Target General Infomation
Target ID
T31391 (Former ID: TTDS00093)
Target Name
Dipeptidyl peptidase 4 (DPP-4)
Synonyms
Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP
Gene Name
DPP4
Target Type
Successful target
[1]
Disease [+] 2 Target-related Diseases +
1 Acute diabete complication [ICD-11: 5A2Y]
2 Type 2 diabetes mellitus [ICD-11: 5A11]
Function
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. Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline. Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation.
BioChemical Class
Peptidase
UniProt ID
DPP4_HUMAN
EC Number
EC 3.4.14.5
Sequence
MKTPWKVLLGLLGAAALVTIITVPVVLLNKGTDDATADSRKTYTLTDYLKNTYRLKLYSL
RWISDHEYLYKQENNILVFNAEYGNSSVFLENSTFDEFGHSINDYSISPDGQFILLEYNY
VKQWRHSYTASYDIYDLNKRQLITEERIPNNTQWVTWSPVGHKLAYVWNNDIYVKIEPNL
PSYRITWTGKEDIIYNGITDWVYEEEVFSAYSALWWSPNGTFLAYAQFNDTEVPLIEYSF
YSDESLQYPKTVRVPYPKAGAVNPTVKFFVVNTDSLSSVTNATSIQITAPASMLIGDHYL
CDVTWATQERISLQWLRRIQNYSVMDICDYDESSGRWNCLVARQHIEMSTTGWVGRFRPS
EPHFTLDGNSFYKIISNEEGYRHICYFQIDKKDCTFITKGTWEVIGIEALTSDYLYYISN
EYKGMPGGRNLYKIQLSDYTKVTCLSCELNPERCQYYSVSFSKEAKYYQLRCSGPGLPLY
TLHSSVNDKGLRVLEDNSALDKMLQNVQMPSKKLDFIILNETKFWYQMILPPHFDKSKKY
PLLLDVYAGPCSQKADTVFRLNWATYLASTENIIVASFDGRGSGYQGDKIMHAINRRLGT
FEVEDQIEAARQFSKMGFVDNKRIAIWGWSYGGYVTSMVLGSGSGVFKCGIAVAPVSRWE
YYDSVYTERYMGLPTPEDNLDHYRNSTVMSRAENFKQVEYLLIHGTADDNVHFQQSAQIS
KALVDVGVDFQAMWYTDEDHGIASSTAHQHIYTHMSHFIKQCFSLP
Drugs and Modes of Action
Approved Drug(s) [+] 8 Approved Drugs +
1 Alogliptin Drug Info Approved Type-2 diabetes [2], [3], [4]
2 Anagliptin Drug Info Approved Type-2 diabetes [4], [5], [6]
3 Dapagliflozin Propanediol; Saxagliptin Hydrochloride Drug Info Approved Type-2 diabetes [7], [4]
4 Kombiglyze XR/Komboglyze FDC Drug Info Approved Diabetic complication [8]
5 Linagliptin Drug Info Approved Type-2 diabetes [9], [10]
6 Saxagliptin Drug Info Approved Type-2 diabetes [4], [11], [12]
7 Sitagliptin Drug Info Approved Type-2 diabetes [4], [13], [14], [15]
8 Vildagliptin Drug Info Approved Type-2 diabetes [16], [17]
Clinical Trial Drug(s) [+] 21 Clinical Trial Drugs +
1 Dutogliptin Drug Info Phase 3 Type-2 diabetes [18]
2 Gemigliptin Drug Info Phase 3 Diabetic complication [19]
3 IDDBCP161883 Drug Info Phase 3 Type-2 diabetes [20]
4 LC-150444 Drug Info Phase 3 Type-2 diabetes [21]
5 MK-3102 Drug Info Phase 3 Type-2 diabetes [22], [23]
6 SAND-26 Drug Info Phase 3 Autoimmune diabetes [24], [25]
7 SaxaDapa FDC Drug Info Phase 3 Diabetic complication [26], [27]
8 SYR-472 Drug Info Phase 3 Metabolic disorder [28]
9 Denagliptin Drug Info Phase 2/3 Type-2 diabetes [29]
10 IP10 C8 Drug Info Phase 2 Psoriasis vulgaris [30]
11 IP10.C8-1 Drug Info Phase 2 Psoriasis vulgaris [30]
12 KRP-104 Drug Info Phase 2 Type-2 diabetes [31]
13 Melogliptin Drug Info Phase 2 Type-2 diabetes [32]
14 P32/98 Drug Info Phase 2 Autism spectrum disorder [33]
15 PF-00734200 Drug Info Phase 2 Type-2 diabetes [34], [35]
16 YSCMA Drug Info Phase 1/2 Haematological malignancy [36]
17 ARI-2243 Drug Info Phase 1 Type-2 diabetes [37]
18 DA-1229 Drug Info Phase 1 Type-2 diabetes [38]
19 REC-01 Drug Info Phase 1 Acute myocardial infarction [39]
20 Teneligliptin Drug Info Phase 1 Type-2 diabetes [40], [4]
21 ZYDPLA 1 Drug Info Phase 1 Type-2 diabetes [4]
Discontinued Drug(s) [+] 11 Discontinued Drugs +
1 ALS 2-0426 Drug Info Discontinued in Phase 2 Type-2 diabetes [41]
2 Isoleucine thiazolidide DPP IV Drug Info Discontinued in Phase 2 Type-2 diabetes [42]
3 NVP-DPP728 Drug Info Discontinued in Phase 2 Type-2 diabetes [43]
4 PSN-9301 Drug Info Discontinued in Phase 2 Diabetic complication [44]
5 R-1438 Drug Info Discontinued in Phase 2 Type-2 diabetes [45]
6 TA-6666 Drug Info Discontinued in Phase 2 Type-2 diabetes [46]
7 ABT-279 Drug Info Discontinued in Phase 1 Type-2 diabetes [47]
8 SSR-162369 Drug Info Discontinued in Phase 1 Type-2 diabetes [48]
9 TAK-100 Drug Info Discontinued in Phase 1 Diabetic complication [49]
10 DSP-7238 Drug Info Terminated Diabetic complication [53]
11 PT-630 Drug Info Terminated Type-2 diabetes [54]
Preclinical Drug(s) [+] 3 Preclinical Drugs +
1 ASP8497 Drug Info Preclinical Type-2 diabetes [50]
2 ER-319711-15 Drug Info Preclinical Type-2 diabetes [51]
3 LY-2463665 Drug Info Preclinical Type-2 diabetes [52]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 136 Inhibitor drugs +
1 Alogliptin Drug Info [1], [17], [55]
2 Linagliptin Drug Info [59], [17]
3 Saxagliptin Drug Info [12], [17], [60]
4 Sitagliptin Drug Info [17], [61], [62], [63]
5 Vildagliptin Drug Info [17]
6 Dutogliptin Drug Info [64]
7 Gemigliptin Drug Info [65]
8 IDDBCP161883 Drug Info [66], [17]
9 LC-150444 Drug Info [67]
10 SYR-472 Drug Info [70], [1], [58]
11 Denagliptin Drug Info [17]
12 IP10.C8-1 Drug Info [30], [71]
13 Melogliptin Drug Info [17]
14 P32/98 Drug Info [33]
15 DA-1229 Drug Info [76]
16 REC-01 Drug Info [39]
17 ZYDPLA 1 Drug Info [4]
18 Aminopiperidine derivative 1 Drug Info [77]
19 Aminopiperidine derivative 2 Drug Info [77]
20 Beta-phe compound 1 Drug Info [77]
21 Beta-phe compound 2 Drug Info [77]
22 Beta-phe compound 3 Drug Info [77]
23 Dihydropyrrolopyrazole derivative 1 Drug Info [77]
24 Imidazo cyclohexylamine derivative 1 Drug Info [77]
25 Imidazo cyclohexylamine derivative 2 Drug Info [77]
26 Imidazo cyclohexylamine derivative 3 Drug Info [77]
27 Imidazo pyridine derivative 2 Drug Info [77]
28 Peptide analog 44 Drug Info [77]
29 Peptide analog 45 Drug Info [77]
30 Peptide analog 46 Drug Info [77]
31 Peptide analog 47 Drug Info [77]
32 Peptide analog 48 Drug Info [77]
33 Peptide analog 49 Drug Info [77]
34 Peptide analog 50 Drug Info [77]
35 Peptide analog 51 Drug Info [77]
36 PMID25482888-Compound-11 Drug Info [77]
37 PMID25482888-Compound-12 Drug Info [77]
38 PMID25482888-Compound-13 Drug Info [77]
39 PMID25482888-Compound-14 Drug Info [77]
40 PMID25482888-Compound-15 Drug Info [77]
41 PMID25482888-Compound-16 Drug Info [77]
42 PMID25482888-Compound-17 Drug Info [77]
43 PMID25482888-Compound-18 Drug Info [77]
44 PMID25482888-Compound-21 Drug Info [77]
45 PMID25482888-Compound-34 Drug Info [77]
46 PMID25482888-Compound-37 Drug Info [77]
47 PMID25482888-Compound-38 Drug Info [77]
48 PMID25482888-Compound-50 Drug Info [77]
49 PMID25482888-Compound-52 Drug Info [77]
50 PMID25482888-Compound-56 Drug Info [77]
51 PMID25482888-Compound-6 Drug Info [77]
52 PMID25482888-Compound-69 Drug Info [77]
53 PMID25482888-Compound-70 Drug Info [77]
54 PMID25482888-Compound-71 Drug Info [77]
55 PMID25482888-Compound-72 Drug Info [77]
56 Pyrimidine derivative 30 Drug Info [77]
57 Pyrimidine derivative 31 Drug Info [77]
58 Pyrimidine derivative 32 Drug Info [77]
59 Pyrimidine derivative 33 Drug Info [77]
60 Pyrimidinedione derivative 1 Drug Info [77]
61 Pyrrolo[1,2-f]triazine derivative 1 Drug Info [77]
62 Pyrrolo[1,2-f]triazine derivative 2 Drug Info [77]
63 Quinazoline derivative 1 Drug Info [77]
64 Thiomorpholine derivative 1 Drug Info [77]
65 Thiomorpholine derivative 2 Drug Info [77]
66 Triazole piperazine derivative 1 Drug Info [77]
67 Triazolo-pyrimidinedione derivative 1 Drug Info [77]
68 Triazolo-pyrimidinedione derivative 2 Drug Info [77]
69 Tricyclic heterocycle derivative 6 Drug Info [77]
70 Xanthine derivative 1 Drug Info [77]
71 Xanthine/amino piperidine compound 1 Drug Info [77]
72 ALS 2-0426 Drug Info [78]
73 Isoleucine thiazolidide DPP IV Drug Info [17]
74 NVP-DPP728 Drug Info [79]
75 PSN-9301 Drug Info [80]
76 R-1438 Drug Info [17]
77 TA-6666 Drug Info [81]
78 ABT-279 Drug Info [17]
79 SSR-162369 Drug Info [17]
80 TAK-100 Drug Info [1]
81 ASP8497 Drug Info [17]
82 ER-319711-15 Drug Info [17]
83 LY-2463665 Drug Info [17]
84 DSP-7238 Drug Info [58]
85 (+/-)-6-(2-chlorophenyl)cyclohex-3-enamine Drug Info [82]
86 (1-phenylcyclopentyl)methanamine Drug Info [83], [84]
87 (1R,2R)-1,2-diphenylethane-1,2-diamine Drug Info [84]
88 (1R,2S)-1,2-diphenylethane-1,2-diamine Drug Info [84]
89 (2-(2-chlorophenyl)pyridin-3-yl)methanamine Drug Info [84]
90 (2-chloro-6-phenoxyphenyl)methanamine Drug Info [84]
91 (2s)-Pyrrolidin-2-Ylmethylamine Drug Info [85]
92 (3S,4R)-3-butyl-1-phenylpiperidin-4-amine Drug Info [86]
93 (5-phenyl-3H-benzo[d]imidazol-4-yl)methanamine Drug Info [87]
94 (R)-1-(2-aminoacetyl)pyrrolidin-2-ylboronic acid Drug Info [88]
95 (S)-2-Amino-1-azetidin-1-yl-2-cyclohexyl-ethanone Drug Info [89]
96 (S)-2-Amino-1-thiazolidin-3-yl-propane-1-thione Drug Info [90]
97 (S)-pyrrolidin-1-yl(pyrrolidin-2-yl)methanone Drug Info [91]
98 (S)-pyrrolidin-2-yl(thiazolidin-3-yl)methanone Drug Info [92]
99 1-benzhydryl-3-butylpiperidin-4-amine Drug Info [86]
100 1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine Drug Info [93]
101 1-biphenyl-2-ylmethanamine Drug Info [83]
102 2-(2-chlorophenyl)-2-morpholinoethanamine Drug Info [84]
103 2-Amino-3-Methyl-1-Pyrrolidin-1-Yl-Butan-1-One Drug Info [94]
104 3-butyl-1-(naphthalen-1-yl)piperidin-4-amine Drug Info [86]
105 4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine Drug Info [93]
106 4-(2,4-dichlorophenyl)-1-tosylpyrrolidin-3-amine Drug Info [93]
107 4-iodophenyl-alaninyl-(S)-2-cyano-pyrrolidine Drug Info [95]
108 ABT-341 Drug Info [82]
109 Alpha-D-Mannose Drug Info [94]
110 ASC-201 Drug Info [58]
111 BPI-711001 Drug Info [58]
112 C-(2'-Chloro-biphenyl-2-yl)-methylamine Drug Info [84]
113 Cyclohexylglycine-(2S)-cyanopyrrolidine Drug Info [96]
114 D-420720 Drug Info [58]
115 D-Val-L-boroPro Drug Info [97]
116 DB-160 Drug Info [58]
117 Diisopropylphosphono Group Drug Info [94]
118 Dipeptidyl peptidase IV inhibitors Drug Info [58]
119 DIPROTIN A Drug Info [98]
120 DPP-IV inhibitors, Phenomix Drug Info [58]
121 DPP-IV inhibitors, Santhera Drug Info [58]
122 DPP-IV inhibitors, Toray Drug Info [58]
123 EMC-0901 Drug Info [58]
124 FE 999011 Drug Info [100]
125 Fucose Drug Info [94]
126 Iodo-Phenylalanine Drug Info [94]
127 KR-62436 Drug Info [101]
128 L-Ala-L-boroPro Drug Info [97]
129 L-Val-L-boroPro Drug Info [97]
130 N-alkyl Gly-boro-Pro derivative Drug Info [102]
131 N-isoleucylthiazolidine Drug Info [96]
132 N4-(4-chlorobenzyl)-2,4-diaminobutanoylpiperidine Drug Info [103]
133 PK-44 Drug Info [58]
134 PMID20684603C24dd Drug Info [104]
135 Retagliptin Drug Info [58]
136 TRC-8XXX series Drug Info [58]
Modulator [+] 12 Modulator drugs +
1 Anagliptin Drug Info [56]
2 Dapagliflozin Propanediol; Saxagliptin Hydrochloride Drug Info [57]
3 Kombiglyze XR/Komboglyze FDC Drug Info [58]
4 MK-3102 Drug Info [68]
5 SaxaDapa FDC Drug Info [26], [27]
6 IP10 C8 Drug Info [30]
7 KRP-104 Drug Info [72]
8 PF-00734200 Drug Info [73]
9 ARI-2243 Drug Info [75]
10 Teneligliptin Drug Info [58]
11 PT-630 Drug Info [57]
12 E-3024 Drug Info [99]
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 1 KEGG Pathways +
1 Protein digestion and absorption
NetPath Pathway [+] 2 NetPath Pathways +
1 IL2 Signaling Pathway
2 TGF_beta_Receptor Signaling Pathway
Target-Related Models and Studies
Target Validation
References
REF 1 Clinical pipeline report, company report or official report of Takeda (2009).
REF 2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6319).
REF 3 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
REF 4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 6 ClinicalTrials.gov (NCT02330406) Randomized Evaluation of Anagliptin Versus Sitagliptin On Low-density lipoproteiN Cholesterol in Diabetes Trial. U.S. National Institutes of Health.
REF 7 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2018
REF 8 KOMBIGLYZE XR tablets approved in the US for the treatment of type 2 diabetes mellitus in adults
REF 9 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6318).
REF 10 Clinical pipeline report, company report or official report of Boehringer Ingelheim.
REF 11 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6316).
REF 12 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
REF 13 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6286).
REF 14 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022044.
REF 15 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
REF 16 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6310).
REF 17 Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87.
REF 18 ClinicalTrials.gov (NCT00690638) Safety and Efficacy Study of Dutogliptin/PHX1149T to Treat Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
REF 19 ClinicalTrials.gov (NCT01990469) Efficacy and Safety of Gemigliptin 50mg qd Added in Patients With Type 2 Diabetes Inadequately Controlled on Glimepiride and Metformin. U.S. National Institutes of Health.
REF 20 ClinicalTrials.gov (NCT01798238) Teneligliptin(MP-513) Versus Placebo in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
REF 21 ClinicalTrials.gov (NCT02089126) Phase III Trial to Evaluate the Efficacy and Safety of Gemigliptin 50mg qd Added to Ongoing Glimepiride as Fix-dose Combination in Patients With Type 2 Diabetes. U.S.National Institutes of Health.
REF 22 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8402).
REF 23 ClinicalTrials.gov (NCT01703208) A Study to Assess Cardiovascular Outcomes Following Treatment With MK-3102 in Participants With Type 2 Diabetes Mellitus (MK-3102-018). U.S. National Institutes of Health.
REF 24 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8691).
REF 25 ClinicalTrials.gov (NCT02411084) Study of BEGEDINA vs "Conventional Treatment" for Treating Steroid-Resistant Acute GvHD. U.S. National Institutes of Health.
REF 26 Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for type 2 diabetes. Cardiol Rev. 2010 Jul-Aug;18(4):213-7.
REF 27 The novel sodium glucose transporter 2 inhibitor dapagliflozin sustains pancreatic function and preserves islet morphology in obese, diabetic rats. Diabetes Obes Metab. 2010 Nov;12(11):1004-12.
REF 28 Clinical pipeline report, company report or official report of Takeda.
REF 29 ClinicalTrials.gov (NCT00387972) Study Of Denagliptin In Subjects With Type 2 Diabetes Mellitus (T2DM). U.S. National Institutes of Health.
REF 30 Recent insights into the role of dipeptidyl aminopeptidase IV (DPIV) and aminopeptidase N (APN) families in immune functions. Clin Chem Lab Med. 2009;47(3):253-61.
REF 31 ClinicalTrials.gov (NCT00525330) A Randomized, Double-Blind, Placebo-Controlled Study to Assess the Safety and Efficacy of KRP-104 in Patients With Type 2 Diabetes Inadequately Controlled on Metformin Alone. U.S. National Institutes of Health.
REF 32 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021640)
REF 33 Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and beta-cell glucose responsiveness in VDF (fa/fa) Zucker rats. Diabetes. 2002 Apr;51(4):943-50.
REF 34 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7413).
REF 35 ClinicalTrials.gov (NCT00473525) 12 Week Study Of PF-00734200 For The Treatment Of Type 2 Diabetes Mellitus In Subjects Treated With Metformin. U.S. National Institutes of Health.
REF 36 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031210)
REF 37 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028500)
REF 38 ClinicalTrials.gov (NCT00961025) A Study to Characterize the Pharmacokinetics/Pharmacodynamics and Effect of Food of DA-1229 in Healthy Male Subjects. U.S. National Institutes of Health.
REF 39 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 40 ClinicalTrials.gov (NCT02449330) Teneligliptin on the Progressive Left Ventricular Diastolic Dysfunction With Type 2 Diabetes Mellitus Study.
REF 41 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022304)
REF 42 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014308)
REF 43 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012640)
REF 44 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019065)
REF 45 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018193)
REF 46 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020875)
REF 47 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025075)
REF 48 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022199)
REF 49 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028364)
REF 50 ASP8497 is a novel selective and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity. Biochem Pharmacol. 2008 Jul 1;76(1):98-107.
REF 51 7-But-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin-8-one is a novel competitive and selective inhibitor of dipeptidyl pepti... J Pharmacol Exp Ther. 2006 Dec;319(3):1253-7.
REF 52 Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem. 2012 Oct 1;20(19):5705-19.
REF 53 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028616)
REF 54 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022168)
REF 55 Combining a dipeptidyl peptidase-4 inhibitor, alogliptin, with pioglitazone improves glycaemic control, lipid profiles and beta-cell function in db... Br J Pharmacol. 2009 Jun;157(3):415-26.
REF 56 Diabetes Treatment. Diabetes Care. 2009 March; 32(3): e25-e30.
REF 57 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 58 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1612).
REF 59 Boehringer Ingelheim. Product Development Pipeline. June 2 2009.
REF 60 Clinical pipeline report, company report or official report of AstraZeneca (2009).
REF 61 Novel therapeutics for type 2 diabetes: incretin hormone mimetics (glucagon-like peptide-1 receptor agonists) and dipeptidyl peptidase-4 inhibitors. Pharmacol Ther. 2009 Oct;124(1):113-38.
REF 62 Dipeptidyl peptidase IV (CD 26) gene expression in enterocyte-like colon cancer cell lines HT-29 and Caco-2. Cloning of the complete human coding sequence and changes of dipeptidyl peptidase IV mRNA levels during cell differentiation. J Biol Chem. 1992 Mar 5;267(7):4824-33.
REF 63 Cloning and functional expression of the T cell activation antigen CD26. J Immunol. 1992 Jul 15;149(2):481-6.
REF 64 Dutogliptin, a selective DPP4 inhibitor, improves glycaemic control in patients with type 2 diabetes: a 12-week, double-blind, randomized, placebo-controlled, multicentre trial. Diabetes Obes Metab. 2010 Apr;12(4):348-55.
REF 65 Evaluation of the pharmacokinetics of the DPP-4 inhibitor gemigliptin when coadministered with rosuvastatin or irbesartan to healthy subjects. Curr Med Res Opin. 2015 Feb;31(2):229-41.
REF 66 Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes. Diabetes Metab Syndr Obes. 2013 May 6;6:187-95.
REF 67 Clinical pipeline report, company report or official report of ShangHai APIs Chemical.
REF 68 Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12.
REF 69 Clinical pipeline report, company report or official report of Siesonline.
REF 70 SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Diabetes Endocrinol. 2014 Feb;2(2):125-32.
REF 71 ClinicalTrials.gov (NCT00824980) Combined Inhibition of Dipeptidyl Peptidase IV (DPIV/CD26) and Aminopeptidase N (APN/CD13) in the Treatment of Psoriasis. U.S. National Institutes of Health.
REF 72 Clinical pipeline report, company report or official report of Activx.
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