Literature summary for 3.4.19.6 extracted from

Scalabrino, G.A.; Hogan, N.; OBoyle, K.M.; Slator, G.R.; Gregg, D.J.; Fitchett, C.M.; Draper, S.M.; Bennett, G.W.; Hinkle, P.M.; Bauer, K.; Williams, C.H.; Tipton, K.F.; Kelly, J.A.
Discovery of a dual action first-in-class peptide that mimics and enhances CNS-mediated actions of thyrotropin-releasing hormone (2007), Neuropharmacology, 52, 1472-1481.

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Inhibitors

Inhibitors	Comment	Organism	Structure
Glp-Asn-Pro-D-Tyr-D-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
Glp-Asn-Pro-D-Tyr-D-Trp-D-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
Glp-Asn-Pro-D-Tyr-D-TrpNH2	potent inhibitor of TRH-DE. Competetive, fully reversible and not time dependent inhibition	Rattus norvegicus
Glp-Asn-Pro-Tyr-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
Glp-Asn-Pro-Tyr-Trp-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
Glp-Asn-Pro-Tyr-TrpNH2	-	Rattus norvegicus

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.035	-	thyrotropin-releasing hormone	-	Rattus norvegicus
0.5	-	(3-Me-His2)thyrotropin-releasing hormone	-	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	male Wistar rats	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
brain	-	Rattus norvegicus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
(3-Me-His2)thyrotropin-releasing hormone + H2O	-	Rattus norvegicus	?	-	?
thyrotropin-releasing hormone + H2O	-	Rattus norvegicus	?	-	?

Synonyms

Synonyms	Comment	Organism
TRH-DE	-	Rattus norvegicus
TRH-degrading ectoenzyme	-	Rattus norvegicus

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000001	-	Glp-Asn-Pro-Tyr-Trp-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
0.000029	-	Glp-Asn-Pro-D-Tyr-D-Trp-D-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
0.000038	-	Glp-Asn-Pro-Tyr-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
0.000096	-	Glp-Asn-Pro-D-Tyr-D-Trp-7-amido-4-methyl-coumarin	-	Rattus norvegicus
0.000151	-	Glp-Asn-Pro-D-Tyr-D-TrpNH2	-	Rattus norvegicus
0.00064	-	Glp-Asn-Pro-Tyr-TrpNH2	-	Rattus norvegicus

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Release 2023.1 (January 2023)