Ligand 7-ethyl-10-hydroxycampothecin

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Basic Ligand Information

Molecular Structure
Picture of 7-ethyl-10-hydroxycampothecin (click for magnification)
Molecular Formula
BRENDA Name
InChIKey
C22H20N2O5
7-ethyl-10-hydroxycampothecin
FJHBVJOVLFPMQE-JOCHJYFZSA-N
Synonyms:
7-Ethyl-10-hydroxy-camptothecin, 7-ethyl-10-hydroxy-camptothecin lactone, 7-ethyl-10-hydroxycamptothecin, SN-38, SN-38[side 1], SN-38[side 2], SN38
Pathway Source
Pathways

Roles as Enzyme Ligand

In Vivo Substrate in Enzyme-catalyzed Reactions (1 result)

EC NUMBER
LITERATURE
REACTION DIAGRAM
PROVEN IN VIVO REACTION
ENZYME 3D STRUCTURE
show the reaction diagram
UDP-glucuronate + 7-ethyl-10-hydroxycamptothecin = UDP + 7-ethyl-10-hydroxycamptothecin 10-O-beta-D-glucuronoside
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In Vivo Product in Enzyme-catalyzed Reactions (1 result)

EC NUMBER
LITERATURE
REACTION DIAGRAM
PROVEN IN VIVO REACTION
ENZYME 3D STRUCTURE
show the reaction diagram
7-ethyl-10[4-(1-piperidino)-1-piperdino]carbonyloxy-camptothecin + H2O = 7-ethyl-10-hydroxy-camptothecin + ?
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Substrate in Enzyme-catalyzed Reactions (9 results)

EC NUMBER
LITERATURE
REACTION DIAGRAM
REACTION
ENZYME 3D STRUCTURE

Product in Enzyme-catalyzed Reactions (12 results)

EC NUMBER
LITERATURE
REACTION DIAGRAM
REACTION
ENZYME 3D STRUCTURE
show the reaction diagram
7-ethyl-10-[4-(1-piperidine)-1-piperidino]carbonyloxycamtothecin + H2O = 7-ethyl-10-hydroxycamptothecin + ?
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Inhibitor in Enzyme-catalyzed Reactions (5 results)

COMMENTARY
EC NUMBER
LITERATURE
ENZYME 3D STRUCTURE
active metabolite of CPT-11
-
enzyme linker fluctuations can have an impact on SN38 binding by reducing the enzyme affinity for the drug. TOP1 mutations are involved in the development of SN38 resistance
-
review of clinical pharmacokinetics
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3D Structure of Enzyme-Ligand-Complex (PDB) (1 result)

EC NUMBER
ENZYME 3D STRUCTURE

Enzyme Kinetic Parameters

KM Value (2 results)

COMMENTARY
EC NUMBER
KM VALUE [MM]
KM VALUE MAXIMUM [MM]
LITERATURE
recombinant UGT1A9 mutant D256N isozyme, pH.4, 37°C
44.4
-
recombinant wild-type isozyme UGT1A9, pH.4, 37°C
19.3
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IC50 Value (5 results)

COMMENTARY
EC NUMBER
IC50 VALUE
IC50 VALUE MAXIMUM
LITERATURE
mutant enzyme R364K/G717R from HCT-116 cells, pH and temperature not specified in the publication
0.0034
-
wild type enzyme from HCT-116 cells, pH and temperature not specified in the publication
0.00005
-
wild type enzyme from HT-29 cells, pH and temperature not specified in the publication
0.00013
-
wild type enzyme from LoVo cells, pH and temperature not specified in the publication
0.00002
-
wild type enzyme, pH and temperature not specified in the publication
0.00005
-

References & Links

Links to other databases for 7-ethyl-10-hydroxycampothecin

ChEBI
PubChem
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PubChem