General Information of Target

Target ID LDTP04242
Target Name Flavin-containing monooxygenase 5 (FMO5)
Gene Name FMO5
Gene ID 2330
Synonyms
Flavin-containing monooxygenase 5; FMO 5; Baeyer-Villiger monooxygenase 1; hBVMO1; EC 1.14.13.-; Dimethylaniline monooxygenase [N-oxide-forming] 5; EC 1.14.13.8; Dimethylaniline oxidase 5; NADPH oxidase; EC 1.6.3.1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTKKRIAVIGGGVSGLSSIKCCVEEGLEPVCFERTDDIGGLWRFQENPEEGRASIYKSVI
INTSKEMMCFSDYPIPDHYPNFMHNAQVLEYFRMYAKEFDLLKYIRFKTTVCSVKKQPDF
ATSGQWEVVTESEGKKEMNVFDGVMVCTGHHTNAHLPLESFPGIEKFKGQYFHSRDYKNP
EGFTGKRVIIIGIGNSGGDLAVEISQTAKQVFLSTRRGAWILNRVGDYGYPADVLFSSRL
THFIWKICGQSLANKYLEKKINQRFDHEMFGLKPKHRALSQHPTLNDDLPNRIISGLVKV
KGNVKEFTETAAIFEDGSREDDIDAVIFATGYSFDFPFLEDSVKVVKNKISLYKKVFPPN
LERPTLAIIGLIQPLGAIMPISELQGRWATQVFKGLKTLPSQSEMMAEISKAQEEIDKRY
VESQRHTIQGDYIDTMEELADLVGVRPNLLSLAFTDPKLALHLLLGPCTPIHYRVQGPGK
WDGARKAILTTDDRIRKPLMTRVVERSSSMTSTMTIGKFMLALAFFAIIIAYF
Target Bioclass
Enzyme
Family
FMO family
Subcellular location
Microsome membrane
Function
Acts as a Baeyer-Villiger monooxygenase on a broad range of substrates. Catalyzes the insertion of an oxygen atom into a carbon-carbon bond adjacent to a carbonyl, which converts ketones to esters. Active on diverse carbonyl compounds, whereas soft nucleophiles are mostly non- or poorly reactive. In contrast with other forms of FMO it is non- or poorly active on 'classical' substrates such as drugs, pesticides, and dietary components containing soft nucleophilic heteroatoms (Probable). Able to oxidize drug molecules bearing a carbonyl group on an aliphatic chain, such as nabumetone and pentoxifylline. Also, in the absence of substrates, shows slow but yet significant NADPH oxidase activity. Acts as a positive modulator of cholesterol biosynthesis as well as glucose homeostasis, promoting metabolic aging via pleiotropic effects.
Uniprot ID
P49326
Ensemble ID
ENST00000254090.9
HGNC ID
HGNC:3773
ChEMBL ID
CHEMBL3430871

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
KASUMI2 Substitution: p.E414R .
KMS12BM SNV: p.L41I .
KPL1 SNV: p.I530T .
MCF7 SNV: p.I530T .
MOLT4 SNV: p.A201G; p.Q210E .
NUGC3 SNV: p.L439F .
RL SNV: p.R43K .
TE4 SNV: p.S17F .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C248(1.93)  LDD3312  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 BRX211 C248(1.83)  LDD2268  [1]
 LDCM0023  KB03 BRX211 C248(4.25)  LDD2685  [1]
 LDCM0024  KB05 HMCB C248(1.93)  LDD3312  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840