Literature summary for 1.13.11.34 extracted from

Maucher, I.V.; Ruehl, M.; Kretschmer, S.B.; Hofmann, B.; Kuehn, B.; Fettel, J.; Vogel, A.; Fluegel, K.T.; Manolikakes, G.; Hellmuth, N.; Haefner, A.K.; Golghalyani, V.; Ball, A.K.; Piesche, M.; Matrone, C.; Geisslinger, G.; Parnham, M.J.; Karas, M.; Steinhilber, D.; Roos, J.; Maier, T.J.
Michael acceptor containing drugs are a novel class of 5-lipoxygenase inhibitor targeting the surface cysteines C416 and C418 (2017), Biochem. Pharmacol., 125, 55-74 .

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Inhibitors

Inhibitors	Comment	Organism
10-nitro-oleic acid	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM	Homo sapiens
AA-861	compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0082 mM	Homo sapiens
baicalein	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0014 mM	Homo sapiens
BWA4C	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.00015 mM	Homo sapiens
chalcone	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.006 mM	Homo sapiens
curcumin	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0016 mM	Homo sapiens
embelin	compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0035 mM	Homo sapiens
luteolin	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0006 mM	Homo sapiens
additional information	naturally occurring or synthetic anti-inflammatory compounds carrying a Michael acceptor, such as thymoquinone, the paracetamol metabolite NAPQI, the 5-Lox inhibitor AA-861, and bardoxolone methyl (i.e. RTA 402 or CDDO-methyl ester) are direct covalent 5-Lox enzyme inhibitors that target the catalytically relevant cysteines 416 and 418	Homo sapiens
NAPQI	compound reacts with catalytically relevant cysteine residues 416 and 418	Homo sapiens
Plumbagin	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.007 mM	Homo sapiens
primin	compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0028 mM	Homo sapiens
shikonin	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM	Homo sapiens
shogaol	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.005 mM	Homo sapiens
thymoquinone	compound reacts with catalytically relevant cysteine residues 416 and 418, inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0015 mM	Homo sapiens
U73122	inhibition of the 5-LO product formation of intact human polymorphonuclear leukocytes, IC50 value 0.0069 mM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P09917	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
leukocyte	polymorphonuclear leukocyte	Homo sapiens	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor
0.00006	-	pH 7.4, 37°C	Homo sapiens	luteolin
0.00017	-	pH 7.4, 37°C	Homo sapiens	U73122
0.0002	-	pH 7.4, 37°C	Homo sapiens	BWA4C
0.00023	-	pH 7.4, 37°C	Homo sapiens	embelin
0.00029	-	pH 7.4, 37°C	Homo sapiens	baicalein
0.0005	-	pH 7.4, 37°C	Homo sapiens	shikonin
0.0006	-	pH 7.4, 37°C	Homo sapiens	shogaol
0.0006	-	pH 7.4, 37°C	Homo sapiens	10-nitro-oleic acid
0.0006	-	pH 7.4, 37°C	Homo sapiens	primin
0.0007	-	pH 7.4, 37°C	Homo sapiens	chalcone
0.0014	-	pH 7.4, 37°C	Homo sapiens	curcumin
0.00143	-	pH 7.4, 37°C	Homo sapiens	Plumbagin
0.003	-	pH 7.4, 37°C	Homo sapiens	NAPQI
0.0038	-	pH 7.4, 37°C	Homo sapiens	AA-861