General Information of Target

Target ID LDTP01971
Target Name Lactotransferrin (LTF)
Gene Name LTF
Gene ID 4057
Synonyms
GIG12; LF; Lactotransferrin; Lactoferrin; EC 3.4.21.-; Growth-inhibiting protein 12; Talalactoferrin) [Cleaved into: Lactoferricin-H; Lfcin-H; Kaliocin-1; Lactoferroxin-A; Lactoferroxin-B; Lactoferroxin-C]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKLVFLVLLFLGALGLCLAGRRRSVQWCAVSQPEATKCFQWQRNMRKVRGPPVSCIKRDS
PIQCIQAIAENRADAVTLDGGFIYEAGLAPYKLRPVAAEVYGTERQPRTHYYAVAVVKKG
GSFQLNELQGLKSCHTGLRRTAGWNVPIGTLRPFLNWTGPPEPIEAAVARFFSASCVPGA
DKGQFPNLCRLCAGTGENKCAFSSQEPYFSYSGAFKCLRDGAGDVAFIRESTVFEDLSDE
AERDEYELLCPDNTRKPVDKFKDCHLARVPSHAVVARSVNGKEDAIWNLLRQAQEKFGKD
KSPKFQLFGSPSGQKDLLFKDSAIGFSRVPPRIDSGLYLGSGYFTAIQNLRKSEEEVAAR
RARVVWCAVGEQELRKCNQWSGLSEGSVTCSSASTTEDCIALVLKGEADAMSLDGGYVYT
AGKCGLVPVLAENYKSQQSSDPDPNCVDRPVEGYLAVAVVRRSDTSLTWNSVKGKKSCHT
AVDRTAGWNIPMGLLFNQTGSCKFDEYFSQSCAPGSDPRSNLCALCIGDEQGENKCVPNS
NERYYGYTGAFRCLAENAGDVAFVKDVTVLQNTDGNNNEAWAKDLKLADFALLCLDGKRK
PVTEARSCHLAMAPNHAVVSRMDKVERLKQVLLHQQAKFGRNGSDCPDKFCLFQSETKNL
LFNDNTECLARLHGKTTYEKYLGPQYVAGITNLKKCSTSPLLEACEFLRK
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Transferrin family
Subcellular location
Secreted; Cytoplasm
Function
Transferrins are iron binding transport proteins which can bind two Fe(3+) ions in association with the binding of an anion, usually bicarbonate.; [Lactotransferrin]: Major iron-binding and multifunctional protein found in exocrine fluids such as breast milk and mucosal secretions . Has antimicrobial activity, which depends on the extracellular cation concentration. Antimicrobial properties include bacteriostasis, which is related to its ability to sequester free iron and thus inhibit microbial growth, as well as direct bactericidal properties leading to the release of lipopolysaccharides from the bacterial outer membrane . Can also prevent bacterial biofilm development in P.aeruginosa infection. Has weak antifungal activity against C.albicans. Has anabolic, differentiating and anti-apoptotic effects on osteoblasts and can also inhibit osteoclastogenesis, possibly playing a role in the regulation of bone growth. Promotes binding of species C adenoviruses to epithelial cells, promoting adenovirus infection. Can inhibit papillomavirus infections. Stimulates the TLR4 signaling pathway leading to NF-kappa-B activation and subsequent pro-inflammatory cytokine production while also interfering with the lipopolysaccharide (LPS)-stimulated TLR4 signaling. Inhibits neutrophil granulocyte migration to sites of apoptosis, when secreted by apoptotic cells. Stimulates VEGFA-mediated endothelial cell migration and proliferation. Binds heparin, chondroitin sulfate and possibly other glycosaminoglycans (GAGs). Also binds specifically to pneumococcal surface protein A (PspA), the lipid A portion of bacterial lipopolysaccharide (LPS), lysozyme and DNA.; Lactoferricin binds to the bacterial surface and is crucial for the bactericidal functions. Has some antiviral activity against papillomavirus infection. N-terminal region shows strong antifungal activity against C.albicans. Contains two BBXB heparin-binding consensus sequences that appear to form the predominate functional GAG-binding site.; [Kaliocin-1]: Has antimicrobial activity and is able to permeabilize different ions through liposomal membranes.; [Lactoferroxin-A]: Has opioid antagonist activity. Shows preference for mu-receptor.; [Lactoferroxin-B]: Has opioid antagonist activity. Shows higher degrees of preference for kappa-receptors than for mu-receptors.; [Lactoferroxin-C]: Has opioid antagonist activity. Shows higher degrees of preference for kappa-receptors than for mu-receptors.; The lactotransferrin transferrin-like domain 1 functions as a serine protease of the peptidase S60 family that cuts arginine rich regions. This function contributes to the antimicrobial activity. Shows a preferential cleavage at -Arg-Ser-Arg-Arg-|- and -Arg-Arg-Ser-Arg-|-, and of Z-Phe-Arg-|-aminomethylcoumarin sites.; [Isoform DeltaLf]: Transcription factor with antiproliferative properties and ability to induce cell cycle arrest. Binds to the DeltaLf response element found in the SKP1, BAX, DCPS, and SELENOH promoters.
TTD ID
T67801
Uniprot ID
P02788
DrugMap ID
TTSZDQU
Ensemble ID
ENST00000231751.9
HGNC ID
HGNC:6720
ChEMBL ID
CHEMBL4523161

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO678 SNV: p.R606K .
HEC1 SNV: p.Y434H DBIA    Probe Info 
HT115 SNV: p.A410V; p.S520Y .
JURKAT SNV: p.V602M .
MDST8 SNV: p.E70K DBIA    Probe Info 
NALM6 SNV: p.V388M .
OVK18 SNV: p.W27Ter .
WM793 SNV: p.E355K; p.A359V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
OPA-S-S-alkyne
 Probe Info 
K476(0.86); K320(1.48)  LDD3494  [1]
DBIA
 Probe Info 
C424(0.74)  LDD0613  [2]
4-Iodoacetamidophenylacetylene
 Probe Info 
C553(0.00); C424(0.00)  LDD0038  [3]
IA-alkyne
 Probe Info 
N.A.  LDD0036  [3]
Lodoacetamide azide
 Probe Info 
C424(0.00); C553(0.00)  LDD0037  [3]
ATP probe
 Probe Info 
N.A.  LDD0035  [4]
NAIA_5
 Probe Info 
C424(0.00); C478(0.00); C200(0.00)  LDD2223  [5]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info 
N.A.  LDD0136  [6]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0230  AC113 HEK-293T C424(0.50)  LDD0828  [2]
 LDCM0231  AC114 HEK-293T C424(0.81)  LDD0829  [2]
 LDCM0232  AC115 HEK-293T C424(0.57)  LDD0830  [2]
 LDCM0233  AC116 HEK-293T C424(0.80)  LDD0831  [2]
 LDCM0234  AC117 HEK-293T C424(0.47)  LDD0832  [2]
 LDCM0235  AC118 HEK-293T C424(0.55)  LDD0833  [2]
 LDCM0236  AC119 HEK-293T C424(1.10)  LDD0834  [2]
 LDCM0238  AC120 HEK-293T C424(1.13)  LDD0836  [2]
 LDCM0239  AC121 HEK-293T C424(0.50)  LDD0837  [2]
 LDCM0240  AC122 HEK-293T C424(0.77)  LDD0838  [2]
 LDCM0241  AC123 HEK-293T C424(0.54)  LDD0839  [2]
 LDCM0242  AC124 HEK-293T C424(0.48)  LDD0840  [2]
 LDCM0243  AC125 HEK-293T C424(0.85)  LDD0841  [2]
 LDCM0244  AC126 HEK-293T C424(1.23)  LDD0842  [2]
 LDCM0245  AC127 HEK-293T C424(0.88)  LDD0843  [2]
 LDCM0263  AC143 HEK-293T C424(0.74)  LDD0861  [2]
 LDCM0264  AC144 HEK-293T C424(0.91)  LDD0862  [2]
 LDCM0265  AC145 HEK-293T C424(0.83)  LDD0863  [2]
 LDCM0266  AC146 HEK-293T C424(1.02)  LDD0864  [2]
 LDCM0267  AC147 HEK-293T C424(0.55)  LDD0865  [2]
 LDCM0268  AC148 HEK-293T C424(0.90)  LDD0866  [2]
 LDCM0269  AC149 HEK-293T C424(0.17)  LDD0867  [2]
 LDCM0271  AC150 HEK-293T C424(0.51)  LDD0869  [2]
 LDCM0272  AC151 HEK-293T C424(0.71)  LDD0870  [2]
 LDCM0273  AC152 HEK-293T C424(0.42)  LDD0871  [2]
 LDCM0274  AC153 HEK-293T C424(0.52)  LDD0872  [2]
 LDCM0621  AC154 HEK-293T C424(0.50)  LDD2162  [2]
 LDCM0622  AC155 HEK-293T C424(0.55)  LDD2163  [2]
 LDCM0623  AC156 HEK-293T C424(0.63)  LDD2164  [2]
 LDCM0624  AC157 HEK-293T C424(0.60)  LDD2165  [2]
 LDCM0296  AC35 HCT 116 C424(0.74)  LDD0613  [2]
 LDCM0297  AC36 HCT 116 C424(0.82)  LDD0614  [2]
 LDCM0298  AC37 HCT 116 C424(0.54)  LDD0615  [2]
 LDCM0299  AC38 HCT 116 C424(0.87)  LDD0616  [2]
 LDCM0300  AC39 HCT 116 C424(0.36)  LDD0617  [2]
 LDCM0302  AC40 HCT 116 C424(0.59)  LDD0619  [2]
 LDCM0303  AC41 HCT 116 C424(0.92)  LDD0620  [2]
 LDCM0304  AC42 HCT 116 C424(0.69)  LDD0621  [2]
 LDCM0305  AC43 HCT 116 C424(0.76)  LDD0622  [2]
 LDCM0306  AC44 HCT 116 C424(0.55)  LDD0623  [2]
 LDCM0307  AC45 HCT 116 C424(0.39)  LDD0624  [2]
 LDCM0308  AC46 HCT 116 C424(0.26)  LDD0625  [2]
 LDCM0309  AC47 HCT 116 C424(0.33)  LDD0626  [2]
 LDCM0310  AC48 HCT 116 C424(0.30)  LDD0627  [2]
 LDCM0311  AC49 HCT 116 C424(0.96)  LDD0628  [2]
 LDCM0313  AC50 HCT 116 C424(1.21)  LDD0630  [2]
 LDCM0314  AC51 HCT 116 C424(0.99)  LDD0631  [2]
 LDCM0315  AC52 HCT 116 C424(0.59)  LDD0632  [2]
 LDCM0316  AC53 HCT 116 C424(0.85)  LDD0633  [2]
 LDCM0317  AC54 HCT 116 C424(0.57)  LDD0634  [2]
 LDCM0318  AC55 HCT 116 C424(0.81)  LDD0635  [2]
 LDCM0319  AC56 HCT 116 C424(0.49)  LDD0636  [2]
 LDCM0367  CL1 HCT 116 C424(0.96)  LDD0684  [2]
 LDCM0368  CL10 HCT 116 C424(1.14)  LDD0685  [2]
 LDCM0379  CL11 HCT 116 C424(1.11)  LDD0696  [2]
 LDCM0387  CL117 HCT 116 C424(0.40)  LDD0704  [2]
 LDCM0388  CL118 HCT 116 C424(0.85)  LDD0705  [2]
 LDCM0389  CL119 HCT 116 C424(0.73)  LDD0706  [2]
 LDCM0390  CL12 HCT 116 C424(0.35)  LDD0707  [2]
 LDCM0391  CL120 HCT 116 C424(0.59)  LDD0708  [2]
 LDCM0392  CL121 HCT 116 C424(0.95)  LDD0709  [2]
 LDCM0393  CL122 HCT 116 C424(0.85)  LDD0710  [2]
 LDCM0394  CL123 HCT 116 C424(0.62)  LDD0711  [2]
 LDCM0395  CL124 HCT 116 C424(0.60)  LDD0712  [2]
 LDCM0400  CL13 HCT 116 C424(0.91)  LDD0717  [2]
 LDCM0401  CL14 HCT 116 C424(1.26)  LDD0718  [2]
 LDCM0402  CL15 HCT 116 C424(1.08)  LDD0719  [2]
 LDCM0403  CL16 HCT 116 C424(1.02)  LDD0720  [2]
 LDCM0404  CL17 HCT 116 C424(0.72)  LDD0721  [2]
 LDCM0405  CL18 HCT 116 C424(0.91)  LDD0722  [2]
 LDCM0406  CL19 HCT 116 C424(1.18)  LDD0723  [2]
 LDCM0407  CL2 HCT 116 C424(1.01)  LDD0724  [2]
 LDCM0408  CL20 HCT 116 C424(1.22)  LDD0725  [2]
 LDCM0409  CL21 HCT 116 C424(1.08)  LDD0726  [2]
 LDCM0410  CL22 HCT 116 C424(1.54)  LDD0727  [2]
 LDCM0411  CL23 HCT 116 C424(0.61)  LDD0728  [2]
 LDCM0412  CL24 HCT 116 C424(0.76)  LDD0729  [2]
 LDCM0413  CL25 HCT 116 C424(1.08)  LDD0730  [2]
 LDCM0414  CL26 HCT 116 C424(0.23)  LDD0731  [2]
 LDCM0415  CL27 HCT 116 C424(1.19)  LDD0732  [2]
 LDCM0416  CL28 HCT 116 C424(1.17)  LDD0733  [2]
 LDCM0417  CL29 HCT 116 C424(0.79)  LDD0734  [2]
 LDCM0418  CL3 HCT 116 C424(0.71)  LDD0735  [2]
 LDCM0419  CL30 HCT 116 C424(1.52)  LDD0736  [2]
 LDCM0421  CL32 HCT 116 C424(1.16)  LDD0738  [2]
 LDCM0422  CL33 HCT 116 C424(0.94)  LDD0739  [2]
 LDCM0423  CL34 HCT 116 C424(1.86)  LDD0740  [2]
 LDCM0424  CL35 HCT 116 C424(1.70)  LDD0741  [2]
 LDCM0425  CL36 HCT 116 C424(2.02)  LDD0742  [2]
 LDCM0426  CL37 HCT 116 C424(0.66)  LDD0743  [2]
 LDCM0428  CL39 HCT 116 C424(0.88)  LDD0745  [2]
 LDCM0429  CL4 HCT 116 C424(0.90)  LDD0746  [2]
 LDCM0430  CL40 HCT 116 C424(0.76)  LDD0747  [2]
 LDCM0431  CL41 HCT 116 C424(1.65)  LDD0748  [2]
 LDCM0432  CL42 HCT 116 C424(1.94)  LDD0749  [2]
 LDCM0433  CL43 HCT 116 C424(1.17)  LDD0750  [2]
 LDCM0434  CL44 HCT 116 C424(2.09)  LDD0751  [2]
 LDCM0435  CL45 HCT 116 C424(1.55)  LDD0752  [2]
 LDCM0436  CL46 HEK-293T C424(1.18)  LDD1034  [2]
 LDCM0437  CL47 HEK-293T C424(1.01)  LDD1035  [2]
 LDCM0438  CL48 HEK-293T C424(0.82)  LDD1036  [2]
 LDCM0439  CL49 HEK-293T C424(0.92)  LDD1037  [2]
 LDCM0440  CL5 HCT 116 C424(0.96)  LDD0757  [2]
 LDCM0441  CL50 HEK-293T C424(0.97)  LDD1039  [2]
 LDCM0442  CL51 HEK-293T C424(0.93)  LDD1040  [2]
 LDCM0443  CL52 HEK-293T C424(1.01)  LDD1041  [2]
 LDCM0444  CL53 HEK-293T C424(1.05)  LDD1042  [2]
 LDCM0445  CL54 HEK-293T C424(1.09)  LDD1043  [2]
 LDCM0446  CL55 HEK-293T C424(1.23)  LDD1044  [2]
 LDCM0447  CL56 HEK-293T C424(2.26)  LDD1045  [2]
 LDCM0448  CL57 HEK-293T C424(0.39)  LDD1046  [2]
 LDCM0449  CL58 HEK-293T C424(0.05)  LDD1047  [2]
 LDCM0450  CL59 HEK-293T C424(0.64)  LDD1048  [2]
 LDCM0451  CL6 HCT 116 C424(1.23)  LDD0768  [2]
 LDCM0452  CL60 HEK-293T C424(1.51)  LDD1050  [2]
 LDCM0462  CL7 HCT 116 C424(1.84)  LDD0779  [2]
 LDCM0469  CL76 HEK-293T C424(4.27)  LDD1067  [2]
 LDCM0470  CL77 HEK-293T C424(0.89)  LDD1068  [2]
 LDCM0471  CL78 HEK-293T C424(6.03)  LDD1069  [2]
 LDCM0472  CL79 HEK-293T C424(1.12)  LDD1070  [2]
 LDCM0473  CL8 HCT 116 C424(0.51)  LDD0790  [2]
 LDCM0474  CL80 HEK-293T C424(5.07)  LDD1072  [2]
 LDCM0475  CL81 HEK-293T C424(1.20)  LDD1073  [2]
 LDCM0476  CL82 HEK-293T C424(3.87)  LDD1074  [2]
 LDCM0477  CL83 HEK-293T C424(5.01)  LDD1075  [2]
 LDCM0478  CL84 HEK-293T C424(1.88)  LDD1076  [2]
 LDCM0479  CL85 HEK-293T C424(0.67)  LDD1077  [2]
 LDCM0480  CL86 HEK-293T C424(5.05)  LDD1078  [2]
 LDCM0481  CL87 HEK-293T C424(0.52)  LDD1079  [2]
 LDCM0482  CL88 HEK-293T C424(2.77)  LDD1080  [2]
 LDCM0483  CL89 HEK-293T C424(0.56)  LDD1081  [2]
 LDCM0484  CL9 HCT 116 C424(0.98)  LDD0801  [2]
 LDCM0485  CL90 HEK-293T C424(1.33)  LDD1083  [2]
 LDCM0427  Fragment51 HCT 116 C424(1.63)  LDD0744  [2]
 LDCM0022  KB02 769-P C478(1.25)  LDD2246  [7]
 LDCM0023  KB03 769-P C478(1.27)  LDD2663  [7]
 LDCM0024  KB05 MONO-MAC-6 C478(1.31)  LDD3335  [7]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lauric Acid Small molecular drug DB03017
Phase 4
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Parecoxib Small molecular drug D05UWI
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Talactoferrin . D0IM6O
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Hlf 1-11 Peptide D0D8EY
Investigative
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
3h-indole-5,6-diol Small molecular drug D0H6MC
3h-indole-56-diol Small molecular drug DB01811
Alpha-d-fucopyranose Small molecular drug DB03485
Alpha-d-fucose Small molecular drug D01XEY
Alpha-d-mannose Small molecular drug D07LUR
Fucose Small molecular drug D0G6XS
Lauric Acid Small molecular drug D0N0UC
Nitrilotriacetic Acid Small molecular drug D03ZSY
Nitrilotriacetic Acid Small molecular drug DB03040
(R)-atenolol . DB06987
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nimesulide Small molecular drug D0C0JT

References

1 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
2 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
3 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
4 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
5 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
6 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
7 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