Literature summary for 1.2.1.36 extracted from

Harper, A.R.; Le, A.T.; Mather, T.; Burgett, A.; Berry, W.; Summers, J.A.
Design, synthesis, and ex vivo evaluation of a selective inhibitor for retinaldehyde dehydrogenase enzymes (2018), Bioorg. Med. Chem., 26, 5766-5779 .

Search for more literature for 1.2.1.36

Cloned(Commentary)

Cloned (Comment)	Organism
expressed in HEK-293 cells	Gallus gallus
expressed in HEK-293 cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
dichloro-all-trans-retinone	irreversible inhibitor that effectively inhibits isoform RALDH1 in the nanomolar range. I.e. (3E,5E,7E,9E)-1,1-dichloro-4,8-dimethyl-10-(2,6,6-trimethylcyclohex-1-en-1-yl)deca-3,5,7,9-tetraen-2-one; irreversible inhibitor that effectively inhibits isoforms RALDH2 in the nanomolar range. I.e. (3E,5E,7E,9E)-1,1-dichloro-4,8-dimethyl-10-(2,6,6-trimethylcyclohex-1-en-1-yl)deca-3,5,7,9-tetraen-2-one; irreversible inhibitor that effectively inhibits isoforms RALDH3 in the nanomolar range. I.e. (3E,5E,7E,9E)-1,1-dichloro-4,8-dimethyl-10-(2,6,6-trimethylcyclohex-1-en-1-yl)deca-3,5,7,9-tetraen-2-one	Gallus gallus
dichloro-all-trans-retinone	irreversible inhibitor that effectively inhibits isoform RALDH2 in the nanomolar range. I.e. (3E,5E,7E,9E)-1,1-dichloro-4,8-dimethyl-10-(2,6,6-trimethylcyclohex-1-en-1-yl)deca-3,5,7,9-tetraen-2-one	Homo sapiens
WIN 18446	-	Gallus gallus
WIN 18446	-	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0807	-	retinal	isoform RALDH2, at pH 8.2 and 25°C	Gallus gallus

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
retinal + NAD+ + H2O	Gallus gallus	-	all-trans-retinoate + NADH + 2 H+	-	?
retinal + NAD+ + H2O	Homo sapiens	-	all-trans-retinoate + NADH + 2 H+	-	?

Organism

Organism	UniProt	Comment	Textmining
Gallus gallus	-	-	-
Gallus gallus	O93344	-	-
Gallus gallus	P27463	-	-
Homo sapiens	O94788	-	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
retinal + NAD+ + H2O	-	Gallus gallus	all-trans-retinoate + NADH + 2 H+	-	?
retinal + NAD+ + H2O	-	Homo sapiens	all-trans-retinoate + NADH + 2 H+	-	?

Synonyms

Synonyms	Comment	Organism
ALDH1A1	-	Gallus gallus
Aldh1a2	-	Homo sapiens
Aldh1a2	-	Gallus gallus
Aldh1a3	-	Gallus gallus
RalDH1	isoform	Gallus gallus
RALDH2	isoform	Homo sapiens
RALDH2	isoform	Gallus gallus
RALDH3	isoform	Gallus gallus
retinaldehyde dehydrogenase	-	Gallus gallus
retinaldehyde dehydrogenase 1	-	Gallus gallus
retinaldehyde dehydrogenase 2	-	Homo sapiens
retinaldehyde dehydrogenase 2	-	Gallus gallus

Cofactor

Cofactor	Comment	Organism	Structure
NAD+	-	Gallus gallus
NAD+	-	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0000051	-	dichloro-all-trans-retinone	isoform RALDH2, at pH 8.2 and 25°C	Gallus gallus
0.00000674	-	dichloro-all-trans-retinone	isoform RALDH3, at pH 8.2 and 25°C	Gallus gallus
0.00006435	-	dichloro-all-trans-retinone	isoform RALDH2, at pH 8.2 and 25°C	Homo sapiens
0.0001944	-	dichloro-all-trans-retinone	isoform RALDH1, at pH 8.2 and 25°C	Gallus gallus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000055	-	isoform RALDH2, at pH 8.2 and 25°C	Gallus gallus	dichloro-all-trans-retinone
0.00016127	-	isoform RALDH3, at pH 8.2 and 25°C	Gallus gallus	dichloro-all-trans-retinone
0.00019132	-	isoform RALDH2, at pH 8.2 and 25°C	Homo sapiens	dichloro-all-trans-retinone
0.0004347	-	isoform RALDH1, at pH 8.2 and 25°C	Gallus gallus	dichloro-all-trans-retinone

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)