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