Details of the Target

General Information of Target

Target ID LDTP03391
Target Name Dipeptidyl peptidase 4 (DPP4)
Gene Name DPP4
Gene ID 1803
Synonyms
ADCP2; CD26; Dipeptidyl peptidase 4; EC 3.4.14.5; ADABP; Adenosine deaminase complexing protein 2; ADCP-2; Dipeptidyl peptidase IV; DPP IV; T-cell activation antigen CD26; TP103; CD antigen CD26) [Cleaved into: Dipeptidyl peptidase 4 membrane form; Dipeptidyl peptidase IV membrane form; Dipeptidyl peptidase 4 soluble form; Dipeptidyl peptidase IV soluble form)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSL
RWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNY
VKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNL
PSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSF
YSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPS
EPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISN
EYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLY
TLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKY
PLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWE
YYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQIS
KALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP
Target Type
Successful
Target Bioclass
Enzyme
Family
Peptidase S9B family, DPPIV subfamily
Subcellular location
Secreted; Cell membrane
Function
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also regulates lymphocyte-epithelial cell adhesion. In association with FAP is involved in the pericellular proteolysis of the extracellular matrix (ECM), the migration and invasion of endothelial cells into the ECM. May be involved in the promotion of lymphatic endothelial cells adhesion, migration and tube formation. When overexpressed, enhanced cell proliferation, a process inhibited by GPC3. Acts also as a serine exopeptidase with a dipeptidyl peptidase activity that regulates various physiological processes by cleaving peptides in the circulation, including many chemokines, mitogenic growth factors, neuropeptides and peptide hormones such as brain natriuretic peptide 32. Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline.; (Microbial infection) Acts as a receptor for human coronavirus MERS-CoV-2.
TTD ID
T31391
Uniprot ID
P27487
DrugMap ID
TTF928K
Ensemble ID
ENST00000360534.8
HGNC ID
HGNC:3009
ChEMBL ID
CHEMBL284

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  		C394(0.98)  LDD3316  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 Hep 3B2.1-7 C649(1.64); C394(1.51)  LDD2353  [1]
 LDCM0023  KB03 Hep 3B2.1-7 C394(1.65)  LDD2770  [1]
 LDCM0024  KB05 MEL167 C394(0.98)  LDD3316  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Dipeptidyl peptidase 4 (DPP4) Peptidase S9B family P27487
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Metabotropic glutamate receptor 2 (GRM2) G-protein coupled receptor 3 family Q14416
Cytokine and receptor
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
C-X-C motif chemokine 10 (CXCL10) Intercrine alpha (chemokine CxC) family P02778
C-X-C motif chemokine 11 (CXCL11) Intercrine alpha (chemokine CxC) family O14625
C-X-C motif chemokine 2 (CXCL2) Intercrine alpha (chemokine CxC) family P19875
C-X-C motif chemokine 9 (CXCL9) Intercrine alpha (chemokine CxC) family Q07325
Eotaxin (CCL11) Intercrine beta (chemokine CC) family P51671
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Pro-glucagon (GCG) Glucagon family P01275
VIP peptides (VIP) Glucagon family P01282

The Drug(s) Related To This Target

Approved
Click To Hide/Show 11 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Exenatide Protein/peptide DB01276
Liraglutide Protein/peptide DB06655
Alogliptin Small molecular drug D0NJ5H
Atorvastatin Small molecular drug DB01076
Linagliptin Small molecular drug D02EYG
Pf-00734200 Small molecular drug D0T8XB
Pk-44 Small molecular drug D05IPF
Saxagliptin Small molecular drug D0K9MY
Semaglutide Small molecular drug DB13928
Sitagliptin Small molecular drug D0U2JP
Vildagliptin Small molecular drug D0L3DK
Phase 3
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Mk-3102 Antibody D0N7JZ
Ari-2243 Small molecular drug D0N6SO
Da-1229 Small molecular drug D0M3XR
Fucose Small molecular drug D06VCN
Gemigliptin Small molecular drug D0ZD3C
Dutogliptin . D04XIO
Lc-150444 . D02ZBW
Peptide Analog 49 . D09XMX
Pmid25482888-compound-37 . D0V0KJ
Phase 2
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
N-isoleucylthiazolidine Antibody D05VXF
3-butyl-1-(Naphthalen-1-yl)Piperidin-4-amine Small molecular drug D0H2IO
D-420720 Small molecular drug D07HZG
(2-(2-chlorophenyl)Pyridin-3-yl)Methanamine . D03SKC
Ip10 C8 . D0E3HY
Pmid25482888-compound-6 . D06VMJ
Phase 1
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Beta-phe Compound 2 Small molecular drug D07EPV
Tak-100 Small molecular drug D05LPW
Db-160 . D03JWU
Pmid25482888-compound-13 . D0BA5E
Pmid25482888-compound-56 . D0Z1OS
Preclinical
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pt630 Peptide D7K0GP
Asc-201 . D0O6DC
N4-(4-chlorobenzyl)-2,4-diaminobutanoylpiperidine . D0XL4I
Triazole Piperazine Derivative 1 . D0Q6ED
Investigative
Click To Hide/Show 89 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(+/-)-6-(2-chlorophenyl)Cyclohex-3-enamine Small molecular drug D05UUA
(1-phenylcyclopentyl)Methanamine Small molecular drug D0W4GM
(1r,2s)-1,2-diphenylethane-1,2-diamine Small molecular drug D07HWI
(2-chloro-6-phenoxyphenyl)Methanamine Small molecular drug D0X2JG
(2s)-pyrrolidin-2-ylmethylamine Small molecular drug D07VDJ
(3s,4r)-3-butyl-1-phenylpiperidin-4-amine Small molecular drug D05LYC
(5-phenyl-3h-benzo[D]Imidazol-4-yl)Methanamine Small molecular drug D05XWX
(R)-1-(2-aminoacetyl)Pyrrolidin-2-ylboronic Acid Small molecular drug D04CAR
(S)-pyrrolidin-1-yl(Pyrrolidin-2-yl)Methanone Small molecular drug D07IJU
1-(1-phenylcyclopentyl)Methylamine Small molecular drug DB04577
1-biphenyl-2-ylmethanamine Small molecular drug D09MVE
2-(2-chlorophenyl)-2-morpholinoethanamine Small molecular drug D02WBC
2-amino-3-methyl-1-pyrrolidin-1-yl-butan-1-one Small molecular drug D0L9XR
4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine Small molecular drug D06UKY
4-(2,4-dichlorophenyl)-1-tosylpyrrolidin-3-amine Small molecular drug D02RIE
4-iodo-l-phenylalanine Small molecular drug DB03660
Abt-341 Small molecular drug D04QDB
Alpha-d-mannose Small molecular drug D00KMP
Aminopiperidine Derivative 2 Small molecular drug D01OUJ
Anagliptin Small molecular drug D0N5CI
C-(2'-chloro-biphenyl-2-yl)-methylamine Small molecular drug D06NRU
Diisopropylphosphono Group Small molecular drug D03FDC
Er-319711-15 Small molecular drug D00HSG
Fe 999011 Small molecular drug D0IQ4S
Gosogliptin Small molecular drug DB08382
Iddbcp161883 Small molecular drug D0PB2M
Imidazo Cyclohexylamine Derivative 3 Small molecular drug D0D9ON
Kr-62436 Small molecular drug D0C2NQ
Ly-2463665 Small molecular drug D0JI3S
Melogliptin Small molecular drug D0L5RI
Nvp-dpp728 Small molecular drug D07LUR
P32/98 Small molecular drug D0R5OE
Pmid25482888-compound-11 Small molecular drug D0G6XS
Pmid25482888-compound-14 Small molecular drug D0O9RD
Pmid25482888-compound-16 Small molecular drug D0T2EW
Pmid25482888-compound-18 Small molecular drug D09BYA
Pmid25482888-compound-34 Small molecular drug D07ALM
Pt-630 Small molecular drug D0N1QQ
Pyrimidine Derivative 32 Small molecular drug D06AUB
Pyrrolo[1,2-f]Triazine Derivative 2 Small molecular drug D0N1FU
Ta-6666 Small molecular drug D0P5OE
Zydpla 1 Small molecular drug D08NMS
(1s)-2-[(2s5r)-2-(Aminomethyl)-5-ethynylpyrrolidin-1-yl]-1-cyclopentyl-2-oxoethanamine . DB07356
(1s)-2-[(2s5r)-2-(Aminomethyl)-5-prop-1-yn-1-ylpyrrolidin-1-yl]-1-cyclopentyl-2-oxoethanamine . DB06880
(1s2r5s)-5-[3-(Trifluoromethyl)-56-dihydro[124]Triazolo[43-a]Pyrazin-7(8h)-yl]-2-(245-trifluorophenyl)Cyclohexanamine . DB07072
(1s3s5s)-2-{(2s)-2-amino-2-[(1r3s5r7s)-3-hydroxytricyclo[3.3.1.1~37~]Dec-1-yl]Acetyl}-2-azabicyclo[3.1.0]Hexane-3-carbonitrile . DB07465
(2r)-4-(2-benzoyl-12-diazepan-1-yl)-4-oxo-1-(245-trifluorophenyl)Butan-2-amine . DB08051
(2r)-4-[(8r)-8-methyl-2-(Trifluoromethyl)-56-dihydro[124]Triazolo[15-a]Pyrazin-7(8h)-yl]-4-oxo-1-(245-trifluorophenyl)Butan-2-amine . DB07081
(2r)-n-[(2r)-2-(Dihydroxyboryl)-1-l-prolylpyrrolidin-2-yl]-n-[(5r)-5-(Dihydroxyboryl)-1-l-prolylpyrrolidin-2-yl]-l-prolinamide . DB07482
(2r3r)-7-(Methylsulfonyl)-3-(245-trifluorophenyl)-1234-tetrahydropyrido[12-a]Benzimidazol-2-amine . DB07193
(2s3s)-3-amino-4-(33-difluoropyrrolidin-1-yl)-nn-dimethyl-4-oxo-2-(Trans-4-[124]Triazolo[15-a]Pyridin-6-ylcyclohexyl)Butanamide . DB07092
(2s3s)-3-amino-4-[(3s)-3-fluoropyrrolidin-1-yl]-nn-dimethyl-4-oxo-2-(Trans-4-[124]Triazolo[15-a]Pyridin-5-ylcyclohexyl)Butanamide . DB07135
(2s3s)-3-{3-[2-chloro-4-(Methylsulfonyl)Phenyl]-124-oxadiazol-5-yl}-1-cyclopentylidene-4-cyclopropyl-1-fluorobutan-2-amine . DB06994
(2s3s)-3-{3-[4-(Methylsulfonyl)Phenyl]-124-oxadiazol-5-yl}-1-oxo-1-pyrrolidin-1-ylbutan-2-amine . DB07067
(2s3s)-4-cyclopropyl-3-{(3r5r)-3-[2-fluoro-4-(Methylsulfonyl)Phenyl]-124-oxadiazolidin-5-yl}-1-[(3s)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine . DB06993
(3r)-4-[(3r)-3-amino-4-(245-trifluorophenyl)Butanoyl]-3-methyl-14-diazepan-2-one . DB07154
(3r4r)-1-{6-[3-(Methylsulfonyl)Phenyl]Pyrimidin-4-yl}-4-(245-trifluorophenyl)Piperidin-3-amine . DB08164
(3r4r)-4-(Pyrrolidin-1-ylcarbonyl)-1-(Quinoxalin-2-ylcarbonyl)Pyrrolidin-3-amine . DB07015
(3r4s)-1-(34-dimethoxyphenyl)-3-(3-methylphenyl)Piperidin-4-amine . DB07851
(3r4s)-1-[6-(6-methoxypyridin-3-yl)Pyrimidin-4-yl]-4-(245-trifluorophenyl)Pyrrolidin-3-amine . DB08445
(3r4s)-1-{6-[3-(Methylsulfonyl)Phenyl]Pyrimidin-4-yl}-4-(245-trifluorophenyl)Pyrrolidin-3-amine . DB07666
(4r5r)-5-amino-1-[2-(13-benzodioxol-5-yl)Ethyl]-4-(245-trifluorophenyl)Piperidin-2-one . DB07830
(7r8r)-8-(245-trifluorophenyl)-6789-tetrahydroimidazo[12-a:45-c']Dipyridin-7-amine . DB07021
(S)-2-[(R)-3-amino-4-(2-fluorophenyl)Butyryl]-1234-tetrahydroisoquinoline-3-carboxamide . DB04578
1-[2-(S)-amino-3-biphenyl-4-yl-propionyl]-pyrrolidine-2-(S)-carbonitrile . DB08024
2-({2-[(3r)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4h)-yl}Methyl)Benzonitrile . DB08588
2-({8-[(3r)-3-aminopiperidin-1-yl]-13-dimethyl-26-dioxo-1236-tetrahydro-7h-purin-7-yl}Methyl)Benzonitrile . DB08743
4'-[(1r)-1-amino-2-(25-difluorophenyl)Ethyl]Biphenyl-3-carboxamide . DB07181
4-[(3r)-3-amino-4-(245-trifluorophenyl)Butanoyl]-3-(222-trifluoroethyl)-14-diazepan-2-one . DB07271
4-[(3r)-3-{[2-(4-fluorophenyl)-2-oxoethyl]Amino}Butyl]Benzamide . DB08672
5-(Aminomethyl)-6-(24-dichlorophenyl)-2-(35-dimethoxyphenyl)Pyrimidin-4-amine . DB02004
6-(4-{(1s2s)-2-amino-1-[(Dimethylamino)Carbonyl]-3-[(3s)-3-fluoropyrrolidin-1-yl]-3-oxopropyl}Phenyl)-1h-[124]Triazolo[15-a]Pyridin-4-ium . DB08504
7-(Aminomethyl)-6-(2-chlorophenyl)-1-methyl-1h-benzimidazole-5-carbonitrile . DB07239
7-benzyl-13-dimethyl-8-piperazin-1-yl-37-dihydro-purine-26-dione . DB08530
Amg-222 . DB06011
Bisegliptin . DB06127
Bpi-711001 . D01ZWF
Cyclohexylglycine-(2s)-cyanopyrrolidine . D0T8UH
D-val-l-boropro . D0L1NF
Imidazo Pyridine Derivative 2 . D0N3YL
Methyl 4-{[({[(2r5s)-5-{[(2s)-2-(Aminomethyl)Pyrrolidin-1-yl]Carbonyl}Pyrrolidin-2-yl]Methyl}Amino)Carbonyl]Amino}Benzoate . DB07328
N-(Trans-4-{(1s2s)-2-amino-3-[(3s)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl}Cyclohexyl)-n-methylacetamide . DB06939
N-({(2s)-1-[(3r)-3-amino-4-(2-fluorophenyl)Butanoyl]Pyrrolidin-2-yl}Methyl)Benzamide . DB07779
N-({(2s)-1-[(3r)-3-amino-4-(3-chlorophenyl)Butanoyl]Pyrrolidin-2-yl}Methyl)-3-(Methylsulfonyl)Benzamide . DB08429
Pmid20684603c24dd . D05WKT
Psn9301 . DB05001
Retagliptin . D05TKO
Saxadapa Fdc . D01KRQ
Syr-472 . D0FH8R
Patented
Click To Hide/Show 54 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(S)-2-amino-1-azetidin-1-yl-2-cyclohexyl-ethanone Peptide D02UOW
Asp8497 Peptide D0QE8Z
Beta-phe Compound 1 Peptide D0W6HL
C-(2'-chloro-biphenyl-2-yl)-methylamine Peptide D0IO0M
Kombiglyze Xr/Komboglyze Fdc Peptide D0B4CH
Peptide Analog 46 Peptide D0WE8K
Peptide Analog 50 Peptide D05GEY
Peptide Analog 51 Peptide D0J4KQ
Pmid25482888-compound-17 Peptide D04XXF
Pmid25482888-compound-70 Peptide D05LJQ
Psn-9301 Peptide D0E8WW
Xanthine Derivative 1 Peptide D0BY2H
(S)-2-amino-1-thiazolidin-3-yl-propane-1-thione Small molecular drug D0EL5B
(S)-pyrrolidin-2-yl(Thiazolidin-3-yl)Methanone Small molecular drug D0ND5K
4-iodophenyl-alaninyl-(S)-2-cyano-pyrrolidine Small molecular drug D0CW9H
Abt-279 Small molecular drug D04MAZ
Als 2-0426 Small molecular drug D0T1WB
Aminopiperidine Derivative 1 Small molecular drug D0A6LI
Beta-phe Compound 3 Small molecular drug D0BJ2X
Denagliptin Small molecular drug D06PDK
Dihydropyrrolopyrazole Derivative 1 Small molecular drug D0XB0Q
Diprotin A Small molecular drug D0J0UN
Dsp-7238 Small molecular drug D0K2ZQ
E-3024 Small molecular drug D00GNP
Imidazo Cyclohexylamine Derivative 1 Small molecular drug D02SUS
Imidazo Cyclohexylamine Derivative 2 Small molecular drug D06GQG
Iodo-phenylalanine Small molecular drug D0KR7R
L-val-l-boropro Small molecular drug D01MMT
Peptide Analog 44 Small molecular drug D0A5QV
Peptide Analog 45 Small molecular drug D06PIP
Peptide Analog 48 Small molecular drug D0JP6A
Pmid25482888-compound-12 Small molecular drug D0N9CV
Pmid25482888-compound-15 Small molecular drug D02LNB
Pmid25482888-compound-21 Small molecular drug D0T6SD
Pmid25482888-compound-38 Small molecular drug D0XN3O
Pmid25482888-compound-50 Small molecular drug D0K5YJ
Pmid25482888-compound-52 Small molecular drug D0PF2W
Pmid25482888-compound-69 Small molecular drug D0E9MO
Pmid25482888-compound-71 Small molecular drug D0G1CF
Pmid25482888-compound-72 Small molecular drug D0O6SK
Pyrimidine Derivative 30 Small molecular drug D0RT1R
Pyrimidine Derivative 31 Small molecular drug D07JJT
Pyrimidine Derivative 33 Small molecular drug D04UXC
Pyrimidinedione Derivative 1 Small molecular drug D0J5EW
Pyrrolo[1,2-f]Triazine Derivative 1 Small molecular drug D0P3DS
Quinazoline Derivative 1 Small molecular drug D05HLQ
Rec-01 Small molecular drug D0G3IL
Teneligliptin Small molecular drug D0UV3I
Thiomorpholine Derivative 1 Small molecular drug D06HJX
Thiomorpholine Derivative 2 Small molecular drug D0D4BP
Triazolo-pyrimidinedione Derivative 1 Small molecular drug D0PM4N
Triazolo-pyrimidinedione Derivative 2 Small molecular drug D0KS8Y
Tricyclic Heterocycle Derivative 6 Small molecular drug D0E8AS
Xanthine/Amino Piperidine Compound 1 Small molecular drug D0LG1I
Discontinued
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1-benzhydryl-3-butylpiperidin-4-amine Small molecular drug D0Q4YP
1-benzyl-4-(2,4-dichlorophenyl)Pyrrolidin-3-amine Small molecular drug D00FYF
Peptide Analog 47 Small molecular drug D0A1NU
Ssr-162369 Small molecular drug D0X5ZO
(1r,2r)-1,2-diphenylethane-1,2-diamine . D0F3TI
Emc-0901 . D0JA1Z
Krp-104 . D0H2KV
R-1438 . D0E4EZ
Sand-26 . D0M9SL
Yscma . D0FD0B

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