporter-1, type 4 P-type ATPas, type II secretion ATPase, type IV P-type ATPase

ECTree

     7 Translocases
         7.6 Catalysing the translocation of other compounds
             7.6.2 Linked to the hydrolysis of a nucleoside triphosphate
                7.6.2.1 P-type phospholipid transporter

Inhibitors

Inhibitors on EC 7.6.2.1 - P-type phospholipid transporter

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-monoolein
-
0.5 mM significantly reduce the P-glycoprotein protein expression, 0.1 mM of 1-monoolein does not have any significant effect on the expression of P-glycoprotein
1-monostearin
-
0.5 mM significantly reduce the P-glycoprotein protein expression, 0.1 mM of 1-monostearin does not have any significant effect on the expression of P-glycoprotein
4-(2-aminoethyl)benzenesulfonyl fluoride
-
flippase activity for 1-oleoyl-2-[6-(7-nitrol-2-1,3-benzonadiol-4-yl)amino]-sn-glycerophosphoethanolamine is inhibited by 72% at 5 mM 4-(2-aminoethyl)benzenesulfonyl fluoride, flippase activity for 1-oleoyl-2-[6-(7-nitrol-2-1,3-benzonadiol-4-yl)amino]-sn-glycerophosphocholine is inhibited by 75% at 5 mM 4-(2-aminoethyl)benzenesulfonyl fluoride
4-hydroxy-2-nonenal
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
flippase activity for 1-oleoyl-2-[6-(7-nitrol-2-1,3-benzonadiol-4-yl)amino]-sn-glycerophosphoethanolamine is inhibited by 80% at 20 mM 5,5'-dithiobis(2-nitrobenzoic acid), flippase activity for 1-oleoyl-2-[6-(7-nitrol-2-1,3-benzonadiol-4-yl)amino]-sn-glycerophosphocholine is inhibited by 60% at 20 mM 5,5'-dithiobis(2-nitrobenzoic acid)
AlFx
trapping of MsbA with 0.8 mM AlFx results in incomplete inhibition of activity
azide
-
-
Bcl-2
-
PLS3 and tBid may form a bidirectional positive feedback loop that is antagonized by Bcl-2
-
BeFx
trapping of MsbA with 0.8 mM BeFx results in incomplete inhibition of activity
Cd2+
-
-
cholesterol
-
the transport activity of P-glycoprotein decreases by about 20% cholesterol
cyclosporin A
-
inhibition of phospholipid flipping
Diamide
-
-
diethyldicarbonate
-
rat liver contains two populations, DEPC-sensitive and DEPC-insensitive, of flippases, which can be in a different of DEPC sensitivity or be two different proteins
DTNB
-
-
EDTA
-
-
elaiophylin
-
partial inhibition of Mg+-ATPase activity, translocation of phosphatidylserine is almost completely abolished
eosin Y
-
almost complete inhibition of both Mg2+-ATPase activity and translocation
Kes1p
-
Kes1p represses the flippase activity of Drs2p in trans-Golgi network membranes
-
lipid A
lipid A inhibits translocation by approx. 30% at 0.01-0.04 mg/ml
methyl-beta-cyclodextrin
-
transport of 0.001 mM tetramethylrosamine is essentially abolished by 1 mM methyl-beta-cyclodextrin, and transport of 0.005 mM H33342 is almost completely inhibited by 5 mM methyl-beta-cyclodextrin
orthovanadate
-
-
phosphate analogue Vi
the presence of 0.1-0.2 m M Vi inhibits flippase activity of MsbA by approx. 50%
pyridyldithioethylamine
-
-
ribavirin
-
prolonged treatment of erythrocytes with ribavirin results in surface exposure of phosphatidylserine, mainly caused by inactivation of the aminophospholipid translocase. Inactivation is due to severe ATP depletion
S-nitroso-L-cysteine-ethyl ester
-
i.e. SNCEE, causes intracellular and extracellular trans-nitrosylation of proteins, respectively. Nitrosative stress inhibits the enzyme, and SNCEE causes significant S-nitrosylation/oxidation of thiols in HL-60 cells. SNCEE also strongly inhibites APLT, activated scramblase, and causes PS externalization, reversible by DTT
sulfhydryl reagents
-
-
suramin
-
competitive inhibitor of ATP towards both Mg2+-ATPase activity and aminophospholipid translocation. Inhibition of translocation occurs at higher inhibitor concentration than the inhibition of Mg2+-ATPase activity
vanadate
vanadyl ion
-
inhibits the enzyme from the extracellular surface
verapamil
vinblastine
-
inhibition of phospholipid flipping
additional information
-