General Information of Target

Target ID LDTP01457
Target Name Dickkopf-related protein 1 (DKK1)
Gene Name DKK1
Gene ID 22943
Synonyms
Dickkopf-related protein 1; Dickkopf-1; Dkk-1; hDkk-1; SK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MMALGAAGATRVFVAMVAAALGGHPLLGVSATLNSVLNSNAIKNLPPPLGGAAGHPGSAV
SAAPGILYPGGNKYQTIDNYQPYPCAEDEECGTDEYCASPTRGGDAGVQICLACRKRRKR
CMRHAMCCPGNYCKNGICVSSDQNHFRGEIEETITESFGNDHSTLDGYSRRTTLSSKMYH
TKGQEGSVCLRSSDCASGLCCARHFWSKICKPVLKEGQVCTKHRRKGSHGLEIFQRCYCG
EGLSCRIQKDHHQASNSSRLHTCQRH
Target Type
Clinical trial
Target Bioclass
Other
Family
Dickkopf family
Subcellular location
Secreted
Function
Antagonizes canonical Wnt signaling by inhibiting LRP5/6 interaction with Wnt and by forming a ternary complex with the transmembrane protein KREMEN that promotes internalization of LRP5/6. DKKs play an important role in vertebrate development, where they locally inhibit Wnt regulated processes such as antero-posterior axial patterning, limb development, somitogenesis and eye formation. In the adult, Dkks are implicated in bone formation and bone disease, cancer and Alzheimer disease. Inhibits the pro-apoptotic function of KREMEN1 in a Wnt-independent manner, and has anti-apoptotic activity.
TTD ID
T56697
Uniprot ID
O94907
DrugMap ID
TTE3RAC
Ensemble ID
ENST00000373970.4
HGNC ID
HGNC:2891
ChEMBL ID
CHEMBL6024

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info 
3.21  LDD0318  [1]
STPyne
 Probe Info 
K222(7.85)  LDD0277  [2]
DBIA
 Probe Info 
C189(1.53)  LDD3316  [3]
CY4
 Probe Info 
C220(0.00); H223(0.00)  LDD0247  [4]
NAIA_5
 Probe Info 
C263(0.00); C189(0.00); C138(0.00)  LDD2223  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2058 C220(1.60)  LDD2253  [3]
 LDCM0023  KB03 A-549 C220(1.77)  LDD2677  [3]
 LDCM0024  KB05 MEL167 C189(1.53)  LDD3316  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
MyoD family inhibitor (MDFI) MDFI family Q99750
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Low-density lipoprotein receptor-related protein 6 (LRP6) LDLR family O75581

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bhq880 Antibody D62FLA
Dkn-01 Antibody DMF73Z
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pf-04840082 . D04OMR

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 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
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
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