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Literature summary extracted from
- Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of type 2 diabetes (2009), Curr. Drug Targets, 10, 71-87.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.4.14.5 | medicine | dipeptidyl peptidase IV is a target for the treatment of type 2 diabetes mellitus | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.14.5 | ABT-279 | - |
Homo sapiens |  |
| 3.4.14.5 | AMG-222 | ALS-2-0426 | Homo sapiens | |
| 3.4.14.5 | ARI-2243 | - |
Homo sapiens | |
| 3.4.14.5 | ASP8497 | - |
Homo sapiens | |
| 3.4.14.5 | Bl-1356 | ondero or linagliptin, competitive, reversible, and long-lasting inhibition | Homo sapiens | |
| 3.4.14.5 | BMS-477118 | saxagliptin, the proprietary name is Onglyza, covalently bound and reversible inhibitor | Homo sapiens | |
| 3.4.14.5 | BMS-686117 | - |
Homo sapiens | |
| 3.4.14.5 | CR-14025 | - |
Homo sapiens | |
| 3.4.14.5 | des-fluoro-sitagliptin | sitagliptin analogue, reversible inhibition | Homo sapiens | |
| 3.4.14.5 | DP-893 | reversible inhibition | Homo sapiens | |
| 3.4.14.5 | E-3024 | - |
Homo sapiens | |
| 3.4.14.5 | ER-319711-15 | - |
Homo sapiens | |
| 3.4.14.5 | GRC 8200 | melogliptin | Homo sapiens | |
| 3.4.14.5 | GSK-823093C | denagliptin | Homo sapiens | |
| 3.4.14.5 | GW-1853 | - |
Homo sapiens | |
| 3.4.14.5 | IP-10.C8 | - |
Homo sapiens | |
| 3.4.14.5 | K-579 | reversibile and long-lasting inhibition | Homo sapiens | |
| 3.4.14.5 | KRP-104 | - |
Homo sapiens | |
| 3.4.14.5 | LAF-237 | vildagliptin, potent, selective DPP IV inhibitor, the proprietary name is Galvus, covalently bound and reversible inhibitor | Homo sapiens | |
| 3.4.14.5 | LC-150444 | reversible inhibition | Homo sapiens | |
| 3.4.14.5 | LY-2463665 | reversible inhibition | Homo sapiens | |
| 3.4.14.5 | MK-0431 | sitagliptin, potent, selective DPP IV inhibitor, the proprietary name is Januvia, reversible and long-lasting inhibition | Homo sapiens | |
| 3.4.14.5 | MP-513 | IDDBCP161883 | Homo sapiens | |
| 3.4.14.5 | NVP DPP728 | slow-binding inhibitor | Homo sapiens | |
| 3.4.14.5 | P32/P98 | isoleucine thiazolidide DPPIV, reversible inhibition | Homo sapiens | |
| 3.4.14.5 | PHX-1149 | dutogliptin tartrate, reversible inhibition | Homo sapiens | |
| 3.4.14.5 | PSN-9301 | P93/01, reversible inhibition, short acting | Homo sapiens | |
| 3.4.14.5 | PT-630 | - |
Homo sapiens | |
| 3.4.14.5 | R-1438 | aminomethylpyridine derivate | Homo sapiens | |
| 3.4.14.5 | R-1579 | carmegliptin, reversible inhibition | Homo sapiens | |
| 3.4.14.5 | RO-0730699 | - |
Homo sapiens | |
| 3.4.14.5 | S-40010 | - |
Homo sapiens | |
| 3.4.14.5 | SK-0403 | - |
Homo sapiens | |
| 3.4.14.5 | SSR-162369 | reversibile and long-lasting inhibition | Homo sapiens | |
| 3.4.14.5 | SYR-322 | 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, also called alogliptin or TAK-322, reversible inhibition | Homo sapiens | |
| 3.4.14.5 | TAK-100 | - |
Homo sapiens | |
| 3.4.14.5 | TRC-XXXX | - |
Homo sapiens | |
| 3.4.14.5 | TS-021 | - |
Homo sapiens | |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.14.5 | alpha1-microglobulin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | aprotinin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | beta-casomorphin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | bradykinin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | enterostatin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | gastrin releasing peptide + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | Glucagon + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | glucagon-like peptide 1 (7-36)-amide + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | glucagon-like peptide 1 (7-37) + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | glucagon-like peptide 2 (1-33) + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | glucose-dependent insulinotropic peptide + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | growth hormone releasing factor + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | growth hormone releasing hormone (1-29) + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | growth hormone releasing hormone (1-44) + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | human chorionic gonadotropin alpha + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | insulin-like growth factor-1 + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | interferon-gamma-inducible protein-10 + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | interleukin 1-beta + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | interleukin-2 + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | leutinising hormone alpha chain + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | macrophage-derived chemokine + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | monocyte chemotactic protein-1 + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | monocyte chemotactic protein-2 + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | neuropeptide Y + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | peptide YY (1-36) + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | pro-colipase + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | prolactin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | RANTES protein + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | stromal cell-derived factor 1alpha + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | stromal cell-derived factor 1beta + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | Substance P + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | thyrotropin + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | Trypsinogen + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | trypsinogen pro-peptide + H2O | Homo sapiens | - |
? | - |
? | |
| 3.4.14.5 | vasostatin-1 + H2O | Homo sapiens | - |
? | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.14.5 | Homo sapiens | - |
- |
- |
Posttranslational Modification
| EC Number | Posttranslational Modification | Comment | Organism |
|---|---|---|---|
| 3.4.14.5 | glycoprotein | - |
Homo sapiens |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.4.14.5 | blood plasma | - |
Homo sapiens | - |
| 3.4.14.5 | kidney | highly expressed in kidney | Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.14.5 | alpha1-microglobulin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | aprotinin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | beta-casomorphin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | bradykinin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | enterostatin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | gastrin releasing peptide + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | Glucagon + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | glucagon-like peptide 1 (7-36)-amide + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | glucagon-like peptide 1 (7-37) + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | glucagon-like peptide 2 (1-33) + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | glucose-dependent insulinotropic peptide + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | growth hormone releasing factor + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | growth hormone releasing hormone (1-29) + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | growth hormone releasing hormone (1-44) + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | human chorionic gonadotropin alpha + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | insulin-like growth factor-1 + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | interferon-gamma-inducible protein-10 + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | interleukin 1-beta + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | interleukin-2 + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | leutinising hormone alpha chain + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | macrophage-derived chemokine + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | monocyte chemotactic protein-1 + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | monocyte chemotactic protein-2 + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | neuropeptide Y + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | peptide YY (1-36) + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | pro-colipase + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | prolactin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | RANTES protein + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | stromal cell-derived factor 1alpha + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | stromal cell-derived factor 1beta + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | Substance P + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | thyrotropin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | Trypsinogen + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | trypsinogen pro-peptide + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.14.5 | vasostatin-1 + H2O | - |
Homo sapiens | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.14.5 | dipeptidyl peptidase IV | - |
Homo sapiens |
| 3.4.14.5 | DPP IV | DPP IV has the preference for X-Pro over X-Ala, where X is any amino acid other than L-proline | Homo sapiens |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.14.5 | 0.0000001 | - |
R-1438 | - |
Homo sapiens | |
| 3.4.14.5 | 0.0000006 | - |
BMS-477118 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000001 | - |
ABT-279 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000001 | - |
Bl-1356 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000007 | - |
LY-2463665 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000009 | - |
MK-0431 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000011 | - |
NVP DPP728 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000017 | - |
LAF-237 | - |
Homo sapiens | |
| 3.4.14.5 | 0.000022 | - |
GSK-823093C | - |
Homo sapiens | |
| 3.4.14.5 | 0.00008 | - |
P32/P98 | - |
Homo sapiens | |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.4.14.5 | 0.000001 | - |
- |
Homo sapiens | Bl-1356 | |
| 3.4.14.5 | 0.00000135 | - |
- |
Homo sapiens | MP-513 | |
| 3.4.14.5 | 0.00000161 | - |
- |
Homo sapiens | GRC 8200 | |
| 3.4.14.5 | 0.0000035 | - |
- |
Homo sapiens | LAF-237 | |
| 3.4.14.5 | 0.0000037 | - |
- |
Homo sapiens | BMS-477118 | |
| 3.4.14.5 | 0.0000053 | - |
- |
Homo sapiens | ASP8497 | |
| 3.4.14.5 | 0.000007 | - |
- |
Homo sapiens | SYR-322 | |
| 3.4.14.5 | 0.000018 | - |
- |
Homo sapiens | SSR-162369 | |
| 3.4.14.5 | 0.000018 | - |
- |
Homo sapiens | MK-0431 | |
| 3.4.14.5 | 0.000022 | - |
- |
Homo sapiens | NVP DPP728 | |
| 3.4.14.5 | 0.000034 | - |
- |
Homo sapiens | LY-2463665 | |
| 3.4.14.5 | 0.000089 | - |
- |
Homo sapiens | ER-319711-15 | |
| 3.4.14.5 | 0.00042 | - |
- |
Homo sapiens | P32/P98 | |
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