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Structure for peptidase S09.003: dipeptidyl-peptidase IV (eukaryote)

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

 

PDB Organism Resolution Comment
1N1M_A Homo sapiens 2.50 Å complex with inhibitor 2-amino-3-methyl-1-pyrrolidin-1-yl-butan-1-one
One peptidase molecule is shown. Catalytic residues are shown in ball-and-stick representation: Ser630 in orange, Asp708 in pink and His740 in purple.
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TERTIARY STRUCTURE DATA
Comment Resolution PDB PDBe SCOP CATH PDBSum Proteopedia Reference
Homo sapiens
mature  peptidase 2.60 Å 1J2E 1J2E 1J2E 1J2E 1J2E 1J2E Hiramatsu et al., 2003
complex with inhibitor 2-amino-3-methyl-1-pyrrolidin-1-yl-butan-1-one 2.50 Å 1N1M 1N1M 1N1M 1N1M 1N1M 1N1M Rasmussen et al., 2003
mature  peptidase 2.10 Å 1NU6 1NU6 1NU6 1NU6 1NU6 1NU6 Thoma et al., 2003
complex with diprotin A 2.50 Å 1NU8 1NU8 1NU8 1NU8 1NU8 1NU8 Thoma et al., 2003
apo form 1.90 Å 1PFQ 1PFQ 1PFQ 1PFQ 1PFQ 1PFQ Oefner et al., 2003
mature  peptidase 2.10 Å 1R9M 1R9M 1R9M 1R9M 1R9M 1R9M Aertgeerts et al., 2004
complex with a decapeptide (TNPY) 2.30 Å 1R9N 1R9N 1R9N 1R9N 1R9N 1R9N Aertgeerts et al., 2004
complex with 5-aminomethyl- 6-(2,4-dichloro-phenyl)-2-(3,5-dimethoxy-phenyl)-pyrimidin- 4-ylamine 2.20 Å 1RWQ 1RWQ 1RWQ 1RWQ 1RWQ 1RWQ Peters et al., 2004
apo form 2.00 Å 1TK3 1TK3 1TK3 1TK3 1TK3 1TK3 Bjelke et al., 2004
human dipeptidyl peptidase iv/cd26 inhibited with diisopropyl fluorophosphate 2.70 Å 1TKR 1TKR 1TKR 1TKR 1TKR 1TKR Bjelke et al., 2004
human dipeptidyl peptidase iv/cd26 mutant y547f 2.20 Å 1U8E 1U8E 1U8E 1U8E 1U8E 1U8E Bjelke et al., 2004
complex with adenosine deaminase 3.03 Å 1W1I 1W1I 1W1I 1W1I 1W1I 1W1I Weihofen et al., 2004
complex with diprotin A 2.20 Å 1WCY 1WCY 1WCY 1WCY 1WCY 1WCY Hiramatsu et al., 2004
complex with sitagliptin 2.10 Å 1X70 1X70 1X70 1X70 1X70 1X70 Kim et al., 2005
x-ray structure of novel biaryl-based dipeptidyl peptidase iv inhibitor 2.50 Å 2AJL 2AJL 2AJL 2AJL 2AJL 2AJL Qiao et al., 2006
hiv-1 tat protein derived n-terminal nonapeptide trp2-tat (1-9) bound to the active site of dipeptidyl peptidase iv (cd26) 3.15 Å 2BGN 2BGN 2BGN 2BGN 2BGN 2BGN Weihofen et al., 2005
complex with HIV-1TAT derived nonapeptides TAT(1- 9) 2.00 Å 2BGR 2BGR 2BGR 2BGR 2BGR 2BGR Weihofen et al., 2005
complex with N-((2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-ylmethyl)benzamide 2.66 Å 2BUB 2BUB 2BUB 2BUB 2BUB 2BUB Nordhoff et al., 2006
complex with 6-(4-(1S,2S)-2-amino-1-[(dimethylamino)carbonyl]-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropylphenyl)-1H-[1,2,4]triazolo[1,5-A]pyridin-4-ium 2.40 Å 2FJP 2FJP 2FJP 2FJP 2FJP 2FJP Edmondson et al., 2006
complex with cyanopyrrolidine (C5-Pro-Pro) inhibitor 21AC 2.40 Å 2G5P 2G5P 2G5P 2G5P 2G5P 2G5P Pei et al., 2006
complex with cyanopyrrolidine (C5-Pro-Pro) inhibitor 21AG 2.30 Å 2G5T 2G5T 2G5T 2G5T 2G5T 2G5T Pei et al., 2006
complex with cyanopyrrolidine (C5-Pro-Pro) inhibitor 24B 2.00 Å 2G63 2G63 2G63 2G63 2G63 2G63 Pei et al., 2006
complex with (2S,3S)-3-3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl-1-oxo-1-pyrrolidin-1-ylbutan-2-amine 2.35 Å 2HHA 2HHA 2HHA 2HHA 2HHA 2HHA Xu et al., 2006
complex with potent alkynyl cyanopyrrolidine (ABT-279) 2.40 Å 2I03 2I03 2I03 2I03 2I03 2I03 Madar et al., 2006
complex with ABT-341, a cyclohexene-constrained phenethylamine inhibitor 2.50 Å 2I78 2I78 2I78 2I78 2I78 2I78
complex with (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one 2.35 Å 2IIT 2IIT 2IIT 2IIT 2IIT 2IIT Biftu et al., 2007
complex with (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one 2.15 Å 2IIV 2IIV 2IIV 2IIV 2IIV 2IIV Biftu et al., 2007
complex with 1-(3,4- dimethoxy-phenyl)-3-m-tolyl-piperidine-4-ylamine 2.80 Å 2JID 2JID 2JID 2JID 2JID 2JID Lubbers et al., 2007
complex with pyrrolidine-constrained phenethylamine 29G 2.30 Å 2OAG 2OAG 2OAG 2OAG 2OAG 2OAG Backes et al., 2007
complex with Lilly aryl ketone inhibitor 4-[(3R)-3-[2-(4-fluorophenyl)-2-oxoethyl]aminobutyl]benzamide 2.10 Å 2OGZ 2OGZ 2OGZ 2OGZ 2OGZ 2OGZ Sheehan et al., 2007
complex with cyclic hydrazine (2R)-4-(2-benzoyl-1,2-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine 2.40 Å 2OLE 2OLE 2OLE 2OLE 2OLE 2OLE Ahn et al., 2007
mature  peptidase 2.55 Å 2ONC 2ONC 2ONC 2ONC 2ONC 2ONC Feng et al., 2007
complex with alpha amino acid inhibitor N-(trans-4-(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin- 1-yl]-1-methyl-3-oxopropylcyclohexyl)-N-methylacetamide 2.40 Å 2OPH 2OPH 2OPH 2OPH 2OPH 2OPH Duffy et al., 2007
human dipeptidyl peptidase iv (dpp4) with piperidinone- constrained phenethylamine 2.80 Å 2OQI 2OQI 2OQI 2OQI 2OQI 2OQI Pei et al., 2007
human dipeptidyl peptidase iv (dpp4) with piperidine- constrained phenethylamine 2.80 Å 2OQV 2OQV 2OQV 2OQV 2OQV 2OQV Pei et al., 2007
complex with cyclohexalamine inhibitor (1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-A]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine 2.20 Å 2P8S 2P8S 2P8S 2P8S 2P8S 2P8S Biftu et al., 2007
complex with inhibitor pzf 2.20 Å 2QJR 2QJR 2QJR 2QJR 2QJR 2QJR
complex structure of dipeptidyl peptidase iv and a oxadiazolyl ketone 3.10 Å 2QKY 2QKY 2QKY 2QKY 2QKY 2QKY Koo et al., 2007
complex with a triazolopiperazine-based beta amino acid inhibitor 2.30 Å 2QOE 2QOE 2QOE 2QOE 2QOE 2QOE Kowalchick et al., 2007
complex with (2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-(trans-4-[1,2,4]triazolo[1,5-A]pyridin-5-ylcyclohexyl)butanamide 2.10 Å 2QT9 2QT9 2QT9 2QT9 2QT9 2QT9 Kaelin et al., 2007
complex with (2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(trans-4-[1,2,4]triazolo[1,5-A]pyridin-6-ylcyclohexyl)butanamide 2.25 Å 2QTB 2QTB 2QTB 2QTB 2QTB 2QTB Kaelin et al., 2007
complex with 8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn- 1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]- 3,7-dihydro-1H-purine-2,6-dione 2.60 Å 2RGU 2RGU 2RGU 2RGU 2RGU 2RGU Eckhardt et al., 2007
complex with (3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinoxalin- 2-ylcarbonyl)pyrrolidin-3-amine 2.90 Å 2RIP 2RIP 2RIP 2RIP 2RIP 2RIP Corbett et al., 2007
complex with (1S,3S, 5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1- yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile 2.35 Å 3BJM 3BJM 3BJM 3BJM 3BJM 3BJM Metzler et al., 2008
complex with (2S,3S)-4-cyclopropyl-3-(3R,5R)-3-[2-fluoro- 4-(methylsulfonyl)phenyl]-1,2,4-oxadiazolidin- 5-yl-1-[(3S)-3-fluoropyrrolidin-1-yl]-1- oxobutan-2-amine 2.30 Å 3C43 3C43 3C43 3C43 3C43 3C43 Edmondson et al., 2008
complex with (2S,3S)-3-3-[2-chloro-4-(methylsulfonyl)phenyl]- 1,2,4-oxadiazol-5-yl-1-cyclopentylidene- 4-cyclopropyl-1-fluorobutan-2-amine 2.05 Å 3C45 3C45 3C45 3C45 3C45 3C45 Edmondson et al., 2008
complex with 1-biphenyl-2-ylmethanamine 2.49 Å 3CCB 3CCB 3CCB 3CCB 3CCB 3CCB Wallace et al., 2008
complex with 7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl- 1H-benzimidazole-5-carbonitrile 2.71 Å 3CCC 3CCC 3CCC 3CCC 3CCC 3CCC Wallace et al., 2008
4'-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]biphenyl- 3-carboxamide 2.00 Å 3D4L 3D4L 3D4L 3D4L 3D4L 3D4L Liang et al., 2008
crystal structure analysis of dppiv inhibitor 2.00 Å 3EIO 3EIO 3EIO 3EIO 3EIO 3EIO Ahn et al., 2008
mature  peptidase 2.43 Å 3F8S 3F8S 3F8S 3F8S 3F8S 3F8S Ammirati et al., 2009
mature  peptidase 2.25 Å 3G0B 3G0B 3G0B 3G0B 3G0B 3G0B Zhang et al., 2011
mature  peptidase 2.69 Å 3G0C 3G0C 3G0C 3G0C 3G0C 3G0C Zhang et al., 2011
mature  peptidase 2.39 Å 3G0D 3G0D 3G0D 3G0D 3G0D 3G0D Zhang et al., 2011
mature  peptidase 2.45 Å 3G0G 3G0G 3G0G 3G0G 3G0G 3G0G Zhang et al., 2011
complex with a reversed amide inhibitor 2.66 Å 3H0C 3H0C 3H0C 3H0C 3H0C 3H0C
mature  peptidase 2.10 Å 3HAB 3HAB 3HAB 3HAB 3HAB 3HAB Edmondson et al., 2009
mature  peptidase 2.00 Å 3HAC 3HAC 3HAC 3HAC 3HAC 3HAC Edmondson et al., 2009
mature  peptidase 2.40 Å 3KWF 3KWF 3KWF 3KWF 3KWF 3KWF Mattei et al., 2010
mature  peptidase 2.80 Å 3KWJ 3KWJ 3KWJ 3KWJ 3KWJ 3KWJ Boehringer et al., 2010
mature  peptidase 2.34 Å 3NOX 3NOX 3NOX 3NOX 3NOX 3NOX Meng et al., 2010
mature  peptidase 2.85 Å 3O95 3O95 3O95 3O95 3O95 3O95 Miyamoto et al., 2011
mature  peptidase 2.75 Å 3O9V 3O9V 3O9V 3O9V 3O9V 3O9V Miyamoto et al., 2011
mature  peptidase 2.70 Å 3OC0 3OC0 3OC0 3OC0 3OC0 3OC0 Mattei et al., 2010
mature  peptidase 2.72 Å 3OPM 3OPM 3OPM 3OPM 3OPM 3OPM Banno et al., 2011
mature  peptidase 2.40 Å 3Q0T 3Q0T 3Q0T 3Q0T 3Q0T 3Q0T
mature  peptidase 3.64 Å 3Q8W 3Q8W 3Q8W 3Q8W 3Q8W 3Q8W
mature  peptidase 2.21 Å 3QBJ 3QBJ 3QBJ 3QBJ 3QBJ 3QBJ
mature  peptidase 2.00 Å 3SWW 3SWW 3SWW 3SWW 3SWW 3SWW Wang et al., 2011
mature  peptidase 2.60 Å 3SX4 3SX4 3SX4 3SX4 3SX4 3SX4 Wang et al., 2011
mature  peptidase 2.49 Å 3VJK 3VJK 3VJK 3VJK 3VJK 3VJK Yoshida et al., 2012
mature  peptidase 2.39 Å 3VJL 3VJL 3VJL 3VJL 3VJL 3VJL Yoshida et al., 2012
mature  peptidase 2.10 Å 3VJM 3VJM 3VJM 3VJM 3VJM 3VJM Yoshida et al., 2012
mature  peptidase 2.36 Å 3W2T 3W2T 3W2T 3W2T 3W2T 3W2T Nabeno et al., 2013
mature  peptidase 2.85 Å 3WQH 3WQH 3WQH 3WQH 3WQH 3WQH Watanabe et al., 2015
mature  peptidase 1.62 Å 4A5S 4A5S 4A5S 4A5S 4A5S 4A5S Sutton et al., 2012
mature  peptidase 3.25 Å 4DSA 4DSA 4DSA 4DSA 4DSA 4DSA
mature  peptidase 3.20 Å 4DSZ 4DSZ 4DSZ 4DSZ 4DSZ 4DSZ
mature  peptidase 3.00 Å 4DTC 4DTC 4DTC 4DTC 4DTC 4DTC
mature  peptidase 2.90 Å 4G1F 4G1F 4G1F 4G1F 4G1F 4G1F Lam et al., 2012
mature  peptidase 3.20 Å 4J3J 4J3J 4J3J 4J3J 4J3J 4J3J Zhu et al., 2013
mature  peptidase 2.35 Å 4JH0 4JH0 4JH0 4JH0 4JH0 4JH0 Devasthale et al., 2013
mature  peptidase 2.70 Å 4KR0 4KR0 4KR0 4KR0 4KR0 4KR0
mature  peptidase 3.00 Å 4L72 4L72 4L72 4L72 4L72 4L72 Wang et al., 2013
mature  peptidase 2.43 Å 4LKO 4LKO 4LKO 4LKO 4LKO 4LKO Devasthale et al., 2013
mature  peptidase 1.65 Å 4N8D 4N8D 4N8D 4N8D 4N8D 4N8D Namoto et al., 2014
mature  peptidase 2.30 Å 4N8E 4N8E 4N8E 4N8E 4N8E 4N8E Namoto et al., 2014
mature  peptidase 1.90 Å 4PNZ 4PNZ 4PNZ 4PNZ 4PNZ 4PNZ Biftu et al., 2014
mature  peptidase 3.24 Å 4PV7 4PV7 4PV7 4PV7 4PV7 4PV7
mature  peptidase 2.59 Å 4QZV 4QZV 4QZV 4QZV 4QZV 4QZV Wang et al., 2014
complex with a novel tricyclic hetero-cycle inhibitor 1.95 Å 5I7U 5I7U 5I7U 5I7U 5I7U 5I7U
human dpp4 in complex with a novel 5,5,6-tricyclic pyrrolidine inhibitor 2.00 Å 5ISM 5ISM 5ISM 5ISM 5ISM 5ISM
complex with hl1 2.75 Å 5J3J 5J3J 5J3J 5J3J 5J3J 5J3J
complex with syr-472 2.24 Å 5KBY 5KBY 5KBY 5KBY 5KBY 5KBY
human dpp4 in complex with a ligand 34a 1.76 Å 5T4B 5T4B 5T4B 5T4B 5T4B 5T4B
human dpp4 in complex with ligand 19a 1.77 Å 5T4E 5T4E 5T4E 5T4E 5T4E 5T4E
human dpp4 in complex with ligand 34p 1.90 Å 5T4F 5T4F 5T4F 5T4F 5T4F 5T4F
human dpp4 in complex with ligand 34n 2.61 Å 5T4H 5T4H 5T4H 5T4H 5T4H 5T4H
complex with inhibitor3 3.00 Å 5Y7H 5Y7H 5Y7H 5Y7H 5Y7H 5Y7H
complex with inhibitor2 2.52 Å 5Y7J 5Y7J 5Y7J 5Y7J 5Y7J 5Y7J
complex with inhibitor1 2.51 Å 5Y7K 5Y7K 5Y7K 5Y7K 5Y7K 5Y7K
complex with hl2 3.00 Å 5ZID 5ZID 5ZID 5ZID 5ZID 5ZID
complex with vildagliptin 1.77 Å 6B1E 6B1E 6B1E 6B1E 6B1E 6B1E
complex with vildagliptin analog 1.91 Å 6B1O 6B1O 6B1O 6B1O 6B1O 6B1O
Rattus norvegicus
native dpp-iv (cd26) from rat 2.80 Å 2GBC 2GBC 2GBC 2GBC 2GBC 2GBC Longenecker et al., 2006
rat dpp-iv with alkynyl cyanopyrrolidine #1 3.10 Å 2GBF 2GBF 2GBF 2GBF 2GBF 2GBF Longenecker et al., 2006
rat dpp-iv with alkynyl cyanopyrrolidine #2 3.00 Å 2GBG 2GBG 2GBG 2GBG 2GBG 2GBG Longenecker et al., 2006
rat dpp-iv with xanthine inhibitor 4 3.30 Å 2GBI 2GBI 2GBI 2GBI 2GBI 2GBI Longenecker et al., 2006
rat dpp-iv with xanthine mimetic inhibitor #7 2.90 Å 2I3Z 2I3Z 2I3Z 2I3Z 2I3Z 2I3Z Kurukulasuriya et al., 2006
complex with thiazole-based peptide mimetic number 31 3.00 Å 2OAE 2OAE 2OAE 2OAE 2OAE 2OAE Backes et al., 2007
mature  peptidase 2.40 Å 4FFV 4FFV 4FFV 4FFV 4FFV 4FFV
mature  peptidase 2.90 Å 4FFW 4FFW 4FFW 4FFW 4FFW 4FFW
complex with a chemibody inhibitor 2.80 Å 5VTA 5VTA 5VTA 5VTA 5VTA 5VTA
Sus scrofa
mature  peptidase 1.80 Å 1ORV 1ORV 1ORV 1ORV 1ORV 1ORV Engel et al., 2003
complex with peptidomimetic inhibitor (2S)-pyrrolidin-2-ylmethylamine 2.84 Å 1ORW 1ORW 1ORW 1ORW 1ORW 1ORW Engel et al., 2003
complex with 7- benzyl-1,3-dimethyl-8-piperazin-1-yl-3,7-dihydro-purine-2, 6-dione (BDPX) 2.11 Å 2AJ8 2AJ8 2AJ8 2AJ8 2AJ8 2AJ8 Engel et al., 2006
complex with the tripeptide tert-butyl-Gly-L-Pro-L-Ile (tbu-GPI) 2.75 Å 2AJB 2AJB 2AJB 2AJB 2AJB 2AJB Engel et al., 2006
complex with 4-(2- aminoethyl)-benzene sulphonyl fluoride (AEBSF) 1.95 Å 2AJC 2AJC 2AJC 2AJC 2AJC 2AJC Engel et al., 2006
complex with L- Pro-boro-L-Pro (boroPro) 2.56 Å 2AJD 2AJD 2AJD 2AJD 2AJD 2AJD Engel et al., 2006
complex with 1-methylamine-1-benzyl-cyclopentane 2.56 Å 2BUA 2BUA 2BUA 2BUA 2BUA 2BUA Nordhoff et al., 2006
complex with (S)-2-[(R)-3-amino-4-(2-fluoro-phenyl)-butyryl]-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid amide 2.50 Å 2BUC 2BUC 2BUC 2BUC 2BUC 2BUC Nordhoff et al., 2006
porcine dipeptidyl peptidase iv in complex with 8-(3-aminopiperidin-1-yl)-7-[(2-bromophenyl)methyl]-1,3-dimethyl-2,3,6,7-tetrahydro-1h- purine-2,6-dione 2.41 Å 5LLS 5LLS 5LLS 5LLS 5LLS 5LLS

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